研究業績

研究業績　-Publication List-
@原著論文 (original papers) ＆ @解説・総説 (reviews), [TBA (to be announced)]

2024

原著論文：
14) Kaneko, K., Mieda, M., Jiang, Y., Takahashi, N., Kakeya, H. Tumescenamide C, a cyclic lipodepsipeptide from Streptomyces sp. KUSC_F05, exerts antimicrobial activity against the scab-forming actinomycete Streptomyces scabiei.J. Antibiot. in press, 2024. [selected as a highlight article.] [Press release]
13) Iseki, S.,# Ikeda, H.,# Kobayashi, S., Irie, K., Harada, H. Kakeya, H. Teleocidin B-4, a PKC activator, upregulates hypoxia-inducible factor 1 (HIF-1) activity by promoting the accumulation of HIF-1α protein via the PKCα/mTOR signaling pathway. (TBA) (#equal contribution)
12) Kishimoto, A., Komiyama, M., Wada, H., Satoh-Asahara, N., Yamakage, H., Aoyama, H., Katsuura, Y., Imaizumi, A., Hashimoto, T., Sunagawa, Y., Morimoto, T., Kanai, M., Kakeya, H., Hasegawa, K. Efficacy of highly bioavailable oral curcumin (curcuRougeⓇ) in asymptomatic or mild COVID-19 patients: A double-blind, randamized, placebo-controlled trial. (TBA)
11) Ozaki, M., Nakade, T., Shimotsuma, M., Ikeda, A., Kuranaga, T., Kakeya, H., Hirose, T. Simultaneous analysis of DL-amino acids in foods and beverages using a highly sensitive chiral resolution labeling reagent. (TBA)
10) Lu, S., Ren, L., Mao, D., Kakeya, H. Mechanistic study of the retro-aza-Michael reaction in saccharothriolide L: Identification of 2-amino-4-methylphenol as an effective protecting tool for the Michael acceptor. J. Antibiot. in press, 2024.
9) Hayashi, K., Takahashi, N., Furutani, Y., Toguchi, M., Shiozaki-Sato, Y., Sudoh, M., Kojima, S., Kakeya, H. (TBA)
8) Mao, D., Yu, P., Shinzato, N., Zhang, L., Zheng, W., Lu, S., Kakeya, H. Precezomysin, a novel antibiotic biosynthetic precursor of cezomycin, from actinomycete Kitasatospora putterlickiae 10-13. J. Antibiot. 77, 189-192, 2024.
7) Takahashi, S., Nakayama, J., Lu, S., Jiang, Y., Yamane, S., Nishimura, S., Hattori, A., Kakeya, H. (TBA)
6) Kakeya, H. (TBA)
5) Ishikawa, F., Konno, S., Kakeya, H., Tababe, G. Development of a chemical scaffold for inhibiting nonribosomal peptide synthetases in live bacterial cells. Beilstein J. Org. Chem. 20, 445-451, 2024.
4) Takenaka, K., Kaneko, K., Takahashi, N., Nishimura, S., Hattori, A. Kakeya, H. (TBA)
3) Konno, S., Ishikawa, F., Kakeya, H., Tanabe, G. Probing for optimal photoaffinity linkers of benzophenone-based photoaffinity probes for adenylating enzymes. (TBA)
2) Abe, T., Kishimoto, A., Katsuura, Y., Imaizumi, A., Hashimoto, T., Asakura, T., Minowa, H., Aoki, K., Kakeya, H., Kanai, M. (TBA)
1) Pan, C.,# Ikeda, H.,# Minote, M., Tokuda, T., Kuranaga, T. Taniguchi, T., Shinzato, N., Onaka, H., Kakeya, H. Amoxetamide A, a new anoikis inducer, produced by combined-culture of Amycolatopsis sp. and Tsukamurella pulmonis. J. Antibiot. 77, 66-70, 2024. (#equal contribution)
総説・著書：
2) 掛谷秀昭, 池田拓慧. 特集「学術研究支援の最先端」：ケミカルバイオロジーを機軸とした分子プロファイリング, 生体の科学, 2024. （2024年10月発刊予定）　　　　
1) 掛谷秀昭. 医薬品モダリティの開発を指向した天然物創薬ケミカルバイオロジー, 医薬品モダリティにおける創薬技術開発と展望. 情報機構, 2024. （2024年6月発刊予定）　　　　

2023

原著論文：
7) Pan, Y., Suzuki, T., Sakai, K., Hirano, Y., Ikeda, H., Hattori, A., Dohmae, N., Nishio, K., Kakeya, H. Bisabosqual A: a novel asparagine synthetase inhibitor suppressing the proliferation and migration of human non-small cell lung cancer A549 cells. Eur. J. Pharmacol. 960, 176156, 2023. [press release]
6) Furutani, Y., Hirano, Y., Toguchi, M., Higuchi, S., Qin, X.-Y., Yanaka, K., Sato-Shiozaki, Y., Takahashi, N., Sakai, M., Kongpracha, P., Suzuki, T., Dohmae, N., Kukimoto-Niino, M., Shirouzu, M., Nagamori, S., Suzuki, H., Kobayashi, K., Masaki, T., Koyama, H., Sekiba, K., Otsuka, M., Koike, K., Kohara, M., Kojima, S., Kakeya, H., Matsuura, T. A small chemical compound iCDM-34 identified by in silico screening suppresses HBV DNA through activation of arylhydrocarbon receptor. Cell Death Discov. 9, 216, 2023. [press release]
5) Ozaki, M., Shimotsuma, M., Kuranaga, T., Kakeya, H., Hirose, T. Simultaneous separation and identification of all structural isomers and enantiomers of aminobutyric acid using a highly sensitive chiral resolution labeling reagent. Anal. Methods, 15, 6648-6655, 2023. [selected as a Front Cover]
4) Matsuoka, T., Hattori, A., Oishi, S., Araki, M., Fujii, T., Arichi, N., Okuno, Y., Kakeya, H., Yamazaki, S., Ohno, H., Inuki, S. Establishment of the MR1-presentation reporter screening system and identification of phenylpropanoid derivatives as MR1 ligands. J. Med. Chem. 66, 12520-12535, 2023.
3) Ozaki, M., Shimotsuma, M., Kuranaga, T., Kakeya, H., Hirose, T. Separation and identification of isoleucine enantiomer and diastereomer using an original chiral resolution labeling reagent. Chem. Pharm. Bull. 71, 824-831, 2023.
2) Ochiai, T., Inukai, T., Akiyama, M., Furui, K., Ohue, M.,　Matsumori, N., Inuki, S., Uesugi, M., Sunazuka, T., Kikuchi, K., Kakeya, H. Sakakibara, Y. Variational autoendoder-based model of constructing chemical latent space for large molecular structures with 3D complexity. Commun. Chem., 16, 249, 2023.
1) Ozaki, M., Shimotsuma, M., Kuranaga, T., Kakeya, H. Hirose, T. Separation of amyloid β fragment peptides with racemised and isomerised aspartic acid residues using an original chiral resolution labeling reagent. Analyst, 148, 1209-1213, 2023. [selected as Hot Articles & Cover Art]
総説・著書：
2) 掛谷秀昭. 創薬リード探索へのケモインフォマティクスの応用. ケモインフォマティクスにおけるデータ収集の最適化と解析方法～組成予測や化学構造の生成・合成経路探索や反応条件最適化・毒性評価～, 技術情報協会, 2023. (2023年4月発刊)　　　　　　　　　
1) 掛谷秀昭. 新講座・天然物化学① 「天然有機化合物と”くすり”」. 日本化学会「化学と教育」, 71, 492-495, 2023.　　　　

2022

原著論文：
9) Ikeda, H., Kawami, M., Imoto, M., Kakeya, H. Identification of the polyether ionophore lenoremycin through a new screening strategy targeting cancer stem cells. J. Antibiot. 75, 671-678, 2022. [selected as a highlight article.] [press release]
8) Sasaki, M., Nishimura, S., Yashiroda, Y., Matsuyama, A., Kakeya, H., Yoshida, M. FK506 binding protein, FKBP12, promotes serine utilization and negatively regulates threonine deaminase in fission yeast. iScience 25, 105659, 2023. [press release]
7) Ishikawa, F., Konno, S., Uchiyama, Y., Takashima, K., Kakeya, H., Tanabe, G. Exploring a chemical scaffold for rapid and selective photoaffinity labeling of nonribosomal peptide synthetases in living bacterial cells. Philos. Trans. R. Soc. Lond., B, Biol. Sci. doi: 10.1098/rstb.2022.0026, 2022.
6) Matsumoto, T., Kuranaga, T., Taniguchi, Y., Wang, W., Kakeya, H. Solid-phase total synthesis and structural confirmation of antimicrobial longicatenamide A. Beilstein J. Org. Chem. 18, 1560-1566, 2022.
5) Ozaki, M., Kuwayama, T., Hirose, T., Shimotsuma, M, Hashimoto, A., Kuranaga, T., Kakeya, H. Separation and identification of the DL-forms of short-chain peptides using a new chiral resolution labeling reagent. Anal. Bioanal. Chem., 414, 4039-4046.
4) Kim, W.E., Ishikawa, F., Re, R.N., Suzuki, T., Dohmae, N., Kakeya, H., Tanabe, G., Burkart, M.D. Developing crosslinkers specific for epimerization domain in NRPS initiation modules to evaluate mechanism. RSC Chem. Biol. 3, 312-319, 2022.
3) Lu, S., Jiang, Y., Shinzato, N., Teruya, Y., Shimo, T., Nishime, A., Kakeya, H. (TBA)
2) Kuranaga, T., Kakeya, H. A special issue of "Chemical Tools in Microbiology": Development and application of highly sensitive labeling reagents for amino acids. Methods in Enzymol., 665, 105-133, 2022.
1) Abe, T., Horisawa, Y., Kikuchi, O., Ozawa-Umeta, H., Kishimoto, A., Imaizumi, A., Hashimoto, T., Shirakawa, K., Takaori-Kondo, A., Yusa, K., Asakura, T. Kakeya, H., Kanai, M. Pharmacologic characterization of TBP1901, a prodrug form of curcumin, and CRISPR-Cas9 screen for therapeutic targets of curcumin. Eur. J. Pharmacol. 935, 175321, 2022. [press release]

