Search Results - "Funabashi, Kaoru"

TAS2940, a novel brain‐penetrable pan‐ERBB inhibitor, for tumors with HER2 and EGFR aberrations by Oguchi, Kei, Araki, Hikari, Tsuji, Shingo, Nakamura, Masayuki, Miura, Akihiro, Funabashi, Kaoru, Osada, Akiko, Tanaka, Sakiho, Suzuki, Takamasa, Kobayashi, Susumu S., Mizuarai, Shinji

“…Genetic alterations in human epidermal growth factor receptor type 2 (HER2)/epidermal growth factor receptor (EGFR) are commonly associated with breast and…”
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Discovery of Futibatinib: The First Covalent FGFR Kinase Inhibitor in Clinical Use by Ito, Satoru, Otsuki, Sachie, Ohsawa, Hirokazu, Hirano, Atsushi, Kazuno, Hideki, Yamashita, Satoshi, Egami, Kosuke, Shibata, Yoshihiro, Yamamiya, Ikuo, Yamashita, Fumiaki, Kodama, Yasuo, Funabashi, Kaoru, Kazuno, Hiromi, Komori, Toshiharu, Suzuki, Satoshi, Sootome, Hiroshi, Hirai, Hiroshi, Sagara, Takeshi

“…Deregulating fibroblast growth factor receptor (FGFR) signaling is a promising strategy for cancer therapy. Herein, we report the discovery of compound 5…”
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Structural Basis of Human p70 Ribosomal S6 Kinase-1 Regulation by Activation Loop Phosphorylation by Sunami, Tomoko, Byrne, Noel, Diehl, Ronald E., Funabashi, Kaoru, Hall, Dawn L., Ikuta, Mari, Patel, Sangita B., Shipman, Jennifer M., Smith, Robert F., Takahashi, Ikuko, Zugay-Murphy, Joan, Iwasawa, Yoshikazu, Lumb, Kevin J., Munshi, Sanjeev K., Sharma, Sujata

“…p70 ribosomal S6 kinase (p70S6K) is a downstream effector of the mTOR signaling pathway involved in cell proliferation, cell growth, cell-cycle progression,…”
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Futibatinib Is a Novel Irreversible FGFR 1-4 Inhibitor That Shows Selective Antitumor Activity against FGFR-Deregulated Tumors by Sootome, Hiroshi, Fujita, Hidenori, Ito, Kenjiro, Ochiiwa, Hiroaki, Fujioka, Yayoi, Ito, Kimihiro, Miura, Akihiro, Sagara, Takeshi, Ito, Satoru, Ohsawa, Hirokazu, Otsuki, Sachie, Funabashi, Kaoru, Yashiro, Masakazu, Matsuo, Kenichi, Yonekura, Kazuhiko, Hirai, Hiroshi

“…FGFR signaling is deregulated in many human cancers, and FGFR is considered a valid target in FGFR-deregulated tumors. Here, we examine the preclinical profile…”
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Discovery of 3-Ethyl-4-(3-isopropyl-4-(4-(1-methyl-1 H-pyrazol-4-yl)-1 H-imidazol-1-yl)-1 H-pyrazolo[3,4- b]pyridin-1-yl)benzamide (TAS-116) as a Potent, Selective, and Orally Available HSP90 Inhibitor by Uno, Takao, Kawai, Yuichi, Yamashita, Satoshi, Oshiumi, Hiromi, Yoshimura, Chihoko, Mizutani, Takashi, Suzuki, Tatsuya, Chong, Khoon Tee, Shigeno, Kazuhiko, Ohkubo, Mitsuru, Kodama, Yasuo, Muraoka, Hiromi, Funabashi, Kaoru, Takahashi, Koichi, Ohkubo, Shuichi, Kitade, Makoto

