Search Results - "Ishikawa, Tomoyasu"

Structural Analysis of the Mechanism of Inhibition and Allosteric Activation of the Kinase Domain of HER2 Protein by Aertgeerts, Kathleen, Skene, Robert, Yano, Jason, Sang, Bi-Ching, Zou, Hua, Snell, Gyorgy, Jennings, Andy, Iwamoto, Keiji, Habuka, Noriyuki, Hirokawa, Aki, Ishikawa, Tomoyasu, Tanaka, Toshimasa, Miki, Hiroshi, Ohta, Yoshikazu, Sogabe, Satoshi

“…Aberrant signaling of ErbB family members human epidermal growth factor 2 (HER2) and epidermal growth factor receptor (EGFR) is implicated in many human…”
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Antitumor Activity of the Selective Pan-RAF Inhibitor TAK-632 in BRAF Inhibitor-Resistant Melanoma by NAKAMURA, Akito, ARITA, Takeo, TSUCHIYA, Shuntarou, DONELAN, Jill, CHOUITAR, Jouhara, CARIDEO, Elizabeth, GALVIN, Katherine, OKANIWA, Masanori, ISHIKAWA, Tomoyasu, YOSHIDA, Sei

“…The mitogen-activated protein kinase (MAPK) pathway is particularly important for the survival and proliferation of melanoma cells. Somatic mutations in BRAF…”
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Design and Synthesis of Novel Human Epidermal Growth Factor Receptor 2 (HER2)/Epidermal Growth Factor Receptor (EGFR) Dual Inhibitors Bearing a Pyrrolo[3,2-d]pyrimidine Scaffold by Ishikawa, Tomoyasu, Seto, Masaki, Banno, Hiroshi, Kawakita, Youichi, Oorui, Mami, Taniguchi, Takahiko, Ohta, Yoshikazu, Tamura, Toshiya, Nakayama, Akiko, Miki, Hiroshi, Kamiguchi, Hidenori, Tanaka, Toshimasa, Habuka, Noriyuki, Sogabe, Satoshi, Yano, Jason, Aertgeerts, Kathleen, Kamiyama, Keiji

“…Dual inhibitors of human epidermal growth factor receptor 2 (HER2) and epidermal growth factor receptor (EGFR) have been investigated for breast, lung,…”
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Structure-Based Approach for the Discovery of Pyrrolo[3,2‑d]pyrimidine-Based EGFR T790M/L858R Mutant Inhibitors by Sogabe, Satoshi, Kawakita, Youichi, Igaki, Shigeru, Iwata, Hidehisa, Miki, Hiroshi, Cary, Douglas R, Takagi, Terufumi, Takagi, Shinji, Ohta, Yoshikazu, Ishikawa, Tomoyasu

“…The epidermal growth factor receptor (EGFR) family plays a critical role in vital cellular processes and in various cancers. Known EGFR inhibitors exhibit…”
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Identification of a new class of potent Cdc7 inhibitors designed by putative pharmacophore model: Synthesis and biological evaluation of 2,3-dihydrothieno[3,2-d]pyrimidin-4(1H)-ones by Kurasawa, Osamu, Oguro, Yuya, Miyazaki, Tohru, Homma, Misaki, Mori, Kouji, Iwai, Kenichi, Hara, Hideto, Skene, Robert, Hoffman, Isaac, Ohashi, Akihiro, Yoshida, Sei, Ishikawa, Tomoyasu, Cho, Nobuo

“…[Display omitted] Cell division cycle 7 (Cdc7) is a serine/threonine kinase that plays important roles in the regulation of DNA replication process. A genetic…”
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Design and Synthesis of Potent Inhibitor of Apoptosis (IAP) Proteins Antagonists Bearing an Octahydropyrrolo[1,2‑a]pyrazine Scaffold as a Novel Proline Mimetic by Hashimoto, Kentaro, Saito, Bunnai, Miyamoto, Naoki, Oguro, Yuya, Tomita, Daisuke, Shiokawa, Zenyu, Asano, Moriteru, Kakei, Hiroyuki, Taya, Naohiro, Kawasaki, Masanori, Sumi, Hiroyuki, Yabuki, Masato, Iwai, Kenichi, Yoshida, Sei, Yoshimatsu, Mie, Aoyama, Kazunobu, Kosugi, Yohei, Kojima, Takashi, Morishita, Nao, Dougan, Douglas R, Snell, Gyorgy P, Imamura, Shinichi, Ishikawa, Tomoyasu