2021

原著論文：
19) Khadka, S., Omura, S., Sato, F., Nishio, K., Kakeya H., Tsunoda, I. Curcumin beta-D-glucuronide modulates an autoimmune model of multiple sclerosis with alteredgut microbiota in the ileum and feces. Front. Cell. Infect. Microbiol. 11, Article 772962, 2021. [Press release]
18) Sakai, M., Takahashi, N., Ikeda, H., Furutani, Y., Higuchi, S., Suzuki, T., Dohmae, N., Kobayashi, S., Harada, H., Kojima, S., Matsuura, T., Hattori, A., Kakeya, H. Design, synthesis, and target identification of new hypoxia-induced factor 1 (HIF-1) inhibitors containing 1-alkyl-1H-pyrazole-3-carboxamide moiety. Bioorg. Med. Chem. 46, 116375, 2021.
17) Kuranaga, T., Tamura, M., Ikeda, H., Terada, S., Nakagawa, Y., Kakeya, H. Identification and total synthesis of an unstable anticancer macrolide presaccharothriolide Z produced by Saccharothrix sp. Org. Lett. 23, 7106-7111, 2021. [Highlight in the category of Chemistry in Medicine and Biology; Synfacts, 18, 0095, 2022]
16) Ikeda, H. Kakeya, H. Targeting hypoxia-inducible factor (HIF-1) signaling with natural products toward cancer chemotherapy. J. Antibiot. 74, 687-695, 2021. [The special issue in "Approach toward cancer-targeting therapy by microbial origin"]
15) Liu, C., Hashimoto, J., Kudo, K., Shin-ya, K., Kakeya, H. An atypical arginine dihydrolase involved in the biosynthesis of cyclic hexapeptide longicatenamides. Chem. Asian J. 16, 1382-1387, 2021
14) Pan, C., Kuranaga, T., Cao, X., Suzuki, T., Dohmae, N., Shinzato, N., Onaka, H., Kakeya, H. Amycolapeptins A and B, cyclic nonadepsipeptides produced by combined-culture of Amicolatopsis sp. and Tsukamurella pulmonis. J. Org. Chem. 86, 1843-1849, 2021.
13) Morimoto, R., Matsumoto, T., Minote, M., Yanagisawa, M., Yamada, R., Kuranaga, T., Kakeya, H. Highly sensitive determination of amino acids by LC-MS under neutral conditions. Chem. Pharm. Bull. 69, 265-270, 2021.
12) Fujita, K., Ikuta, M., Nishimura, S., Sugiyama, R., Yoshimura, A., Kakeya, H. Amphiol, an antifungal fungal pigment from Pseudogymnoascus sp. PF1464. J. Nat. Prod. 84, 986-992, 2021.
11) Takenaka, K., Kaneko, K., Takahashi, N., Nishimura, S., Kakeya, H. Retro-aza-Michael reaction of an o-aminophenol adduct in protic solvents inspired by natural products. Bioorg. Med. Chem. 35, 116059, 2021.
10) Tanaka, M., Kondo, J., Kaneko, K., Endo, H., Onuma, K., Coppo, R., Masuda, M., Kamiura, S., Yoshino, K., Ueda, Y., Kakeya, H. Kimura, T., Inoue, M. Heterogenous chemosensitivity of a panel of organoid lines derived from small cell neuroendocrine carcinoma of the uterine cervix. Human Cell. 34, 889-900, 2021.
9) Sunagawa, Y., Funamoto, M., Shimizu, K., Shimizu, S., Sari, N., Katanasaka, Y., Miyazaki, Y., Kakeya, H., Hasegawa, K., Morimoto, T. Curcumin, an inhibitor of p300-HAT activity, suppresses the development of hypertension-induced left ventricular hypertrophy with preserved ejection fraction in dahl rats. Nutrients, 13, 2608, 2021.
8) Kanoh, N., Terashima, R., Nishiyama, H., Terajima, Y., Nagasawa, S., Sasano, Y., Iwabuchi, Y., Saito, H., Egoshi, S., Dodo, K., Sodeoka, M., Pan, C., Ikeuchi, Y., Nishimura, S., Kakeya, H. Design, synthesis, and antifungal activity of 16,17-dihydroheronamide C and ent-heronamide C. J. Org. Chem. 86, 16249-16258, 2021.
7) Kanoh, N., Terajima, Y., Tanaka, S., Terashima, R. Nishiyama, H., Nagasawa, S., Sasano, Y., Iwabuchi, Y., Nishimura, S., Kakeya, H. Toward the creation of induced pluripotent small (iPS) molecules: Establishment of a modular synthetic strategy to the heronamide C-type polyene macrolactams and their conformational and reactivity analysis. J. Org. Chem. 86, 16231-16248, 2021.
6) Ishikawa, F., Konno, S., Uchida, C., Suzuki, T., Takashima, K., Dohmae, N., Kakeya, H., Tanabe, G. Chemoproteomics profiling of surfactin-producing nonribosormal peptide synthetases in vitro and in living bacterial cells. Cell Chem. Biol. 28, 1-21, 2021.
5) Ishikawa, F., Konno, S., Takashima, K., Kakeya, H.Tanabe, G. Inhibition of efflux pumps aids small-molecule probe-based fluorescence labeling and imaging in the gram-negative bacterium Escherichia coli. Org. Biomol. Chem. 19, 8906-8911, 2021.
4) Matsuoka, T., Motozono, C., Hattori, A., Kakeya, H., Yamasaki, S., Oishi, S., Ohno, H., Inuki, S. The effects of 5-OP-RU stereochemistry on its stability and MAIT-MR1 axis. ChemBioChem, 22, 672-678, 2021.
3) Pan, C., Kuranaga, T., Kakeya, H. Application of the highly sensitive labeling reagent to the structural confirmation of readily isomerizable peptides. J. Nat. Med. 75, 339-343, 2021.
2) Elsadek, L.A., Matthews, J.H., Nishimura, S., Nakatani, T., Ito, A., Gu, T., Luo, D., Salvador-Reyes, L.A., Paul, V.J., Kakeya, H., Luesch, H. Genomic and targeted approachs unveil the cell membrane as a major target of the antifungal cytotoxin amantelide A. ChemBioChem, 22, 1790-1799, 2021.
1) Jiang, Y.#, Matsumoto, T.#, Kuranaga, T., Lu, S., Wang, W., Onaka, H., Kakeya, H. Longicatenamides A-D, two diastereomeric pairs of cyclic hexapeptides produced by combined-culture of Streptomyces sp. KUSC_F05 and Tsukamurella pulmonis TP-B0596. (#equal contribution) J. Antibiot. 74, 307-316, 2021.
総説・著書：
3) 掛谷秀昭（監修）. くすり大図鑑, Newton大図鑑シリーズ, Newton （ニュートン）, ニュートンプレス社, 2021.（2021年11月発刊）
2) 掛谷秀昭. 特集・ポストゲノム時代の天然物化学：　希少放線菌と異属微生物間化学コミュニケーションを活用したケミカルスペース拡充戦略. ファインケミカル, シーエムシー出版, 50, 33-39, 2021.
1) 掛谷秀昭（監修）. Newton 別冊 「くすりの科学知識-今こそ知っておきたいくすりの効能、しくみ、正しい付き合い方-（増補 第3版）」, pp.4-119, Newton （ニュートン）, ニュートンプレス社, 2021.

2020

原著論文：
12) Kuranaga, T., Minote, M., Morimoto, R., Pan, C., Ogawa, H., Kakeya, H. Highly sensitive labeling reagents for scarce natural products. ACS Chem. Biol. 15, 2499-2506, 2020. [Press release]
11) Pan, C., Kuranaga, T., Kakeya, H. Total synthesis of thioamycolamide A via a biomimetic route. Org. Biomol. Chem. 18, 8366-8370, 2020.
10) Ikeda, H., Muroi, M., Kondoh, Y., Ishikawa, S., Kakeya, H., Osada, H., Imoto, M. Miclxin, a novel MIC60 inhibitor, induces apoptosis via mitochondrial stress in beta-catenin mutant tumor cells. ACS Chem. Biol. 15, 2195-2204, 2020.
9) Fustin, J.M., Ye, S., Rakers, C., Kaneko, K., Fukumoto, K., Yamano, M., Versteven, M., Grunewald, E., Cargill, S.J., Tamai, K.T., Xu, Y., Jabbur, M.L., Kojima, R., Lamberti, M.L., Yoshioka-Kobayashi, K., Whitmore, D., Tammam, S., Howell, L., Kageyama, R., Matsuo, T., Stanewsky, R., Golombek, D.A., Johnson, C.H., Kakeya, H., Van Ooijen, G., Okamura, H. Methylation deficiency disrupts biological rhythms from bacteria to humans. Commun. Biol. 3, 211, 2020. doi. 10.1038/s42003-0200942-0. [Press release]
8) Pan, C., Kuranaga, T., Liu, C., Lu, S., Shinzato, N., Kakeya, H. Thioamycolamides A-E, sulfur-containing cycliclipopeptides produced by the rare actinomycete Amycolatopsis sp. Org. Lett. 22, 3014-3017, 2020.
7) Takahashi, N., Kaneko, K., Kakeya, H. Total synthesis and antimicrobial activity of tumescenamide C and its derivatives. J. Org. Chem. 85, 4530-4535, 2020.
6) Kanou, A., Nishimura, S., Tabuchi, T., Matsuyama, A., Yoshida, M., Kato, T., Kakeya, H. Serine catabolism produce ROS, sensitizes cells to actin dysfunction, and suppresses cell growth in fission yeast. J. Antibiot. 73, 574-580, 2020. doi: 10.1038/s41429-020-0305-6.
5) Shimizu, K., Funamoto, M., Sunagawa, Y., Wakabayashi, H., Genpei, M., Miyazaki, Y., Katanasaka, Y., Sari, N., Shimizu, S., Katayama, A., Moki, H., Shibata, H., Iwabuchi, Y., Kakeya, H., Wada, H., Hasegawa, K., Morimoto, T. The synthetic curcumin analogue GO-Y030 effectively suppresses the development of pressure overload-induced heart failure in mice. Sci. Rep. 10, 7172, 2020. doi: 10.1038/s41598-020-64207-w.
4) Baba, K., Kuwada, S., Nakao, A., Li, X., Okuda, A., Nishida, A., Matsuda, S., Fukuoka, N., Kakeya, H., Kataoka, T. Different localization of lysosomal-associated membrane protein 1(LAMP1) in mammalian cultured cell lines. Histochem. Cell. Biol. 153, 199-213, 2020. doi: 10.1007/s00418-019-01842-z.
3) Liu, C., Kakeya, H. Cryptic chemical communication: Secondary metabolic responses revealed by microbial co-culture. Chem. Asian. J. 15, 327-337, 2020. [Selected as a cover feature.]
2) Ozawa-Umeta, H., Kishimoto, A., Imaizumi, A., Hashimoto, T., Kakeya, H., Kanai, M. Curcumin beta-D-glucuronide (CMG) exhibits anti-tumor effects on oxaliplatin-resistant colon cancer with less toxicity. Cancer Sci. 111, 1785-1793, 2020. [Press release]
1) Li, X.-B., Hattori, A., Takahashi, S., Goto, Y., Harada, H., Kakeya, H. Ubiquitin carboxyl-terminal hydrolase L1 promotes hypoxia-inducible factor 1-dependent tumor cell malignancy in spheroid models. Cancer Sci. 111, 239-252, 2020.
総説・著書：
3) 掛谷秀昭. 寄稿「新しい素材の探索・創製・解析研究に誇りを秘めて」. 新規素材探索研究会会報, 18, p.3, 2020.
2) 掛谷秀昭. Coffee Break: 小さき命（微生物）に感謝して. MEDCHEM NEWS, 2020. (TBA)
1) 中山和真, 掛谷秀昭. News&View: ニトリルオキシドのプロドラッグ化に基づくGPX4に対する選択的共有結合阻害剤の開発. 日本ケミカルバイオロジー学会機関誌「ケミカルバイオロジー(Chemical Biology)」, 13, 2020. (TBA)

