Publications

-Publication List-
TBA (to be announced)

2024

224) Kaneko, K., Mieda, M., Jiang, J., 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. [Press release]
223) Iseki, S.,# Ikeda, H.,# Kobayashi, S., Irie, K., Harada, H. Kakeya, H. (TBA) (#equal contribution)
222) 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)
221) Lu, S., Ren, L., Mao, D., Kakeya, H. (TBA)
220) 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)
219) Hayashi, K., Takahashi, N., Furutani, Y., Toguchi, M., Shiozaki-Sato, Y., Sudoh, M., Kojima, S., Kakeya, H. (TBA)
218) 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, 2023.
217) Takahashi, S., Nakayama, J., Lu, S., Jiang, Y., Yamane, S., Nishimura, S., Hattori, A., Kakeya, H. (TBA)
216) Kakeya, H. (TBA)
215) Ishikawa, F., Konno, S., Kakeya, H., Tanabe, G. Develpment of a chemical scaffold for inhibiting nonribosomal peptide synthetases in live bacterial cells. Beilstein, J. Org. Chem. 20, 445-451, 2024.
214) Takenaka, K., Kaneko, K., Takahashi, N., Nishimura, S., Hattori, A. Kakeya, H. (TBA)
213) Abe, T., Kishimoto, A., Katsuura, Y., Imaizumi, A., Hashimoto, T., Asakura, T., Minowa, H., Aoki, K., Kakeya, H., Kanai, M. (TBA)
212) 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)

2023

211) 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 lung cancer A549 cells. Eur. J. Pharmacol. 960, 176156, 2023. [Press release]
210) 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 aryl hydrocarbon receptor. Cell Death Discov. 9, 216, 2023. [Press release]
209) Ozaki, M., Shimotsuma, M., Kuranaga, K., 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, in press, 2023. [selected as a Front Cover]
208) 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.
207) Ozaki, M., Shimotsuma, M., Kuranaga, K., 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.
206) 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 autoencoder-based model of constructing chemical latent space for large molecular structures with 3D complexity. Commun. Chem. 6, 249, 2023.
205) 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]

2022

204) 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]
203) Sasaki, M., Nishimura, S., Yashiroda, Y., Matsuyama, A., Kakeya, H., Yoshida, M. FK506 binding protein, FKBP12, promotes serine utilization and nagatively regulates threonine deaminase in fission yeast. iScience, 25, 105659, 2022. [press release]
202) Ishikawa, F., Konno, S., Uchiyama, Y., Takashima, K., Kakeya, H., Tanabe, G. Explring 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.
201) Matsumoto, T., Kuranaga, T., Taniguchi, Y., Wang, W., Kakeya, H. Solid-phase total synthesis and structural confirmation of antimicrobial longicatenamide A. Bielstein J. Org. Chem. 18, 156-1566, 2022.
200) Ozaki, M., Kuwayama, T., Hirose, T., Shimotsuma, M., Hashimoto, A., Kuranaga, T., Kakeya, H. Separation and identification of the DL-forms of short-chain eptides using a new chiral resolutuion labeling reagent. Anal. Bioanal. Chem. 414, 4039-4046, 2022..
199) 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 initioation modules to evaluate mechanism. RSC Chem. Biol. 3, 312-319, 2022.
198) Lu, S., Jiang, Y., Shinzato, N., Teruya, Y., Shimo, T., Nishime, A., Kakeya, H. (TBA)
197) 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 Enzymology, 665, 105-133, 2022.
196) 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

