Výsledky vyhledávání - "Takaharu Hirayama"

Prolyl-tRNA synthetase inhibition promotes cell death in SK-MEL-2 cells through GCN2-ATF4 pathway activation

Autor: Takahito Hara, Satoshi Kitazawa, Misa Iwatani, Hitoshi Miyashita, Ryutaro Adachi, Yukiko Yamamoto, Megumi Morimoto, Takeo Arita, Sou Sakamoto, Takaharu Hirayama, Kazumasa Miyamoto

Publikováno v: Biochemical and Biophysical Research Communications. 488:648-654

Protein translation is highly activated in cancer tissues through oncogenic mutations and amplifications, and this can support survival and aberrant proliferation. Therefore, blocking translation could be a promising way to block cancer progression.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fda348abfaf1262d6c6f1c6c91988b09
https://doi.org/10.1016/j.bbrc.2017.01.045

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Design and synthesis of fused bicyclic inhibitors targeting the L5 loop site of centromere-associated protein E

Autor: Masanori Okaniwa, Hiroyuki Kakei, Tomoyasu Ishikawa, Tomohiro Kawamoto, Takaharu Hirayama, Akihiro Yokota, Maki Miyamoto, Momoko Ohori, Kenichi Iwai, Hiroshi Banno, Akihiro Ohashi, Tadahiro Nambu

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 26:4296-4300

Centromere-associated protein-E (CENP-E) is a mitotic kinesin which plays roles in cell division, and is regarded as a promising therapeutic target for the next generation of anti-mitotic agents. We designed novel fused bicyclic CENP-E inhibitors sta

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::87ff2e7ae2e49f60e3c025a32118bf5e
https://doi.org/10.1016/j.bmcl.2016.07.038

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Design and synthesis of selective CDK8/19 dual inhibitors: Discovery of 4,5-dihydrothieno[3',4':3,4]benzo[1,2-d]isothiazole derivatives

Autor: Koji Ono, Yukiko Hikichi, Masanori Okaniwa, Douglas R. Cary, Maki Hasegawa, Kazunobu Aoyama, Hiroshi Banno, Saomi Murai, Kazuko Yonemori, Yuka Hasegawa, Akito Hata, Takaharu Hirayama, Naoki Iwamura

Publikováno v: Bioorganicmedicinal chemistry. 25(8)

To develop a novel series of CDK8/19 dual inhibitors, we employed structure-based drug design using docking models based on a library compound, 4,5-dihydroimidazolo[3',4':3,4]benzo[1,2-d]isothiazole 16 bound to CDK8. We designed various [5,6,5]-fused

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9aeaf3b9361ec8d63e87cc7de2289f43
https://pubmed.ncbi.nlm.nih.gov/28302507

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Studies of CDK 8/19 inhibitors: Discovery of novel and selective CDK8/19 dual inhibitors and elimination of their CYP3A4 time-dependent inhibition potential

Autor: Douglas R. Cary, Kazunobu Aoyama, Yuka Hasegawa, Yasuhiro Hirata, Jun Fujimoto, Kazuko Yonemori, Takaharu Hirayama, Akito Hata, Yukiko Hikichi, Maki Hasegawa, Saomi Murai

Publikováno v: Bioorganicmedicinal chemistry. 25(12)

In this article, synthetic studies around a pyridylacrylamide-based hit compound (1), utilizing structure-based drug design guided by CDK8 docking models, is discussed. Modification of the pendant 4-fluorophenyl group to various heteroaromatic rings

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e57d1410cb2fe9786098a1e595ebabe6
https://pubmed.ncbi.nlm.nih.gov/28392276

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Discovery of N -[5-({2-[(cyclopropylcarbonyl)amino]imidazo[1,2- b ]pyridazin-6-yl}oxy)-2-methylphenyl]-1,3-dimethyl-1 H -pyrazole-5-carboxamide (TAK-593), a highly potent VEGFR2 kinase inhibitor

Autor: Akira Hori, Yoshiko Awazu, Terufumi Takagi, Yuya Oguro, Nozomu Sakai, Takaharu Hirayama, Kengo Okada, Naoki Miyamoto, Hideyuki Oki, Hiroshi Miki, Shinichi Imamura, Hidehisa Iwata, Toshiyuki Takeuchi, Seiji Yamasaki, Kazuhiro Miwa