2019

原著論文：
10) Sugiyama, R., Nakatani, T., Nishimura, S., Takenaka, K., Ozaki, T., Asamizu, S., Onaka, Y., Kakeya, H. Chemical interaction of cryptic actinomycete metabolite 5-alkyl-1,2,3,4-tetrahydroquinolines through aggregate formation. Angew. Chem. Int. Ed. 58, 13486-13491, 2019. [Press release]
9) Yoshimura, A., Nishimura, S., Suzuki, T., Hattori, A., Dohmae, N. Kato, T., Kakeya, H. Isolation, structure elucidation and conformational regulation of myropeptins, lipopeptides from a fungus Myrothecium rodium. Org. Lett. 21, 7524-7528, 2019.
8) Jiang, Y., Lu, S., Hirai, G., Kato, T., Onaka, H., Kakeya, H. Enhancement of saccharothriolide production and discovery of a new metabolite, saccharothriolide C2, by combined-culture of Saccharothrix sp. and Tsukamurella pulmonis. Tetrahedron Lett. 60, 1072-1074, 2019.
7) Kakeya, H., Kuranaga, T. Precious Microorganisms as Productive Resources: Marine-derived Microorganisms and Combined-Culture. Comprehensive Natural Products III: Chemistry and Biology, Elsevier, in press, 2019. (invited review)
6) Furutani, Y., Toguchi M., Shiozaki-Sato, Y., Qin, X.Y., Ebisui, E., Higuchi, S., Sudoh, M., Suzuki, H., Takahashi, N., Watashi, K., Wakita, T., Kakeya, H., Kojima, S. An interferon-like small chemical compound CDM-3008 suppresses hepatitis B virus through induction of interferon-stimulated genes. PLOS ONE, 14, e0216139, 2019. [Press release]
5) Funamoto, M., Shimizu, K., Sunagawa, Y., Katanasaka, Y., Miyazaki, Y., Kakeya, H., Yamakage, H., Satoh-Asahara, N., Wada, H., Hasegawa, K., Morimoto, T. Effects of highly absorbable curcumin in patients with impaired glucose tolerance and non-insulin dependent diabetes mellitus. J. Diabetes Res. 2019, 8208237, 2019..
4) Takahashi, N., Hayashi, H., Poznaks, V., Kakeya, H. Total synthesis of verucopeptin, an inhibitor of hypoxia-inducible factor 1 (HIF-1). Chem. Commun. 55, 11956-11959, 2019.
3) Cornelio, K., Espiritu, R. A., Hanashima, S., Todokoro, Y., Malabed, R., Murata, M., Kinoshita, M., Matsumori, N., M., Nishimura, S., Kakeya, H., Yoshida, M., Matsunaga, S. Theonellamide A, a marine-sponge-derived bicyclicpeptide, binds to sterol in aqueous DMSO: Solution NMR-based analysis of peptide-sterol interactions using hydroxylated cholesterol. Biochim. Biophys. Acta Biomembr. 1861, 228-235, 2019.
2) Takahashi, N., Hayashi, K., Nakagawa, Y., Furutani, Y., Toguchi M., Shiozaki-Sato, Y., Sudoh, M., Kojima, S., Kakeya, H. Development of an anti-hepatitis B virus (HBV) agent through the structure-activity relationship of the interferon-like small compound CDM-3008. Bioorg. Med. Chem. 27, 470-478, 2019.
1) Ozaki, T., Sugiyama, R., Nishimura, S., Asamizu, S., Katsuyama, Y., Kakeya, H., Onaka, H. Identification of the common biosynthetic gene cluster for both antimicrobial streptoaminals and antifungal 5-alkyl-1,2,3,4-tetrahydroquinolines. Org. Biomol. Chem. 17, 2370-2378, 2019[HOT article collectionに選ばれました]
総説・著書：
4) 掛谷秀昭（監修）. 薬の基礎知識・創薬の世界, Newton 別冊 「くすりの科学知識（増補 第2版）」, Newton （ニュートン）, ニュートンプレス社, pp.4-89, 2019.（印刷中）
3) 掛谷秀昭. 研究トピックス：がんと宿主の化学コミュニケーション阻害を指向した水溶性プロドラッグ型抗がん剤CMGの開発研究. 新学術領域研究「化学コミュニケーションのフロンティア」・Newsletter, vol. 3, 10, 2019.　　　　　　　　　　　　　　　　　　
2) 掛谷秀昭. 研究トピックス：微生物間化学コミュニケーションの利活用によるケミカルスペース拡充戦略. 新学術領域研究「化学コミュニケーションのフロンティア」・Newsletter, vol. 3, 9, 2019.　　　　　　　　　　　　　　　　　　
1) 今野　翔, 石川文洋, 掛谷秀昭. 化学標識法を用いた非リボソームペプチド合成酵素の活性検出と機能解析. 日本ケミカルバイオロジー学会機関誌「ケミカルバイオロジー(Chemical Biology)」, 12, 3-7, 2019.

2018

原著論文：
4) Sunagawa, Y., Funamoto, M., Sono, S., Shimizu, K., Shimizu, S., Genpei, M., Miyazaki, Y., Katanasaka, Y., Morimoto, E., Ueno, M., Komiyama, M., Kakeya, H., Wada, H., Hasegawa, K., Morimoto, T. Curcumin and its demethoxy derivatives possess p300 HAT inhibitory activity and suppress hypertrophic responses in cardiomyocytes. J. Pharmacol. Sci. 136, 212-217, 2018.
3) Kakeya, H. Natural products-inspired chemical biology toward development of new antibiotics. Jpn. J. Antibiot. 71, 181-191, 2018.
2) Ishikawa, F., Tanabe, G., Kakeya, H. Activity-based protein profiling of non-ribosomal peptide synthetases. Curr. Top. Microbiol. Immunol. doi: 10.1007/82_2018_133 (in press)
1) Lu, S., Nishimura, S., Takenaka, K., Ito, M., Kato, T., Kakeya, H. Discovery of presaccharothriolide X, a retro-Michael product of saccharothriolide B, from the rare actinomycete Saccharothrix sp. A1506. Org. Lett. 20, 4406-4410, 2018. [Press release]
総説・著書：
3) 掛谷秀昭. Discovery Scienceに魅せられて：天然物創薬ケミカルバイオロジーの最前線. 化学と生物, 56, 210-216, 2018.[遠藤章先生ガードナー国際賞受賞記念特集]
2) 西村慎一, 掛谷秀昭, 松森信明. 生体膜を標的にする天然有機化合物：天然物による厳密な脂質認識とそれに基づく表現型. 化学と生物, 56, 678-685, 2018.
1) 掛谷秀昭, 李　雪氷,　吉村　彩, 小川はるか. 低酸素誘導因子HIFs活性化経路を標的とする化合物. ケミカルバイオロジー化合物集（日本におけるケミカルバイオロジーの新展開第198委員会編）, pp82-84, 2018.

2017

　　　
原著論文：
5) Ozawa, H., Imaizumi, A., Sumi, Y., Hashimoto, T., Kanai, M., Makino, Y., Tsuda, T., Takahashi, N., Kakeya, H. Curcumin beta-D-glucuronide plays an important role to keep high levels of free-form curcumin in the blood. Biol. Pharm. Bull. 40, 1515-1524, 2017. [Press release]
4) Ishikawa, F., Kasai, S., Kakeya, H. Tanabe, G. Visualizing the adenylation activities and protein-protein interactions of aryl acid adenylating enzymes. ChemBioChem. 18, 2199-2204, 2017.
3) Konno, S., Ishikawa, F., Suzuki, T., Dohmae, N., Kakeya, H., Tanabe, G. A chemoproteomics approach to investigate phosphopantetheine transferase activity at the cellular level. ChemBioChem. 18, 1855-1862, 2017.
2) Ishikawa, F., Kakeya, H. The chemical biology of natural product biosynthesis: chemical tools for the proteomic analysis of nonribosomal peptide synthetases. Frontiers in Natural Product Chemistry, 3, 65-90 (2017).
1) Lu, S., Nishimura, S., Ito, M., Kato, T., Kakeya, H. Precursor-directed in situ synthesis of saccharothriolides G and H by the actinomycete Saccharothrix sp. A1506. J. Antibiot. 70, 718-720, 2017. [The special issue in 2017 featuring Professor Satoshi Ōmura, a distinguished Novel Prize awardee in Physiology or Medicine 2015]
総説・著書：
4) 掛谷秀昭. 創薬ケミカルバイオロジー：自然に学ぶ薬づくり. 「くすりをつくる研究者の仕事―薬のタネ探しから私たちに届くまで」 （京都大学大学院薬学研究科編, 第3章）, pp63-82, 化学同人, 2017.
3) 掛谷秀昭（監修）. 1. 薬の基礎知識 & 2. 創薬の世界, Newton 別冊 「くすりの科学知識：くすりのしくみと、奥深き創薬の世界」, pp6-37, Newton （ニュートン）, ニュートンプレス社, 2017.
2) 掛谷秀昭（協力）. 画期的な薬, Newton 別冊 「くすりの科学知識：くすりのしくみと、奥深き創薬の世界」, pp74-81, Newton （ニュートン）, ニュートンプレス社, 2017.
1) 森山彰博, 片桐直宏, 西村慎一, 掛谷秀昭. 生体膜を標的とする天然物の作用機序解析を指向したLiDEL法の開発. 日本ケミカルバイオロジー学会機関誌「ケミカルバイオロジー(Chemical Biology)」, 10, 2-5, 2017.