“…The molecular chaperone heat shock protein 90 (HSP90) is a promising target for cancer therapy, as it assists in the stabilization of cancer-related proteins,…”
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TAS6417/CLN-081 Is a Pan-Mutation-Selective EGFR Tyrosine Kinase Inhibitor with a Broad Spectrum of Preclinical Activity against Clinically Relevant EGFR Mutations by Udagawa, Hibiki, Hasako, Shinichi, Ohashi, Akihiro, Fujioka, Rumi, Hakozaki, Yumi, Shibuya, Mikiko, Abe, Naomi, Komori, Toshiharu, Haruma, Tomonori, Terasaka, Miki, Fujita, Ryoto, Hashimoto, Akihiro, Funabashi, Kaoru, Yasuda, Hiroyuki, Miyadera, Kazutaka, Goto, Koichi, Costa, Daniel B, Kobayashi, Susumu S

“…Despite the worldwide approval of three generations of EGFR tyrosine kinase inhibitors (TKI) for advanced non-small cell lung cancers with mutations, no TKI…”
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TAS0728, A Covalent-binding, HER2-selective Kinase Inhibitor Shows Potent Antitumor Activity in Preclinical Models by Irie, Hiroki, Ito, Kimihiro, Fujioka, Yayoi, Oguchi, Kei, Fujioka, Akio, Hashimoto, Akihiro, Ohsawa, Hirokazu, Tanaka, Kenji, Funabashi, Kaoru, Araki, Hikari, Kawai, Yuichi, Shimamura, Tadashi, Wadhwa, Renu, Ohkubo, Shuichi, Matsuo, Kenichi

“…Activated HER2 is a promising therapeutic target for various cancers. Although several reports have described HER2 inhibitors in development, no…”
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Abstract 4008: TAS2940, a novel brain-penetrable pan-ERBB inhibitor, exhibits tumor regression and prolongs survival in intracranial models bearing ERBB aberrations by Oguchi, Kei, Araki, Hikari, Tsuji, Shingo, Nakamura, Masayuki, Miura, Akihiro, Funabashi, Kaoru, Osada, Akiko, Tanaka, Sakiho, Suzuki, Takamasa, Mizuarai, Shinji

“…Abstract Background: Primary and metastatic brain tumors have significant unmet medical needs as few drugs can penetrate the blood-brain barrier (BBB). Brain…”
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Abstract 1329: Preclinical evaluation of TAS6417 as a highly effective, pan-mutation-selective EGFR tyrosine kinase inhibitor by Udagawa, Hibiki, Hasako, Shinichi, Ohashi, Akihiro, Abe, Naomi, Haruma, Tomonori, Komori, Toshiharu, Terasaka, Miki, Fujita, Ryoto, Funabashi, Kaoru, Yasuda, Hiroyuki, Miyadera, Kazutaka, Goto, Koichi, Costa, Daniel B., Kobayashi, Susumu S.

“…Abstract Objectives: Three generations of epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) have developed to treat advanced non-small…”
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Abstract 4784: TAS0286/HM05, a novel highly selective RET inhibitor, prominently inhibits various RET defective tumor growth by Fujita, Hidenori, Miyazaki, Isao, Kato, Masanori, Yamada, Yukari, Ishida, Keiji, Haruma, Tomonori, Nagasaki, Haruka, Ito, Kenjiro, Hashimoto, Akihiro, Kodama, Yasuo, Funabashi, Kaoru, Lovati, Emanuela, Miyadera, Kazutaka, Matsuo, Kenichi, Iwasawa, Yoshikazu