Publikováno v: Bioorganic & Medicinal Chemistry. 21:2333-2345

Vascular endothelial growth factor (VEGF) plays important roles in tumor angiogenesis, and the inhibition of its signaling pathway is considered an effective therapeutic option for the treatment of cancer. In this study, we describe the design, synth

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::db8a3cc876ef7cb28cf6dbe5c21fb1c5
https://doi.org/10.1016/j.bmc.2013.01.074

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Nucleophilic Cyclopropanation Reaction with Bis(iodozincio)methane by 1,4-Addition to α,β-Unsaturated Carbonyl Compounds

Autor: Takaharu Hirayama, Kenichi Nomura, Seijiro Matsubara

Publikováno v: Chemistry - An Asian Journal. 4:1298-1303

Treatment of alpha,beta-unsaturated ketones with an electrophilic site at the gamma-position in the presence of trimethylsilyl cyanide with bis(iodozincio)methane afforded the (Z)-silyl enol ether of the beta-cyclopropyl substituted ketone in good yi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dcf2e73c90cd9b5d0950783bf7c048d5
https://doi.org/10.1002/asia.200900123

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Synthetic Studies on Centromere-Associated Protein-E (CENP-E) Inhibitors: 2. Application of Electrostatic Potential Map (EPM) and Structure-Based Modeling to Imidazo[1,2-a]pyridine Derivatives as Anti-Tumor Agents

Autor: Akihiro Ohashi, Kouji Mori, Hiroshi Banno, Takaharu Hirayama, Gotou Mika, Hiroyuki Kakei, Tomoyasu Ishikawa, Tomohiro Kawamoto, Momoko Ohori, Kenichi Iwai, Akihiro Yokota, Masanori Okaniwa

Publikováno v: Journal of medicinal chemistry. 58(20)

To develop centromere-associated protein-E (CENP-E) inhibitors for use as anticancer therapeutics, we designed novel imidazo[1,2-a]pyridines, utilizing previously discovered 5-bromo derivative 1a. By site-directed mutagenesis analysis, we confirmed t

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7fe3d14cadb66e130d9852b9e4ca33a2
https://pubmed.ncbi.nlm.nih.gov/26372373

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Aneuploidy generates proteotoxic stress and DNA damage concurrently with p53-mediated post-mitotic apoptosis in SAC-impaired cells

Autor: Hiroshi Banno, Tomohiro Kawamoto, Daisuke Morishita, Takaharu Hirayama, Kenichi Iwai, Kentaro Iwata, Momoko Ohori, Tomoyasu Ishikawa, Akihiro Ohashi, Yusuke Nakayama, Tadahiro Nambu, Maki Miyamoto, Masanori Okaniwa, Hitoshi Kandori

Publikováno v: Nature Communications

The molecular mechanism responsible that determines cell fate after mitotic slippage is unclear. Here we investigate the post-mitotic effects of different mitotic aberrations—misaligned chromosomes produced by CENP-E inhibition and monopolar spindl

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b84a67845af668a6d5c61b8a8f4d67d1
https://pubmed.ncbi.nlm.nih.gov/26144554

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Structure-based design, synthesis, and evaluation of imidazo[1,2-b]pyridazine and imidazo[1,2-a]pyridine derivatives as novel dual c-Met and VEGFR2 kinase inhibitors

Autor: Takaharu Hirayama, Hideyuki Oki, Naoki Miyamoto, Shinichi Imamura, Michiko Tawada, Kazuhide Nakamura, Hidehisa Iwata, Akira Hori, Hiroshi Miki, Seiji Yamasaki, Shigemitsu Matsumoto, Kengo Okada

Publikováno v: Bioorganicmedicinal chemistry. 21(24)

To identify compounds with potent antitumor efficacy for various human cancers, we aimed to synthesize compounds that could inhibit c-mesenchymal epithelial transition factor (c-Met) and vascular endothelial growth factor receptor 2 (VEGFR2) kinases.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::960db091ed505395e35737cff00078d3
https://pubmed.ncbi.nlm.nih.gov/24216091

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