2016

原著論文：
16) Yeom, C.J., Zeng, L., Goto, Y., Morinobu, A., Shinomiya, K., Kobayashi, M., Itasaka, S., Yoshimura, M., Hur, C.G., Kakeya, H., Hammond, E.M., Hiraoka, M., Harada, H. LY6E: a conductor of malignant tumor growth through modulation of the PTEN/PI3K/Akt/HIF-1 axis. Oncotarget, doi: 10.18632/oncotarget.11670, 2016.
15) Sugiyama, R., Nishimura, S., Ozaki, T., Asamizu, S., Onaka, H., Kakeya, H. Discovery and total synthesis of streptoaminals, antimicrobial [5,5]-spirohemiaminals from the combined-culture of Streptomyces nigrescens and Tsukamurella pulmonis. Angew. Chem. Int. Ed. 55, 10278-10282, 2016. [Press release]
14) Kasai, S., Ishikawa, F., Suzuki, T., Dohmae, N., Kakeya, H. A chemical proteomic probe for detecting naive carrier protein motifs in nonribosomal peptide synthetases. Chem Commun, 52, 14129-14132, 2016.
13) Matsumoto, Y., Hibino, K., Yonaga, M., Kakeya, H., Hayashi, Y. Enantioselective total synthesis of RQN-18690A (18-deoxyherboxidiene). Org. Lett. 18, 3382-3385, 2016.
12) Lu, S., Nishimura, S., Ito, M., Tsuchida, T., Kakeya, H. Isolation and structure elucidation of cytotoxic saccharothriolides D to F from a rare actinomycete Saccharothrix sp. and their structure-activity relationship. J. Nat. Prod. 79, 1891-1895, 2016.
11) Ishikawa, F., Sugimoto, H., Kakeya, H. In vitro investigation of crosstalk between fatty acid and polyketide syntases in the andrimid biosynthetic assembly line. ChemBioChem. 17, 2137-2142, 2016.
10) Fujita, K., Sugiyama, R., Nishimura, S., Ishikawa, N., Arai, M., Ishibashi, M., Kakeya, H. Stereochemical assignment and biological evaluation of BE-14106 unveils the importance of one acetate unit for the antifungal activity of polyene macrolactams. J. Nat. Prod. 79, 1877-1880, 2016.
9) Ishikawa, F., Kakeya, H. A competitive enzyme-linked immunosorbent assay system for adenylation domains in nonribosormal peptide synthetases. ChemBioChem. 17, 474-478, 2016.
8) Kakeya, H., Kaida, D. Sekiya, H., Nagai, K., Yoshida, M., Osada, H. RQN-18690A (18-deoxyherboxidiene) targets SF3b, a spliceosome component, and inhibits angiogenesis. J. Antibiot. 69, 121-123, 2016.
7) Funamoto, M., Sunagawa, Y., Katanasaka, Y., Miyazaki, Y., Imaizumi, A., Kakeya, H., Yamakage, H., Satoh-Asahara, N., Komiyama, M., Wada, H., Hasegawa, K., Morimoto, T. Highly absorption curcumin reduces serum levels of atherosclerotic low-density lipoprotein in patients with mild chronic obstructive pulmonary disease. Int. J. Chron. Obstruct. Pulmon. Dis. (Int. J. COPD), 11, 2029-2034, 2016.
6) Ishikawa, F., Kakeya, H. Affinity purification method for the identification of nonribosormal peptide biosynthetic enzymes using a synthetic probe for adenylation domains. Methods Mol. Biol. 1401, 63-76, 2016.
5) Yamamae, Y., Fujita, K., Nishimura, S., Kakeya, H. Generation of heronamides A and B from heronamide C produced by a marine-derived Streptomyces sp. and their antifungal activity.ELCAS J. 1, 66-68, 2016.
4) Cornelio, K., Espiritu, R. A., Todokoro, Y., Hamashima, S., Kinoshita, M., Matsumori, N., Murata, M. Nishimura, S., Kakeya, H., Yoshida, M., Matsunaga, S. Sterol-dependent membrane association of the marine sponge-derived bicyclic peptide theonellamide A as examined by 1H NMR. Bioorg. Med. Chem. 24, 5235-5242, 2016.
3) Espiritu, R. A., Cornelio, K., Kinoshita, M., Matsumori, N., Murata, M., Nishimura, S., Kakeya, H., Yoshida, M., Matsunaga, S. Marine sponge cyclic peptide theonellamide A disrupts lipid bilayer integrity without forming distinct membrane pores. Biochem. Biophys. Acta, 1858, 1373-1379, 2016.
2) Kanoh, N., Itoh, S., Fujita, K., Sakanishi, K., Sugiyama, R., Iwabuchi, Y., Nishimura, S., Kakeya, H. Asymmetric total synthesis of heronamides A-C: Stereochemical confirmation and impact of long-range stereochemical communication on the biological activity. Chem. Eur. J. 22, 8586-8595, 2016.
1) Kakeya, H. Natural products-prompted chemical biology: Phenotypic screening and a new platform for target identification. Nat. Prod. Rep. 33, 648-654, 2016.
総説・著書：
5) 都築健悟, 掛谷秀昭. 感染症の脅威と闘う―ヒトマイクロバイオームと特殊培養デバイスの活用. 化学, 71 (12), 70-71, 化学同人, 2016.
4) 掛谷秀昭. 低酸素応答シグナルを標的とした分子標的抗がん剤開発. 展望 -Promising Vistas in Cancer Research-. 10, 50-55, 小林がん学術振興会. 2016.
3) Shan Lu, 杉崎俊文, 岸本真治, 西村慎一, 掛谷秀昭. 特集「ケミカルバイオロジーの新展開」：表現系スクリーニングを基盤とした先導的ケミカルバイオロジー研究. 化学工業 , 67, 676-681, 化学工業社, 2016.
2) 四方田悠輔, 掛谷秀昭. がん化学療法の標的としての低酸素誘導因子HIF活性化経路. 医学のあゆみ. 257, 246-248, 2016.
1) 掛谷秀昭（協力）. プロローグ「大村智博士ノーベル賞受賞」, Newton 別冊 「驚異のバクテリア：バクテリア＝細菌の生態と可能性」, Newton （ニュートン）, pp4-17, ニュートンプレス社, 2016.

2015

原著論文：
17) Yoshimura, A., Nishimura, S., Otsuka, S., Hattori, A., Kakeya, H. Structure elucidation of verucopeptin, a HIF-1 inhibitory polyketide-hexapeptide hybrid metabolite from an actinomycete. Org. Lett. 17, 5364-5367, 2015. [Press release]
16) Moriyama, A., Katagiri, N., Nishimura, S., Takahashi, N., Kakeya, H. In vivo linking of membrane lipids and the anion transporter band 3 with thiourea-modified amphiphilic lipid probe. Sci. Rep. 5, 17427, 2015.
15) Kishimoto, S., Nishimura, S., Hatano, M., Igarashi, M., Kakeya, H. Total synthesis and antimicrobial activity of chlorocatechelin A. J. Org. Chem. 80, 6076-6082, 2015.
14) Yasuda, Y., Arakawa, T., Nawata, Y., Shimada, S., Oishi, S., Fujii, N., Nishimura, S., Hattori, A., Kakeya, H. Design, synthesis and structure-activity relationships of 1-ethylpyrazole-3-carboxamide as novel HIF-1 inhibitors. Bioorg. Med. Chem. 23, 1776-1787, 2015.
13) Goto, Y., Zeng, L., Yeom, C.J., Zhu, Y., Morinobu, A., Shinomiya, K., Kobayashi, M., Hirota, K., Itasaka, S., Yoshimura, M., Tanimoto, K., Torii, M., Sowa, T., Menju, T., Sonobe, M., Kakeya, H., Toi, M., Date, H. Hammond, E.M., Hiraoka, M., Harada, H. UCHL1 provides diagnostic and antimetastatic strategies due to its deubiquitinating effect on HIF-1α. Nat. Commun. 6:6153. doi: 10.1038/ncomms7153, 2015. [Press release]
12) Lu, S., Nishimura, S., Hirai, G., Ito, M., Kawahara, T., Izumikawa, M., Sodeoka, M., Shin-ya, K., Tsuchida, T., Kakeya, H. Saccharothriolides A-C, novel phenyl-substituted 10-membered macrolides from a rare actinomycete Saccharothrix sp. Chem. Commun. 51, 8074-8077, 2015.
11) Ishikawa, F. Miyamoto, K., Konno, S., Kasai, S., Kakeya, H. Accurate detection of adenylation domains in nonribosomal peptide synthetases by an enzyme-linked immunosorbent assay system using active site-directed probes for adenylation domains. ACS Chem. Biol. 10, 2816-2826, 2015. [Press release]
10) Kishimoto, S., Nishimura, S., Kakeya, H. Total synthesis and structure revision of mirubactin, and its iron binding activity. Chem. Lett. 44, 1303-1305, 2015.
9) Sugiyama, R., Nishimura, S., Ozaki, T., Asamizu, S., Onaka, H., Kakeya, H. 5-Alkyl-1,2,3,4-tetrahydroquinolines, new membrane-interacting lipophilic metabolites, produced by combined culture of Streptomyces nigrescens and Tsukamurella pulmonsis. Org. Lett. 17, 1918-1921, 2015.
8) Piao, J.H., Tashiro, A., Nishikawa, M., Aoki, Y., Moriyoshi, E., Hattori, A., Kakeya, H. Expression, purification and enzymatic characterization of a recombinant human ubiquitin-specific protease 47. J. Biochem. 158, 477-484, 2015.
7) Ishikawa F., Suzuki, T., Dohmae, N., Kakeya, H. A multiplex labeling strategy for nonribosomal peptide synthetases using active site-directed proteomic probes for adenylation domains. ChemBioChem. 16, 2590-2594, 2015.
6) Kasai, S., Konno, S., Ishikawa F., Kakeya, H. Functional profiling of adenylation domains in nonribosomal peptide synthetases by competitive activity-based protein profiling. Chem. Commun. 51, 15764-15767, 2015. [Selected as a "Back Cover Highlight"]
5) Ishikawa, F. Konno, S., Suzuki, T., Dohmae, N., Kakeya, H. Profiling nonribosomal peptide synthetase activities using chemical proteomic probes for adenylation domains. ACS Chem. Biol. 10, 1989-1997, 2015.
4) Ishikawa, F. Kakeya, H. Recent advances in adenylation domain enzymology in nonribosomal peptide biosynthesis. Curr. Org. Chem. 19, 1204-1221, 2015.
3) Konno, S., Ishikawa, F., Suzuki, T., Dohmae, N., Burkart, M.D., Kakeya, H. Active site-directed proteomic probes for adenylation domains in nonribosormal peptide synthetases. Chem. Commun. 51, 2262-2265, 2015.
2) Sunagawa, Y., Hirano, S., Katanasaka, Y., Miyazaki, Y., Funamoto, M., Okamura, N., Hojo, Y., Suzuki, H., Doi, O., Yokoji, T., Morimoto, E., Takahashi, T., Ozawa, H., Imaizumi, A., Ueno, M., Kakeya, H., Shimatsu, A., Wada, H., Hasegawa, K., Morimoto, T. Colloidal submicron-particle curcumin exhibits high absorption efficiency-A double-blind, 3-way crossover study-. J. Nutr. Sci. Vitaminol. 61, 37-44, 2015.
1) Tsunematsu, Y., Nishimura, S., Hattori, A., Oishi, S., Fujii, N., Kakeya, H. Isolation, structure elucidation and total synthesis of tryptopeptins A and B, new TGF-β signaling modulators from Streptomyces sp. Org. Lett. 17, 258-261, 2015.
総説・著書：
6) 掛谷秀昭（監修）. Newton Special 「知られざる創薬の世界：夢のくすりを求めて」, Newton（ニュートン）, 35巻(8), pp40-77, ニュートンプレス社, 2015.
5) 西村慎一, 掛谷秀昭. ステロール標的抗真菌剤の活性発現における細胞膜輸送バランスの重要性. バイオサイエンスとインダストリー, 73, 383-385, 2015.
4) 掛谷秀昭（協力）. 数億の人々を救った薬とは？, Newton （ニュートン）, pp18-23, ニュートンプレス社, 2015.
3) 西村慎一, 掛谷秀昭. 生体膜微小環境への挑戦：膜ステロールに作用する海洋天然物セオネラミド, CSJカレントレビュー19号（日本化学会編）「生物活性分子のケミカルバイオロジー」, 102-108, 化学同人, 2015.
2) 掛谷秀昭. 「天然物化学研究の最前線：生合成とケミカルバイオロジーの新展開」, 創薬シーズ開発を指向した天然物ケミカルバイオロジー, 第二次先端ウォッチング調査：融合領域の創成, pp. 21-24, 日本化学会・学術研究活性化委員会, 2015.
1) 掛谷秀昭. 特集「細胞を化学で観察する・操作する」ー発展著しい日本のケミカルバイオロジーを俯瞰するー. 創薬ケミカルバイオロジー： シード分子開発と分子プロファイリング, 生体の科学, 66, 119-125, 医学書院, 2015.