“…To develop novel inhibitor of apoptosis (IAP) proteins antagonists, we designed a bicyclic octahydropyrrolo[1,2-a]pyrazine scaffold as a novel proline…”
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Screening and Characterization of Hydrate Forms of T-3256336, a Novel Inhibitor of Apoptosis (IAP) Protein Antagonist by Takeuchi, Shoko, Kojima, Takashi, Hashimoto, Kentaro, Saito, Bunnai, Sumi, Hiroyuki, Ishikawa, Tomoyasu, Ikeda, Yukihiro

“…Different crystal packing of hydrates from anhydrate crystals leads to different physical properties, such as solubility and stability. Investigation of the…”
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Design, stereoselective synthesis, and biological evaluation of novel tri-cyclic compounds as inhibitor of apoptosis proteins (IAP) antagonists by Asano, Moriteru, Hashimoto, Kentaro, Saito, Bunnai, Shiokawa, Zenyu, Sumi, Hiroyuki, Yabuki, Masato, Yoshimatsu, Mie, Aoyama, Kazunobu, Hamada, Teruki, Morishita, Nao, Dougan, Douglas R., Mol, Clifford D., Yoshida, Sei, Ishikawa, Tomoyasu

“…We recently reported the discovery of octahydropyrrolo[1,2-a]pyrazine A as a lead compound for an inhibitor of apoptosis proteins (IAP) antagonist. To develop…”
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Stability and Stabilization Studies of TAK-599 (Ceftaroline Fosamil), a Novel N-Phosphono Type Prodrug of Anti-methicillin Resistant Staphylococcus aureus Cephalosporin T-91825 by Ikeda, Yukihiro, Ban, Junko, Ishikawa, Tomoyasu, Hashiguchi, Shohei, Urayama, Shinichi, Horibe, Hidetoshi

“…TAK-599 (known as ceftaroline fosamil) is a novel N-phosphono type prodrug of a cephalosporin compound, T-91825, that exhibits strong activity against…”
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In vitro antimicrobial activity of T-91825, a novel anti-MRSA cephalosporin, and in vivo anti-MRSA activity of its prodrug, TAK-599 by Iizawa, Yuji, Nagai, Junko, Ishikawa, Tomoyasu, Hashiguchi, Shohei, Nakao, Masafumi, Miyake, Akio, Okonogi, Kenji

“…TAK-599 is a water-soluble prodrug of a cephalosporin compound, T-91825. In vitro and in vivo antibacterial activities of T-91825 and TAK-599, respectively,…”
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(+)-Phorboxazole A Synthetic Studies. A Highly Convergent, Second Generation Total Synthesis of (+)-Phorboxazole A by Smith, Amos B, Razler, Thomas M, Ciavarri, Jeffrey P, Hirose, Tomoyasu, Ishikawa, Tomoyasu

“…A second generation total synthesis of the potent antitumor agent (+)-phorboxazole A (1) has been achieved. The cornerstone of this approach comprises a more…”
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Screening and Characterization of Hydrate Forms of T-3256336, a Novel Inhibitor of Apoptosis (IAP) Protein Antagonist by Shoko Takeuchia, Takashi Kojimaa, Kentaro Hashimotob, Bunnai Saitob, Hiroyuki Sumib, Tomoyasu Ishikawab, Yukihiro Ikedaa

“…Different crystal packing of hydrates from anhydrate crystals leads to different physical properties, such as solubility and stability. Investigation of the…”
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Aneuploidy generates proteotoxic stress and DNA damage concurrently with p53-mediated post-mitotic apoptosis in SAC-impaired cells by Ohashi, Akihiro, Ohori, Momoko, Iwai, Kenichi, Nakayama, Yusuke, Nambu, Tadahiro, Morishita, Daisuke, Kawamoto, Tomohiro, Miyamoto, Maki, Hirayama, Takaharu, Okaniwa, Masanori, Banno, Hiroshi, Ishikawa, Tomoyasu, Kandori, Hitoshi, Iwata, Kentaro