“…Abstract The rearranged during transfection (RET) gene is a well-known proto-oncogene and encodes a single-pass transmembrane receptor tyrosine kinase. RET…”
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Vepafestinib is a pharmacologically advanced RET-selective inhibitor with high CNS penetration and inhibitory activity against RET solvent front mutations by Miyazaki, Isao, Odintsov, Igor, Ishida, Keiji, Lui, Allan J W, Kato, Masanori, Suzuki, Tatsuya, Zhang, Tom, Wakayama, Kentaro, Kurth, Renate I, Cheng, Ryan, Fujita, Hidenori, Delasos, Lukas, Vojnic, Morana, Khodos, Inna, Yamada, Yukari, Ishizawa, Kota, Mattar, Marissa S, Funabashi, Kaoru, Chang, Qing, Ohkubo, Shuichi, Yano, Wakako, Terada, Ryuichiro, Giuliano, Claudio, Lu, Yue Christine, Bonifacio, Annalisa, Kunte, Siddharth, Davare, Monika A, Cheng, Emily H, de Stanchina, Elisa, Lovati, Emanuela, Iwasawa, Yoshikazu, Ladanyi, Marc, Somwar, Romel

“…RET receptor tyrosine kinase is activated in various cancers (lung, thyroid, colon and pancreatic, among others) through oncogenic fusions or gain-of-function…”
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Author Correction: Vepafestinib is a pharmacologically advanced RET-selective inhibitor with high CNS penetration and inhibitory activity against RET solvent front mutations by Miyazaki, Isao, Odintsov, Igor, Ishida, Keiji, Lui, Allan J. W., Kato, Masanori, Suzuki, Tatsuya, Zhang, Tom, Wakayama, Kentaro, Kurth, Renate I., Cheng, Ryan, Fujita, Hidenori, Delasos, Lukas, Vojnic, Morana, Khodos, Inna, Yamada, Yukari, Ishizawa, Kota, Mattar, Marissa S., Funabashi, Kaoru, Chang, Qing, Ohkubo, Shuichi, Yano, Wakako, Terada, Ryuichiro, Giuliano, Claudio, Lu, Yue Christine, Bonifacio, Annalisa, Kunte, Siddharth, Davare, Monika A., Cheng, Emily H., de Stanchina, Elisa, Lovati, Emanuela, Iwasawa, Yoshikazu, Ladanyi, Marc, Somwar, Romel

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In vitro biological profile of a highly potent novel endothelin (ET) antagonist BQ-123 selective for the ETA receptor by Ihara, M, Ishikawa, K, Fukuroda, T, Saeki, T, Funabashi, K, Fukami, T, Suda, H, Yano, M

“…The novel endothelin (ET) receptor antagonists BE-18257A and BE-18257B were isolated from the fermentation products of Streptomyces misakiensis. The…”
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Discovery of 3‑Ethyl-4-(3-isopropyl-4-(4-(1-methyl‑1H‑pyrazol-4-yl)‑1H‑imidazol-1-yl)‑1H‑pyrazolo[3,4‑b]pyridin-1-yl)benzamide (TAS-116) as a Potent, Selective, and Orally Available HSP90 Inhibitor by Uno, Takao, Kawai, Yuichi, Yamashita, Satoshi, Oshiumi, Hiromi, Yoshimura, Chihoko, Mizutani, Takashi, Suzuki, Tatsuya, Chong, Khoon Tee, Shigeno, Kazuhiko, Ohkubo, Mitsuru, Kodama, Yasuo, Muraoka, Hiromi, Funabashi, Kaoru, Takahashi, Koichi, Ohkubo, Shuichi, Kitade, Makoto

“…The molecular chaperone heat shock protein 90 (HSP90) is a promising target for cancer therapy, as it assists in the stabilization of cancer-related proteins,…”
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Renin Inhibitors. II. Synthesis and Structure-Activity Relationships of N-Terminus Modified Inhibitors Containing a Homostatine Analogue by ATSUUMI, Shugo, NAKANO, Masato, KOIKE, Yutaka, TANAKA, Seiichi, FUNABASHI, Hiroshi, MATSUYAMA, Kenji, NAKANO, Makiko, SAWASAKI, Yoshio, FUNABASHI, Kaoru, MORISHIMA, Hajime

“…The synthesis and structure-activity relationships of N-terminus modified renin inhibitors containing the homostatine analogue, (2RS, 4S,…”
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