2014

原著論文：
9) Kishimoto,S., Nishimura, S., Hattori, A., Tsujimoto, M., Hatano, M., Igarashi, M.,Kakeya, H. Chlorocatechelins A and B from Streptomyces sp.: new siderophores containing chlorinated catecholate groups and an acylguanidine structure. Org. Lett. 16, 6108-6111, 2014.
8) Nishimura, S., Tokukura, M., Ochi, J., Yoshida, M., Kakeya, H. Balance between exocytosis and endocytosis determines the efficacy of sterol-targeting antibiotics. Chem. Biol. 21, 1690-1699, 2014. [Press release]
7) Fujita, K., Ishikawa, F., Kakeya, H. Biosynthetic origins of the epoxyquinone skeleton in epoxyquinols A and B. J. Nat. Prod. 77, 2707-2710, 2014.
6) Yoshimura, A., Kishimoto, S., Nishimura, S., Otsuka, S., Sakai, Y., Hattori, A., Kakeya, H. Prediction and determination of the stereochemistry of the 1,3,5-trimethyl substituted alkyl chain in verucopeptin, a microbial metabolite. J. Org. Chem. 79, 6858-6867, 2014.
5) Sugiyama, R., Nishimura, S., Matsumori, N., Tsunematsu, Y., Hattori, A., Kakeya, H. Structure and biological activity of 8-deoxyheronamide C from a marine-derived Streptomyces sp.: heronamides target saturated hydrocarbon chains in lipid membranes. J. Am. Chem. Soc. 136, 5209-5212, 2014. [Press release]
4) Miyamoto, K., Ishikawa, F., Nakamura, S., Hayashi, Y., Nakanishi, I., Kakeya, H. A 7-dimethylallyl tryptophan synthase from a fungal Neosartorya sp.: biochemical characterization and structural insight into the regioselective prenylation. Bioorg. Med. Chem. 22, 2517-2528, 2014.
3) Sakanishi, K., Itoh, S., Sugiyama, R., Nishimura, S., Kakeya, H., Iwabuchi, Y., Kanoh, N. Total synthesis of the proposed structure of heronamide C. Eur. J. Org. Chem. 1376-1380, 2014
2) Sunagawa, Y., Sono, S., Katanasaka, Y., Funamoto, M., Hirano, S., Miyazaki, Y., Hojo, Y., Suzuki, H., Miyoshi-Morimoto, E., Marui, A., Sakata, R., Ueno, M., Kakeya, H., Wada, H., Hasegawa, K., Morimoto, T. Optimal dose-setting study of curcumin for improvement of left ventricular systolic function after myocardial infarction in rats. J. Pharmacol. Sci. 126, 329-336, 2014.
1) Ishikawa, F., Kakeya, H. Specific enrichment of nonribosomal peptide synthetase module by an affinity probe for adenylation domains. Bioorg. Med. Chem. Lett. 24, 865-869, 2014.

2013

原著論文：
8) Fustin, JM, Doi, M., Yamaguchi, Y., Hida, H., Nishimura, S., Yoshida, M., Isagawa, T., Morioka, MS, Kakeya, H., Manabe, I., Okamura, H. RNA-methylation-dependent RNA processing controls the speed of the circadian clock. Cell, 155, 793-806, 2013. [Press release]
7) Morimoto, T., Sunagawa, Y., Katanasaka, Y., Hirano, S., Namiki, M., Watanabe, Y., Suzuki, H., Doi, O., Suzuki, K., Yamauchi, M., Yokoji, T., Miyoshi-Morimoto, E., Otsuka Y., Hamada, Y., Imaizumi, A., Nonaka, Y., Fuwa, T., Teramoto, T., Kakeya, H., Wada, H., Hasegawa, K. Drinkable preparation of theracurmin exhibits high absorption efficiency – A single-dose, double-blind, 4-way crossover study-. Biol. Pharm. Bull. 36, 1708-1714, 2013.
6) Ohno, Y., Hattori, A., Yoshiki, T., Kakeya, H. Association of epigenetic alterations in the human C7orf24 gene with the aberrant gene expression in malignant cells. J. Biochem., 154, 355-362, 2013.
5) Nishimura, S., Ishii, K., Iwamoto, K., Arita, Y., Matsunaga, S., Ohno-Iwashita, Y., Sato, B. S., Kakeya, H., Kobayashi, T., Yoshida, M.Visualization of Sterol-Rich Membrane Domains with Fluorescently-Labeled Theonellamides. PLoS ONE, 8, e83716, 2013.
4) Otsuki, S., Nishimura, S., Takabatake, H., Nakajima, K., Takasu, Y., Yagura, T., Sakai, Y., Hattori, A., Kakeya, H. Chemical tagging of a drug target using 5-sulfonyl tetrazole. Bioorg. Med. Chem. Lett. 23, 1608-1611, 2013.
3) Sugiyama, R., Nishimura, S., Kakeya, H. Stereochemical reassignment of heronamide A, a polyketide macrolactam from Streptomyces sp. Tetrahedron Lett. 54, 1531-1533, 2013.
2) Espiritu, R. A., Matsumori, N., Murata, M., Nishimura, S., Kakeya, H., Matsunaga, S., Yoshida, M. Interaction between the marine sponge cyclic peptide theonellamide A and sterols in lipid bilayers as vieweed by surface plasmon resonance and solid-state 2H nuclear magnetic resonance. Biochemistry, 52, 2410-2418, 2013.
1) Nagamoto, Y., Hattori, A., Kakeya, H., Takemoto, Y., Takasu, K. pH-sensitive DNA cleaving agents: in situ activation by ring construction of benzo-fused cylcobutanols. Chem. Commun. 49, 2622-2624, 2013.
総説・著書：
3) 笠井昭太, 西村慎一, 掛谷秀昭. 熱ショックタンパク質阻害剤の現状と可能性, がん分子標的治療, メディカルレビュー社, 11, 59-64, 2013.
2) 安田順信, 掛谷秀昭. 可逆的共有結合を利用した非特異的相互作用回避への化学的戦略. 日本ケミカルバイオロジー学会機関誌「ケミカルバイオロジー(Chemical Biology)」, 6, 21, 2013.
1) 矢守隆夫, 上原至雅, 深澤秀輔, 吉田稔 井本正哉, 清宮啓之, 馬島哲夫, 水上民夫, 川田学, 長田裕之, 旦慎吾, 松浦正明, 掛谷秀昭, 冨田章弘. 特集・制がん剤の分子標的スクリーニング成績「化学療法基盤情報支援班」報告-制がん候補物質のスクリーニング成績・第15報-. 癌と化学療法 40, supplement I, 癌と化学療法社, 2013.

2012

原著論文：
3) Kishimoto, S., Tsunematsu, Y., Nishimura, S., Hayashi, Y., Hattori, A., Kakeya, H. Tumescenamide C, an antimicrobial cyclic lipodepsipeptide from Streptomyces sp. Tetrahedron, 68, 5572-5578, 2012.
2) Sunagawa, Y., Wada, H., Sasaki, A., Imaizumi, A., Fukuda, H., Hashimoto, T., Katanasaka, Y., Shimatsu, A., Kimura, T., Kakeya, H., Fujita, M., Hasegawa, K., Morimoto, T. A novel drug delivery system of oral curcumin markedly improves efficacy of treatment for heart failure after myocardial infarction in rats. Biol. Pharm. Bull., 35, 139-144, 2012.
1) Shimatsu, A., Kakeya, H., Imaizumi, A., Morimoto, T., Kanai, M., Maeda, S. Clinical application of "curcumin", a multi-functional substance. Anti-Aging Med. 9, 75-83 , 2012. (review)
総説・著書：
2) 大野裕司, 服部 明, 掛谷秀昭. 分子標的薬-がんから他疾患までの治癒をめざして-：新しいがん分子標的としてのヒトC7orf24/γ-グルタミルシクロトランスフェラーゼ. 日本臨床社, 70, 723-727, 2012.
1) 石川文洋, 荒木通啓, 掛谷秀昭. 特集号「創薬を牽引する有機化学」：天然物創薬とケモインフォマティクス, ファルマシア, 48, 658-662, 2012.

2011

原著論文：
4) Ohno, Y., Hattori, A., Ueda, M., Kageyama, S., Yoshiki, T., Kakeya, H. Multiple NF-Y-binding CCAAT boxes are essential for transcriptional regulation of the human C7orf24 gene, a novel tumor-associated gene. FEBS J. 278, 4088-4099, 2011.
3) Takashima, K., Saitoh, A., Hirose, S., Nakai, W., Kondo, Y., Takasu, Y., Kakeya, H., Shin, H.-W., Nakayama, K. GBF1-Arf-COPI-ArfGAP-mediated Goldi-to-ER transport involved in regulation of lipid homeostasis. Cell Struct. Funct. 36, 223-235, 2011
2) Sunagawa, Y., Morimoto, T., Wada, H., Takaya, T., Katanasaka, Y., Kawamura, T., Yanagi, S., Marui, A., Sakata, R., Shimatsu, A., Kimura, T., Kakeya, H., Fujita, M., Hasegawa, K. A natural p300-specific histone acetyltransferase inhibitor, curcumin, in addition to angiotensin converting enzyme inhibitor exerts beneficial effects on left ventricular systolic function after myocardial infarction in rats. Cir. J. 75, 2151-2159, 2011.
1) Sasaki, H., Sunagawa, Y., Takahashi, K., Imaizumi, A., Fukuda, H., Hashimoto, T., Wada, H., Katanasaka, Y., Kakeya, H., Fujita, M., Hasegawa, K., Morimoto, T. Innovative preparation of curcumin for improved oral bioavailability. Biol. Pharm. Bull. 34, 660-665, 2011.
総説・著書：
2) 林　豊, 中村拓朗, 杉本泰康, 掛谷秀昭. 新規創薬リード化合物創製を指向した生合成遺伝子クラスター解析研究. 遺伝子医薬MOOK20号: ナノバイオ技術と最新創薬応用研究. （佐治英郎, 橋田　充（編））. 60-65, 2011.
1) 西村慎一, 掛谷秀昭, 吉田稔. 細胞膜を撹乱する海洋天然物 -セオネラミドはステロールに結合し、異常な細胞壁合成を誘導する-, 化学と生物., 49, 295-297, 2011.