195) Khadka, S., Omura, S., Sato, F., Nishio, K., Kakeya, H., Tsunoda, I. Curcumin beta-D-glucuronide modulates an autoimmune model of multiple sclerosis with altered gut microbiota in the ileum and feces. Front. Cell. Infect. Microbiol. 11, Article 772962, 2021. [Press release]
194) Sakai, M., Takahashi, N., Ikeda, H., Furutani, Y.,Higuchi, S., Kobayashi, S., Harada, H., Kojima, S., Matsuura, T., Hattori, A., Kakeya, H. Design, synthesis, and target identification of new hypoxia-inducible factor 1 (HIF-1) inhibitors containing 1-alkyl-1H-pyrazole-3-carboxamide moiety. Bioorg. Med. Chem. 46, 116375, 2021.
193) Kuranaga, T., Tamura, M., Ikeda, H., Terada, S., Nakagawa, S., Kakeya, H. Identification and total synthesis of an unstable anticancer macrolide presacchrothriolide Z produced by Saccharothrix sp. A1506. Org. Lett. 23, 7106-7111, 2021. [Highlight in the category of "Chemistry in Medicine and Biology", Synfacts, 18, 0095, 2022]
192) Ikeda, H. Kakeya, H. Targeting hypoxia-inducible factor 1 (HIF-1) signaling with natural products towards cancer chemotherapy. J. Antibiot. 2021, 74, 687-695, 2021. [The special issue in "Approach toward cancer-targeting therapy by microbial origin"]
191) Liu, C., Hashimoto, J., Kudo, K., Shin-ya, K., Kakeya, H. An atypical arginine dihydolase involved in the biosynthesis of cyclic hexapeptide longicatenamides. Chem. Asian J. 16, 1382-1387, 2021.
190) 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 Amycolatopsis sp. and Tsukamurella pulmonis. J. Org. Chem. 86, 1843-1849, 2021.
189) 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.
188) 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.
187) 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.
186) 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.
185) 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.
184) 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.
183) 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 confomational and reactivity analysis. J. Org. Chem. 86, 16231-16248, 2021.
182) Ishikawa, F., Konno, S., Uchida, C., Suzuki, T., Takashima, K., Dohmae, N., Kakeya, H., Tanabe, G. Chemoproteomics profiling of surfactin-producing process of nonribosormal peptide synthetases in vitro and in living bacterial cells. Cell Chem. biol. 28, 1-21, 2021.
181) Ishikawa, F., Konno, S., Takashima, K., Kakeya, H., Tanabe, G. Inhibition of efflux pumps aids small-molecul probe-based fluorescence labeling and imaging in the gram-negative bavterium Escherichia coli. Org. Biomol. Chem. 19, 8906-8911, 2021.
180) Matsuoka, T., Motozono, C., Hattori, A., Kakeya, H., Sho Yamasaki, 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.
179) 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.
178) 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.
177) 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.

2020

176) 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]
175) Pan, C., Kuranaga, T., Kakeya, H. Total synthesis of thioamycolamide A via a biomimetic route. Org. Biomol. Chem. 18, 8366-8370, 2020.
174) 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.
173) 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. dio: 10.1038/s42003-020-0942-0. [Press release]
172) 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.
171) Takahashi, N., Kaneko, K., Kakeya, H. Total synthesis and antimicrobial activity of tumescenamide C and its derivatives. J. Org. Chem. 85, 4530-4535, 2020.
170) 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.
160) Shimizu, K., Funamoto, M., Sunagawa, Y., Wakabayashi, H., Genpei, M., Miyazaki, Y., Katanasaka, Y., Sari N., Shimizu, S., 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 overloaded-induced heart failure in mice. Sci. Rep. 10, 7172, 2020.
168) Baba, K., Kuwada, S., Nakao, A., Li, X., Okuda, N., Nishida, A., Mitsuda, 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.
167) Liu, C., Kakeya, H. Cryptic Chemical Comunication: Secondary metabolic responses revealed by microbial co-culture. Chem. Asian J. 15, 327-337. [Selected as a cover feature.]
166) 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]
165) 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.

2019

164) Sugiyama, R., Nakatani, T., Nishimura, S., Takenaka, K., Ozaki, T., Asamizu, S., Onaka, H., 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. [Press release]
163) Yoshimura, A., Nishimura, S., Suzuki, T., Hattori, A., Dohmae, N. Kato, T., Kakeya, H. Isolation, structure elucidation and conformational regulation of myropeptins, new lipopeptides from a fungus Myrothecium rodium. Org. Lett. in press, 2019.
162) 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.
161) Kakeya, H., Kuranaga, T. Precious Micoorganisms as Productive Resources: Marine-derived Microorganisms and Combined-Culture. Comprehensive Natural Products III: Chemistry and Biology, Elsevier., in press, 2019.
160) 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]
159) 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. in press.
158) 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.
157) 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.
156) 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.
155) 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. [Selected as a HOT article collection.]