“…The molecular mechanism responsible that determines cell fate after mitotic slippage is unclear. Here we investigate the post-mitotic effects of different…”
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Discovery of Potent Mcl-1/Bcl-xL Dual Inhibitors by Using a Hybridization Strategy Based on Structural Analysis of Target Proteins by Tanaka, Yuta, Aikawa, Katsuji, Nishida, Goushi, Homma, Misaki, Sogabe, Satoshi, Igaki, Shigeru, Hayano, Yumi, Sameshima, Tomoya, Miyahisa, Ikuo, Kawamoto, Tomohiro, Tawada, Michiko, Imai, Yumi, Inazuka, Masakazu, Cho, Nobuo, Imaeda, Yasuhiro, Ishikawa, Tomoyasu

“…Mcl-1 and Bcl-xL are crucial regulators of apoptosis, therefore dual inhibitors of both proteins could serve as promising new anticancer drugs. To design…”
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Discovery of a Selective Kinase Inhibitor (TAK-632) Targeting Pan-RAF Inhibition: Design, Synthesis, and Biological Evaluation of C‑7-Substituted 1,3-Benzothiazole Derivatives by Okaniwa, Masanori, Hirose, Masaaki, Arita, Takeo, Yabuki, Masato, Nakamura, Akito, Takagi, Terufumi, Kawamoto, Tomohiro, Uchiyama, Noriko, Sumita, Akihiko, Tsutsumi, Shunichirou, Tottori, Tsuneaki, Inui, Yoshitaka, Sang, Bi-Ching, Yano, Jason, Aertgeerts, Kathleen, Yoshida, Sei, Ishikawa, Tomoyasu

“…With the aim of discovering a selective kinase inhibitor targeting pan-RAF kinase inhibition, we designed novel 1,3-benzothiazole derivatives based on our…”
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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 by Hirayama, Takaharu, Okaniwa, Masanori, Banno, Hiroshi, Kakei, Hiroyuki, Ohashi, Akihiro, Iwai, Kenichi, Ohori, Momoko, Mori, Kouji, Gotou, Mika, Kawamoto, Tomohiro, Yokota, Akihiro, Ishikawa, Tomoyasu

“…To develop centromere-associated protein-E (CENP-E) inhibitors for use as anticancer therapeutics, we designed novel imidazo­[1,2-a]­pyridines, utilizing…”
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Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors by Kawakita, Youichi, Seto, Masaki, Ohashi, Tomohiro, Tamura, Toshiya, Yusa, Tadashi, Miki, Hiroshi, Iwata, Hidehisa, Kamiguchi, Hidenori, Tanaka, Toshimasa, Sogabe, Satoshi, Ohta, Yoshikazu, Ishikawa, Tomoyasu

“…A novel 7,6 fused bicyclic scaffold, pyrimido[4,5-b]azepine was designed to fit into the ATP binding site of the HER2/EGFR proteins. The synthesis of this…”
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T-3256336, a novel and orally available small molecule IAP antagonist, induced tumor cell death via induction of systemic TNF alpha production by Sumi, Hiroyuki, Inazuka, Masakazu, Hashimoto, Kentaro, Ishikawa, Tomoyasu, Yoshida, Sei, Yabuki, Masato

“…Inhibitors of apoptosis proteins (IAPs) are a family of antiapoptotic regulators that have attracted attention as potential targets for cancer therapeutics…”
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Stability and Stabilization Studies of TAK-599 (Ceftaroline Fosamil), a Novel N-Phosphono Type Prodrug of Anti-methicillin Resistant Staphylococcus aureus Cephalosporin T-91825 by Yukihiro IKEDAa, Junko BANa, Tomoyasu ISHIKAWAa, Shohei HASHIGUCHIa, Shinichi URAYAMAb, Hidetoshi HORIBEa

“…TAK-599 (known as ceftaroline fosamil) is a novel N-phosphono type prodrug of a cephalosporin compound, T-91825, that exhibits strong activity against…”
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Design and Synthesis of Pyrrolo[3,2-d]pyrimidine Human Epidermal Growth Factor Receptor 2 (HER2)/Epidermal Growth Factor Receptor (EGFR) Dual Inhibitors: Exploration of Novel Back-Pocket Binders by Kawakita, Youichi, Banno, Hiroshi, Ohashi, Tomohiro, Tamura, Toshiya, Yusa, Tadashi, Nakayama, Akiko, Miki, Hiroshi, Iwata, Hidehisa, Kamiguchi, Hidenori, Tanaka, Toshimasa, Habuka, Noriyuki, Sogabe, Satoshi, Ohta, Yoshikazu, Ishikawa, Tomoyasu

“…To develop novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) kinase inhibitors, we explored…”
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