2010

原著論文：
2) Lindqvist, L., Robert, F., Merrick, W., Kakeya, H., Fraser, C., Osada, H., Pelletier, J. Inhibition of translation by cytotrienin A - a member of the ansamycin family. RNA, 16, 2404-2413, 2010.
1) Nishimura, S., Arita, Y., Honda, M., Iwamoto, K., Matsuyama, A., Shirai, A., Kawasaki, H., Kakeya, H., Kobayashi, T., Matsunaga, S., Yoshida, M. Marine antifungal theonellamides target 3beta-hydroxysterol to activate Rho1 signaling. Nat. Chem. Biol. 6, 519-526, 2010. [Press release]
総説・著書：
2) 掛谷秀昭, 西村慎一. 特集号「日本の天然物化学の展望　-生命科学解明の機能分子、新たな創薬分子として-」；　新規有用天然有機化合物の開拓とケミカルバイオロジー研究. 有機合成化学協会誌, 68, 490-500, 2010.
1) 大槻さつき, 掛谷秀昭. Meeting Report：第14回日本がん分子標的治療学会. がん分子標的治療（メディカルレビュー社）. 8, 67-69, 2010.

2009

原著論文：
2) N. Kato, H. Suzuki, H. Takagi, Y. Asami, H. Kakeya, M. Uramoto, T. Usui, S. Takahashi, Y. Sugimoto, H. Osada. Identification of cytochrome P450s required for fumitremorgen biosynthesis in Aspergillus fumigatus. ChemBioChem. 10, 920-928, 2009.
1) Y. Hayashi, K. Sankar, H. Ishikawa, Y. Nozawa, K. Mizoue, H. Kakeya. Total synthesis and determination of the absolute configuration of FD-838, a naturally occuring azaspirobicyclic product. Bioorg. Med. Chem. Lett. 19, 3863-3865, 2009

2008

原著論文：
6) Y. Asami, H. Kakeya, Y. Komi, S. Kojima, K. Beebe, L. Neckers, K. Nishikawa, H. Osada. Azaspirene, a fungal product, inhibits angiogenesis by blocking raf-1 activation. Cancer Sci. 99, 1853-1858, 2008. [Selected as an issue highlight and a cover page.]
5) H. Kamiyama, T. Usui, H. Sakurai, M. Shoji, Y. Hayashi, H. Kakeya, H. Osada. Epoxyquinol B, a naturally occurring pentaketide dimer, inhibits NF-κB signaling by crosslinking TAK1. Biosci. Biotechnol. Biochem. 72, 1894-1900, 2008.
4) Y. Hayashi, M. Shoji, H. Ishikawa, J. Yamaguchi, T. Tamura, H. Imai, Y. Nishigaya, K. Takabe, H. Kakeya, H. Osada, First asymmetric total synthesis of (+)-cytotrienin A, an ansamycin-type anticancer drug. Angew. Chem. Int. Ed. 47, 6657-6660, 2008.
3) H. Kamiyama, T. Usui, M. Uramoto, H. Takagi, M. Shoji, Y. Hayashi, H. Kakeya, H. Osada. Fungal metabolite, epoxyquinol B crosslinks proteins by epoxy-thiol conjugation. J. Antibiot. 61, 94-97 (2008).
2) H. Kamiyama, H. Kakeya, T. Usui, K. Nishikawa, M. Shoji, Y. Hayashi, H. Osada. Epoxyquinol B shows antiangiogenic effects in vitro and in vivo by inhibiting VEGFR, and EGFR, FGFR, and PDGFR. Oncol. Res. 17, 11-21, 2008.
1) HD. Jain, C. Zhang, S. Zhou, H. Zhou, J. Ma, X. Liu, AM. Deveau, CM. Dieckhaus, MA. Johnson, KS. Smith, TL. Macdonald, H. Kakeya, H. Osada, JM, Cook. Synthesis and structure-activity relationship studies on tryprostatin A, an inhibitor of breast cancer resistance protein. Bioorg. Med. Chem. 16, 4626-4651, 2008.
総説・著書：
5) 西村慎一、掛谷秀昭. 生体高分子の多面性の理解に向けたケミカルジェネティクス：新規素材探索とその応用. 新規素材探索―医薬品リード化合物・食品素材を求めて―（上村大輔（監修）、シーエムシー出版）、 pp. 85-94, 2008年.
4) 掛谷秀昭. "微生物"からの贈り物. 入門・ケミカルバイオロジー. （入門・ケミカルバイオロジー編集委員会（編）、オーム社）、pp. 11-25, 2008年.
3) 掛谷秀昭、大石真也、矢倉徹、藤井信孝. 創薬研究における化合物ライブラリー. インシリコ創薬科学―ゲノム情報から創薬へ―（藤井信孝、辻本豪三、奥野恭史（編）、京都廣川書店）、pp. 46-62, 2008年.
2) 服部明、掛谷秀昭. ケミカルジェネティクスを基盤としたケモゲノミクスおよびケミカルバイオロジー. インシリコ創薬科学―ゲノム情報から創薬へ―（藤井信孝、辻本豪三、奥野恭史（編）、京都廣川書店）、pp. 37-46, 2008年.
1) 掛谷秀昭. ケミカルバイオロジー研究による新たな創薬標的の提示. 化学, 63，68-69，2008年.

2007

　　　　　
総説・著書：
5) 掛谷秀昭. 有用天然有機化合物の開拓とケミカルバイオロジー研究. 平成19年度後期（秋季）有機合成化学講習会テキスト-有機合成化学のダイナミズム：その基礎から広範な応用まで. 有機合成化学協会(編). 89-100, 2007.
4) 掛谷秀昭. 微生物が生産する新規生理活性物質の開拓とケミカルバイオロジー研究. Jpn. J. Antibiot. 60, 181-187, 2007.
3) 掛谷秀昭、長田裕之. 天然物化学・生命科学ディビジョンレポート ―医薬品探索と創薬研究；ケミカルバイオロジー研究. 日本化学会. 2007.
2) 掛谷秀昭、齋藤安貴子、長田裕之. 微生物代謝産物由来の小分子ライブラリーの利用技術-スクリーニングとケミカルバイオロジー研究-, BIO INDUSTRY , 24, 48-54, 2007
1) 掛谷秀昭. Natural products-based chemical biology -独創的なケミカルバイオロジー研究を目指して-. バイオサイエンスとインダストリー, 65, 75, 2007.