2018

154) 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.
153) Kakeya, H. Natural products-inspired chemcial biology towardd development of new antibiotics. Jpn. J. Antibiot. 71, 181-191, 2018.
152) 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)
151) Lu, S., Nishimura, S., 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, 2019. [Press release]

2017

150) 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]
149) 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.
148) 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.
147) 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.
146) 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]

2016

145) 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.
144) 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]
143) Kasai, S., Ishikawa, F., Suzuki, T., Dohmae, N., Kakeya, H. A chemical proteomic probe for detecting native carrier protein motifs in nonribosomal peptide synthetases. Chem. Commun. 52, 14129-14132, 2016.
142) Matsumoto, Y., Hibino, K., Yonaga, M., Kakeya, H., Hayashi, Y. Enantioselective total synthesis of RQN-18690A (18-deoxyherboxidiene). Org. Lett. 18, 3382-3385, 2016.
141) Lu, S., Nishimura, S., Ito, M., Tsuchida, T., Kakeya, H. Isolation and structure determination of cytotoxic sacharothriolides D to F from a rare actinomycete Saccharothrix sp. and their structure-activity relationship. J. Nat. Prod. 79, 1891-1895, 2016.
140) Ishikawa, F., Sugimoto, Y., Kakeya, H. In vitro investigation of crosstalk between fatty acid and polyketide synthases in the andrimid biosynthetic assembly line. ChemBioChem. 17, 2137-2142, 2016.
139) 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.
138) Ishikawa, F., Kakeya, H. A competitive enzyme-linked immunosorbent assay system for adenylation domains in nonribosormal peptide synthetases. ChemBioChem. 17, 474-478, 2016.
137) 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.
136) 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.
135) Ishikawa, F., Kakeya, H. Affinity purification method for the identification of nonribosomal peptide biosynthetic enzymes using a synthetic probe for adenylation domains. Methods Mol. Biol. 1401, 63-76, 2016.
134) 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.
133) Cornelio, K., Espiritu, R. A., Todokoro, Y., Hanashima, 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.
132) 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.
131) Kanoh, N., Itoh, S., Fujita, K., Sakanishi, K., Sugiyama, R., Iwabuchi, Y., Nishimura, S., Kakeya, H. Asymmetric total synthesis of heronamide C and its non-enzymatic access to heronamides A and B: stereochemical confirmation and impact of long-range stereochemical communication on the biological activity. Chem. Eur. J. 22, 8586-8595, 2016.
130) Kakeya, H. Natural products-prompted chemical biology: Phenotypic screening and a new platform for target identification. Nat. Prod. Rep. 33, 648-654, 2016.

2015

129) 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]
128) 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.
127) 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.
126) 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 compounds as novel HIF-1 inhibitors. Bioorg. Med. Chem. 23, 1776-1787, 2015.
125) 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]
124) 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.
123) Ishikawa, F. Miyamoto, K., Konno, S., Kasai, S., Kakeya, H. Accurate detection of adenylation domain functions 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]
122) Kishimoro, S., Nishimura, S., Kakeya, H. Total synthesis and structure revision of mirubactin, and its iron binding activity. Chem. Lett. 44, 1303-1305, 2015.
121) 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.
120) 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.
119) Ishikawa, F., Suzuki, T., Dohmae, N., Kakeya, H. A multiplex labeling strategy for nonribosimal peptide synthetases using active site-directed proteomic probes for adenylation domins. ChemBioChem, 16, 2590-2594, 2015.
118) 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"]
117) Ishikawa, F., Konno, S., Suzuki, T., Dohmae, N., Kakeya, H. Profiling of nonribosomal peptide synthetase activitites using chemical proteomic probes for adenylation domains. ACS Chem. Biol. 10, 1989-1997, 2015.
116) Ishikawa, F., Kakeya, H. Recent advances in adenylation domain enzymology in nonribosomal peptide biosynthesis. Curr. Org. Chem. 19, 1204-1221, 2015.
115) 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.
114) 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.
113) 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.