-2006

原著論文：
75) Y. Asami, H. Kakeya, G. Okada, M. Toi, H. Osada. RK-95113, a new angiogenesis inhibitor produced by Aspergillus fumigatus. J. Antibiot. 59, 724-728, 2006.
74) M. Matsuzawa, H. Kakeya, J. Yamaguchi, M. Shoji, R. Onose, H. Osada, Y. Hayashi. Enantio- and diastereoselective total synthesis of (+)-panepophenanthrin, an ubiquitin-activating enzyme inhibitor, and biological properties of its new derivatives. Chem. Asian J. 1, 845-851, 2006.
73) N. Watanabe, Y. Nishihara, T. Yamaguchi, A. Koito, H. Miyoshi, H. Kakeya, H. Osada. Fumagillin suppresses HIV-1 infection of macrophages through the inhibition of VPR activity. FEBS Lett. 580, 2598-2602, 2006.
72) H. Taguchi, A. Ohkubo, M. Sekine, K. Seio, H. Kakeya, H. Osada, T. Sasaki. Synthesis and biological properties of new phosmidosine analogs having an N-acylsulfamate linkage. Nucleos. Nucleot. Nucl. 25, 647-654, 2006.
71) I. Shiina, T. Uchimaru, M. Shoji, H. Kakeya, H. Osada, Y. Hayashi. Computational study on the reaction mechanism of the key thermal [4+4] cycloaddition reaction in the biosynthesis of epoxytwinol A. Org. Lett. 8, 1041-1044, 2006.
70) J. Yamaguchi, M. Toyoshima, M. Shoji, H. Kakeya, H. Osada, Y. Hayshi. Concise, enantio- and diastereo-selective total syntheses of fumagillol, RK-805, FR65814, ovalicin and 5-demethylovalicin, using the proline-mediated, catalytic, asymmetric a-aminoxylation. Angew. Chem. Int. Ed. 45, 789-793, 2006.
69) H. Tomiki, T. Saito, M. Ueki, H. Konno, T. Asaoka, R. Suzuki, M. Uramoto, H. Kakeya, H. Osada. RIKEN natural products encyclopedia (RIKEN NPEdia), a chemical database of RIKEN natural products depository (RIKEN NPDepo). J. Comput. Aided Chem. 7, 156-161, 2006.
68) H. Kakeya, R. Onose, H. Koshino, H. Osada. Epoxytwinol A, a novel unique angiogenesis inhibitor with C2 symmetry, produced by a fungus. Chem. Commun. 2005, 2575-2577, 2005.
67) Y. Nagumo, H. Kakeya, M. Shoji, Y. Hayashi, N. Dohmae, and H. Osada. Epolactaene binds human Hsp60 Cys442 resulting in the inhibition of chaperone activity. Biochem. J. 387, 835-840, 2005.
66) M. Shoji, T. Uno, H. Kakeya, R. Onose, I. Shiina, H. Osada, Y. Hayashi. Enantio- and diastereo-selective total synthesis of EI-1941-1, -2, and ?3, inhibitors of interleukin-1b converting enzyme and biological properties of their derivatives. J. Org. Chem., 70, 9905-9915, 2005.
65) T. Mitsui, Y. Miyake, H. Kakeya, Y. Hayashi, H. Osada, T. Kataoka. RKTS-33, an epoxycyclohexenone derivative that specificically inhibits Fas ligand-dependent apoptosis in CTL-mediated cytotoxicity. Biosci. Bitechnol. Biochem. 69, 1923-1928, 2005.
64) J. Yamaguchi, H. Kakeya, T. Uno, M. Shoji, H. Osada, Y. Hayashi. Determination by asymmetric total synthesis of the absolute configuration of lucilactaene, a cell cycle inhibitor in p53-transfected cancer cells. Angew. Chem. Int. Ed. 44, 3110-3115, 2005.
63) Y. Hayashi, M. Shoji, T. Mukaiyama, H. Gotoh, S. Yamaguchi, M. Nakata, H. Kakeya, H. Osada. The first asymmetric total synthesis of synerazol, an antifungal antibiotic, and determination of its absolute stereochemistry. J. Org. Chem. 70, 5643-5654, 2005.
62) M. Shoji, H. Imai, M. Mukaida, K. Sakai, H. Kakeya, H. Osada, and Y. Hayashi. Total synthesis of epoxyquinols A, B, and C and epoxytwinol A and the reactivity of a 2H-pyran derivatives as the diene component in the Diels-Alder reaction. J. Org. Chem. 70, 79-91, 2005.
61) Y. Nagumo, H. Kakeya, J. Yamaguchi, T. Uno, M. Shoji, Y. Hayashi, and H. Osada. Structure-activity relationships of epolactaene derivatives: Structural requirements for inhibition of HSP60 chaperone activity. Bioorg. Med. Chem. Lett., 14, 4425-4429, 2004.
60) Y. Asami, H. Kakeya, R. Onose, Y. ?H. Chang, M. Toi, and H. Osada. RK-805, an endothelial-cell-growth inhibitor produced by Neosartorya sp., and a docking model with methionine aminopeptidase-2. Tetrahedron, 60, 7085-7091, 2004.
59) T. Mitsui, Y. Miyake, H. Kakeya, and H. Osada. Epoxycyclohexenone, a specific inhibitor of Fas ligand-dependent apoptosis in CCTL-mediated cytotoxicity. J. Immunology. 172, 3423-3436, 2004.
58) M. Sekine, K. Okada, K. Seio, T. Obata, T. Sasaki, H. Kakeya, H. Osada. Synthesis of a biotin-conjugate of phosmidosine O-ethyl ester as a G1 arrest antitumor drug. Bioorg. Med. Chem. 12, 6343-6349, 2004.
57) M. Sekine, K. Okada, K. Seio, H. Kakeya, H. Osada, T. Sasaki. Structure-activity relationship of phosmidosine: importance of the 7,8-dihydro-8-oxoadenosine residue for antitumor activity. Bioorg. Med. Chem., 12, 5193-5201, 2004
56) M. Sekine, K. Okada, K. Seio, H. Kakeya, H. Osada, T. Obata, T. Sasaki. Synthesis of chemically stabilized phosmidosine analogues and the structure-activity relationship of phosmidosine. J. Org. Chem., 69, 314-326, 2004.
55) M. Shoji, H. Imai, I.Shiina, H. Kakeya, H. Osada, and Y. Hayashi. Different reaction modes for the oxidative dimerization of epoxyquinols and epoxyquinones ? Importance of the intermolecular hydrogen-bonding. J. Org. Chem. 69, 1548-1556, 2004.
54) H. Kakeya, Y. Miyake, M. Shoji, Satoshi Kishida, Y. Hayashi, T. Kataoka, and H. Osada Novel non-peptide inhibitors targeting death receptor-mediated apoptosis. Bioorg. Med. Chem. Lett., 13, 3743-3746, 2003.
53) M. Shoji, S. Kishida, Y. Kodera, I. Shiina, H. Kakeya, H. Osada, and Y. Hayashi. Reaction modes of oxidative dimerization of epoxycyclohexenols. Tetrahedron Lett., 44, 7205-7207, 2003.
52) Y. Hayashi, M. Shoji, S. Yamaguchi, T. Mukaiyama, J. Yamaguchi, H. Kakeya, and H. Osada. Asymmetric total synthesis of pseurotin A. Org. Lett. 5, 2287-2290, 2003.
51) Y. Miyake, H. Kakeya, T. Kataoka, and H. Osada. Epoxycyclohexenone inhibits Fas-mediated apoptosis by blocking activation of pro-caspase-8 in the death-inducing signaling complex. J. Biol. Chem. 278, 11213-11220, 2003.
50) S. Su, H. Kakeya, H. Osada, and J. Porco, Jr. Synthesis and cell cycle inhibition of the peptide enamide natural products terpeptin and the aspergillamides. Tetrahedron, 59, 8931-8946, 2003.
49) H. Kakeya, R. Onose, H. Koshino, A. Yoshida, K. Kobayashi, S.-I. Kageyama, and H. Osada. Epoxyquinol A, a highly functionalized pentaketide dimer with antiangiogenic activity isolated from fungal metabolites. J. Am. Chem. Soc. 124, 3496-3497, 2002.
48) H. Kakeya, R. Onose, A. Yoshida, H. Koshino, and H. Osada. Epoxyquinol B, a fungal metabolite with a potent antiangiogenic activity. J. Antibiot. 55, 829-831, 2002.
47) M. Shoji, J. Yamaguchi, H. Kakeya, H. Osada, and Y. Hayashi. Total synthesis of (+)-epoxyquinols A and B. Angew. Chem. Int. Ed. 41, 3192-3194, 2002.
46) H. Kakeya, N. Takahashi-Ando, M. Kimura, R. Onose, I. Yamaguchi, and H. Osada. Biotransformation of the mycotoxin zearalenone to a non-estrogenic compound by a fungal strain Clonostachys sp. Biosci. Bitechnol. Biochem. 66, 2723-2726, 2002.
45) M. Shoji, S. Kishida, M. Takeda, H. Kakeya, H. Osada, and Y. Hayashi. A practical total synthesis of both enantiomers of epoxyquinols A and B. Tetrahedron Lett., 43, 9155-9158, 2002.
44) Y. Asami, H. Kakeya, R. Onose, A. Yoshida, H. Matsuzaki, and H. Osada. Azaspirene: A novel angiogenesis inhibitor containing 1-oxa-7-azaspirol[4.4]non-2-ene-4,6-dione skeleton produced by the fungus Neosartorya sp. Org. Lett. 4, 2845-2848, 2002.
43) Y. Hayashi, M. Shoji, J. Yamaguchi, K. Sato, S. Yamaguchi, T. Mukaiyama, K. Sakai, Y. Asami, H. Kakeya, and H. Osada. Asymmetric total synthesis of (-)-azaspirene, a novel angiogenesis inhibitor. J. Am. Chem. Soc. 124, 12078-12079, 2002.
42) N. Takahashi-Ando, M. Kimura, H. Kakeya, H. Osada., and I. Yamaguchi. A lactonohydrolase responsible for the detoxification of zearalenone. Enzyme purification and gene cloning. Biochemical J. 365, 1-6, 2002.
41) H.-R. Ko, H. Kakeya, A. Yoshida, R. Onose, M. Ueki, M. Muroi, A. Takatsuki, H. Matsuzaki, and H. Osada. PC-766B’ and PC-766B, 16-membered macrolide angiogenesis inhibitors produced by Nocardia sp. RK97-56. J. Micobiol. Biotechnol., 12, 829-833, 2002.
40) H. Kakeya, S.-I. Kageyama, L. Nie, R. Onose, G. Okada, T. Beppu, C. J. Norbury, and H. Osada. Lucilactaene, a new cell cycle inhibitor in p53-transfected cancer cells, produced by a Fusarium sp. J. Antibiot., 54, 850-854, 2001.
39) L. Nie, M. Ueki, H. Kakeya, and H. Osada. A facile and effective screening method for p21WAF1 promoter activators from microbial metabolites. J. Antibiot., 54, 783-788, 2001.
38) M. Watabe, R. Onose, A. Ikeno, H. Kakeya, and H. Osada. Effect of microgravity on cell proliferation signal. J. Japan Society of Microgravity Application. 17, 87~90, 2000.
37) M. Watabe, H. Kakeya, R. Onose, and H. Osada. Activation of MST/Krs and c-Jun-N-terminal kinases by different signaling pathways during cytotrienin A-induced apoptosis. J. Biol. Chem., 275, 8766~8771, 2000.
36) H. Kakeya, R. Onose, and H. Osada. Activation of a 36-kD MBP kinase, an active proteolytic fragment of MST/Krs proteins, during anticancer drug-induced apoptosis. Ann.N.Y. Acad. Sci., 886, 273~275, 1999.
35) A. Sato, T. Hamazaki, T. Oomura, H. Osada, H. Kakeya, M. Watabe, T. Nakamura, Y. Nakamura, N. Koshikawa, I. Yoshizaki, S. Aizawa, S. Yoda, A. Ogiso, M. Takaoki, Y. Kohno, and H. Tanaka. Effect of microgravity on c-fos gene expression in osteoblast-like MC3T3-E1 cells. Life Sciences, Microgravity Research II, 24, 807~813, 1999.
34) H. Kakeya, M. Morishita, H. Koshino, T.-i. Morita, K. Kobayashi, and H. Osada. Cytoxazone: a novel cytokine modulator containing 2-oxazolidinone ring produced by Streptomyces sp. J. Org. Chem., 64, 1052~1053, 1999.
33) M. Watabe, H. Kakeya, and H. Osada. Requirement of protein kinase (Krs/Mst) ctivation for MT-21-induced apoptosis. Oncogene, 18, 5211~5220, 1999.
32) H. Kakeya, R. Onose, and H. Osada. Caspase-mediated activation of a 36-kDa myelin basic protein kinase during anticancer drug-induced apoptosis. Cancer Res., 58, 4888~4894, 1998.
31) H. Kakeya, M. Morishita, K. Kobinata, M. Osono, M. Ishizuka, and H. Osada. Isolation and biological activity of a novel cytokine modulator, cytoxazone. J. Antibiot,. 51, 1126~1128, 1998.
30) K.-i. Togashi, H. Kakeya, M. Morishita, Y.-X. Song, and H. Osada. Inhibition of human telomerase activity by alterperylenol. Oncol. Res., 10, 449~453,1998.
29) H. Kakeya, R. Onose, P. C. C. Liu, C. Onozawa, F. Matsumura, and H. Osada. Inhibition of cyclin D1 expression and phosphorylation of retinoblastoma protein by phosmidosine, a nucleotide antibiotic. Cancer Res., 58, 704-710, 1998
28) H. Kakeya and H. Osada. Induction of neurite outgrowth by epolactaene derivatives, 3-substituted 3-pyrrolin-2-ones. RIKEN Review, 18, 35-36, 1998.
27) H. Kakeya, M. Morishita, A. Ikeno, K. Kobinata, T. Yano, and H. Osada. Factumycin and its new derivative RK-1009 enhance threonine-phophorylation of a 60-kDa protein in Streptomyces griseus. J. Antibiot., 51, 963~966, 1998.
26) H.-p. Zhang, H. Kakeya, and H. Osada. Biosynthesis of 1-aminocyclopropane-1-carboxylic acid moiety on cytotrienin A in Streptomyces sp. Tetrahedron Lett., 39, 6947-6948, 1998.
25) H. Kakeya, M. Morishita, C. Onozawa, K.-i. Kimura, M. Yoshihama, R. Usami, K. Horikoshi, and H. Osada. RKS-1778, a new mammalian cell-cycle inhibitor and a key intermediate of the [11]cytochalasin group. J. Nat. Prod., 60, 669~672, 1997.
24) H. Kakeya, H.-p. Zhang, K. Kobinata, R. Onose, C. Onozawa, T. Kudo, and H. Osada. Cytotrienin A, a novel apoptosis inducer in human leukaemia HL-60 Cells. J. Antibiot., 50, 370~372 , 1997.
23) H.-p. Zhang, H. Kakeya, and H. Osada. Novel triene-ansamycins, cytotrienins A and B inducing apoptosis on human leukaemia HL-60 Cells. Tetrahedron Lett., 38, 1789~1792, 1997.
22) H. Kakeya, C. Onozawa, M. Sato, K. Arai, and H. Osada. Neuritogenic effect of epolactaene derivatives on human neuroblastoma cells which lack high-affinity nerve growth factor receptors. J. Med. Chem., 40, 391~394, 1997.
21) C.-B. Cui, H. Kakeya and H. Osada. Novel mammalian cell cycle inhibitors, cyclotryprostatins A-D, produced by Aspergillus fumigatus, which inhibit mammalian cell cycle at G2/M phase. Tetrahedron, 53, 59~72, 1997.
20) M. Ubukata, T.-i. Morita, H. Kakeya, K. Kobinata, T. Kudo, and H. Osada. Sparoxomycins A1 and A2, new inducers of the flat reversion of NRK cells transformed by temperature sensitive Rous Sarcoma Virus. I. Taxonomy of the producing organism, fermentation and biological Activity. J. Antibiot., 49, 1096~1100, 1996.
19) C.-B. Cui, H. Kakeya and H. Osada. Novel mammalian cell cycle inhibitors, spirotryprostatins A and B, produced by Aspergillus fumigatus, which inhibit mammalian cell cycle at G2/M phase. Tetrahedron, 52, 12651~12666, 1996.
18) C.-B. Cui, H. Kakeya and H. Osada. Spirotryprostatin B, a novel mammalian cell cycle inhibitor produced by Aspergillus fumigatus. J. Antibiot., 49, 832~835, 1996.
17) C.-B. Cui, H. Kakeya, G. Okada, R. Onose and H. Osada. Novel mammalian cell cycle inhibitors, tryprostatins A, B and other diketopiperazines produced by Aspergillus fumigatus. I. Taxonomy, fermentation, isolation and biological properties. J. Antibiot., 49, 527~533, 1996.
16) C.-Bin C., H. Kakeya and H. Osada. Novel Mammalian Cell Cycle Inhibitors, Tryprostatins A, B and other diketopiperazines produced by Aspergillus fumigatus. II. Physico-chemical properties and structure. J. Antibiot., 49, 534~540, 1996.
15) C.-B. Cui, M. Ubukata, H. Kakeya, R. Onose, G. Okada, I. Takahashi, K. Isono and H. Osada. Acetophthalidin, a novel inhibitor of mammalian cell cycle, produced by a fungus isolated from a sea sediment. J. Antibiot., 49, 216~219, 1996.
14) C.-B. Cui, H. Kakeya, G. Okada, R. Onose, M. Ubukata, I. Takahashi, K. Isono and H. Osada. Tryprostatins A and B, novel mammalian cell cycle inhibitors produced by Aspergillus fumigatus. J. Antibiot., 48, 1382~1384, 1995.
13) H. Kakeya, I. Takahashi, G. Okada, K. Isono, and H. Osada. Epolactaene, a novel neuritogenic compound in human neuroblastoma cells, produced by a marine fungus. J. Antibiot., 48, 733~735, 1995.
12) H. Kakeya, M. Imoto, Y. Takahashi, H. Naganawa, T. Takeuchi, and K. Umezawa. Dephostatin, a novel protein tyrosine phosphatase inhibitor produced by Streptomyces. II. Structure determination. J. Antibiot., 46, 1716~1719, 1993.
11) M. Imoto, H. Kakeya, T. Sawa, M. Hamada, C. Hayashi, T. Takeuchi, and K. Umezawa. Dephostatin, a novel protein tyrosine phosphatase inhibitor produced by Streptomyces. I. Taxonomy, isolation, and characterization. J. Antibiot., 46, 1342~1346, 1993.
10) Y. Watanabe, H. Kakeya, E. Ikoma, and K. Umezawa. Induction of morphological and enzymic differentiation in rat pheochromocytoma PC12h cells by stable erbstatin analogues. Drugs Exptl. Clin. Res., XIX, 1~6, 1993.
9) H. Kakeya, M. Imoto, Y. Tabata, J. Iwami, H. Matsumoto, K. Nakamura, K.-i. Tadano, and K. Umezawa. Isolation of a novel tyrosine kinase inhibitor, desmal, from the plant Desmos chinensis. FEBS Lett., 320, 169~172, 1993.
8) H. Kakeya, N. Sakai, A. Sano, M. Yokoyama, T. Sugai, and H. Ohta. Microbial hydrolysis of 3-substituted glutaronitriles. Chem. Lett., 1823~1824, 1991.
7) H. Kakeya, N. Sakai, T. Sugai, and H. Ohta. Preparation of optically active a-hydroxy acid derivatives by microbial hydrolysis of cyanohydrins and its application to the synthesis of (R)-4-dodecanolide. Agric. Biol. Chem., 55, 1877~1881, 1991.
6) H. Kakeya, N. Sakai, T. Sugai, and H. Ohta. Microbial hydrolysis as a potent method for the preparation of optically active nitriles, amides, and carboxylic acids. Tetrahedron Lett., 32, 1343~1346, 1991.
5) H. Kakeya, T. Sugai, and H. Ohta. Biochemical preparation of optically active 4-hydroxy-b-ionone and its transformation to (S)-6-hydroxy-a-ionone. Agric. Biol. Chem., 55, 1873~1876, 1991.
4) T. Sugai, H. Kakeya, and H. Ohta. A Synthesis of (R)-(-)-mevalonolactone by the combination of enzymatic and chemical methods. Tetrahedron, 46, 3463~3468, 1990.
3) M. Morooka, S. Ohba, T. Sugai, H. Kakeya, H. Ohta, and Y. Saito. Structure of (±)-2-hydroxymethyl-2,6-dimethylcyclohexan-1-ol. Acta. Crystallogr., C46, 168-170, 1990
2) T. Sugai, H. Kakeya, and H. Ohta. Enzymatic preparation of enantiomerically enriched tertiary a-benzyloxy acid esters. Application to the synthesis of (S)-(-)-frontalin. J. Org. Chem., 55, 4643~4647, 1990.
1) T. Sugai, H. Kakeya, H. Ohta, M. Morooka, and S. Ohba. A synthesis of (-)-deoxypodocarpic acid methyl ester via an enzymatic enantioselective hydrolysis by the key intermediate enol ester. Tetrahedron, 45, 6135~6144, 1989.
解説・総説 (review)
22) 長田裕之、 掛谷秀昭.　固形がんの征圧を目指した抗がん剤の開発. がん分子標的治療. 4, 24-31, 2006.
21) K. Kikuchi, H. Kakeya. A bridge between chemistry and biology. Nature Chem. Biol. 2, 392-394, 2006.
20) 掛谷秀昭. Researcher’s eye“ものとり”と“匠”. 三田評論 (慶應義塾大学出版会), 1093, 64, 2006.
19) 掛谷秀昭. (書評) バイオテクノロジー教科書シリーズ17「天然物化学」. 有機合成化学協会誌. 64, 968, 2006.
18) 掛谷秀昭. （書評）マッキー生化学　分子から解き明かす生命「第3版」. バイオサイエンスとインダストリー. 63, 772, 2005.
17) H.-J. Kwon、(訳) 掛谷秀昭.　新しい血管新生阻害剤におけるケミカルゲノミクス. 蛋白質 核酸 酵素. 50, 1056-1062, 2005.
16) 掛谷秀昭、長田裕之. 血管内皮増殖因子(VEGF)の機能を標的とした新規血管新生阻害剤. 日本臨床. 62, 1264-1270, 2004.
15) 長田裕之、掛谷秀昭. 癌分子標的治療のための新しい血管新生阻害剤. 日本臨床. 62, 1257-1263, 2004.
14) 三宅靖延、掛谷秀昭、長田裕之. デスレセプター依存性アポトーシス抑制化合物ECHの作用機序および標的分子. 日本臨床. 62, 1283-1289, 2004.
13) 掛谷秀昭. 細胞の生死を制御する天然有機化合物を利用した化学生物学的研究. 日本農芸化学会誌. 76, 708-713, 2002.
12) 掛谷秀昭、長田裕之. がん征圧と化学-最新抗がん剤事情-. 化学と工業. 55, 555-559, 2002.
11) 掛谷秀昭. 低分子マイクロアレイ-有機化学を基盤としたポストゲノム科学への挑戦-. 化学、 56, 60-61, 2002.
10) 掛谷秀昭. 抗感染症薬の標的：ミトコンドリア呼吸鎖・複合体I. ファルマシア. 38, 247-248, 2002.
9) 掛谷秀昭、三宅靖延、長田裕之. ミトコンドリアを標的にした抗癌剤 -アポトーシス研究におけるバイオプローブの貢献-、化学、 56, 60-61, 2001.
8) 長田裕之、掛谷秀昭.　バイオプローブの開発動向と将来性、科学技術予測レポート第4巻「バイオテクノロジー」、107-112, 2000.
7) 渡部正彦、小野瀬利恵、池野あゆみ、掛谷秀昭、長田裕之.　細胞の増殖シグナルに及ぼす微小重力の影響、日本マイクログラビティ応用学会誌、17, 87-90, 2000.
6) H. Kakeya and H. Osada. Induction of neurite outgrowth by epolactaene derivatives, 3-substituted 3-pyrrolin-2-ones. RIKEN Review, 18, 35-36, 1998.
5) 長田裕之、臼井健郎、掛谷秀昭.　アポトーシス誘導性バイオプローブの探索と作用機構、バイオインダストリー、15, 14-21, 1998.
4) 長田裕之、八尾良司、掛谷秀昭.　神経栄養因子活性を示す低分子化合物、組織培養工学、23, 511-513, 1997.
3) 掛谷秀昭、長田裕之. 海洋に住む微生物から抗癌剤を探す、日本農芸化学会誌、71, 512-515, 1997.
2) 掛谷秀昭.　低分子バイオプローブを利用して初めて哺乳類ヒストンデアセチラーゼが同定された、化学と工業、50, 627, 1997.
1) 掛谷秀昭.　脳疾患治療薬を目指した微生物由来の化合物、バイオサイエンスとインダストリー、53, 973-975,1995.