2014

112) 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.
111) 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]
110) Fujita, K., Ishikawa, F., Kakeya, H. Biosynthetic origins of the epoxyquinone skeleton in epoxyquinols A and B. J. Nat. Prod. 77, 2707-2710, 2014.
109) 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.
108) 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]
107) 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.
106) 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.
105) 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.
104) 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

103) 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]
102) 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.
101) 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.
100) 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.
99) 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.
98) Sugiyama, R., Nishimura, S., Kakeya, H. Stereochemical reassignment of heronamide A, a polyketide macrolactam from Streptomyces sp. Tetrahedron Lett. 54, 1531-1533, 2013.
97) 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.
96) 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.

2012

95) 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.
94) 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.
93) 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).

2011

92) Takashima, K., Saitoh, A., Hirose, S., Nakai, W., Kondo, Y., Kakeya, H., Shin, H.-W., Nakayama, K.. GBF-Arf-COPI-ArfGAP-mediated Goldi-to-ER transport involved in regulation of lipid homeostasis. Cell Struct. Funct., 36, 223-235, 2011.
91) Ohno, Y., Hattori, A., Ueda, M., Kageyama, S., Yoshiki, T., Kakeya, H. Multiple NF-Y-binding CCAAT boxes are essential for transcrptional regulation of the human C7orf24 gene, a novel tumor-associated gene. FEBS J. 278, 4088-4099, 2011
90) 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.
89) 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.

2010

88) Lindqvist, L., Robert, F., Merrick, W., Kakeya, H., Fraser, C., Osada, H., Pelletier, J. Inhibition of translation by cytotreinin A - a member of the ansamycin family. RNA, 16, 2404-2413, 2010.
87) S. Nishimura, Y. Arita, M. Honda, K. Iwamoto, A. Matsuyama, A. Shirai, H. Kawasaki, H. Kakeya, T. Kobayashi, S. Matsunaga, M. Yoshida. Marine antifungal theonellamides target 3beta-hydroxysterol to activate Rho1 signaling. Nat. Chem. Biol. 6, 519-526, 2010. [Press release]
86) H. Kakeya, S. Nishimura. Novel natural products open the door of chemical biology and medicinal chemistry. J. Synth. Org. Chem. Jpn. 68, 490-500, 2010.

2009

85) 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.
84) Y. Hayashi, K. Sankar, H. Ishikawa, Y. Nozawa, M. 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

83) 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.]
82) 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.
81) 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.
80) 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).
79) 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).
78) 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).

-2007

77) 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.
76) K. Kikuchi, H. Kakeya. A bridge between chemistry and biology. Nature Chem. Biol. 2, 392-394, 2006.
75) 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.
74) 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.
73) 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.
72) 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.
71) 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.
70) 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.
69) 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.
68) 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.
67) 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.
66) 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.
65) 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.
64) 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.
63) 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.
62) 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.
61) 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.
60) 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.
59) 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.
58) 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
57) 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.
56) 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.
55) 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.
54) 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.
53) 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.
52) 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.
51) 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.
50) 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.
49) 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.
48) 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.
47) 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.
46) 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.
45) 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.
44) 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.
43) 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.
42) 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.
41) 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.
40) 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.
39) 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.
38) 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.
37) 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.
36) 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.
35) 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.
34) M. Watabe, H. Kakeya, and H. Osada. Requirement of protein kinase (Krs/Mst) ctivation for MT-21-induced apoptosis. Oncogene, 18, 5211~5220, 1999.
33) H. Kakeya and H. Osada. Induction of neurite outgrowth by epolactaene derivatives, 3-substituted 3-pyrrolin-2-ones. RIKEN Review, 18, 35-36, 1998.
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.