Disruption of CRAF-Mediated MEK Activation Is Required for Effective MEK Inhibition in KRAS Mutant Tumors
Lito, Piro, Saborowski, Anna, Yue, Jingyin, Solomon, Martha, Joseph, Eric, Gadal, Sunyana, Saborowski, Michael, Kastenhuber, Edward, Fellmann, Christof, Ohara, Kazuhiro, Morikami, Kenji, Miura, Takaaki, Lukacs, Christine, Ishii, Nobuya, Lowe, Scott, Rosen, Neal
Published in Cancer cell (12.05.2014)
Published in Cancer cell (12.05.2014)
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Halogen Bonding at the Active Sites of Human Cathepsin L and MEK1 Kinase: Efficient Interactions in Different Environments
Hardegger, Leo A., Kuhn, Bernd, Spinnler, Beat, Anselm, Lilli, Ecabert, Robert, Stihle, Martine, Gsell, Bernard, Thoma, Ralf, Diez, Joachim, Benz, Jörg, Plancher, Jean-Marc, Hartmann, Guido, Isshiki, Yoshiaki, Morikami, Kenji, Shimma, Nobuo, Haap, Wolfgang, Banner, David W., Diederich, François
Published in ChemMedChem (04.11.2011)
Published in ChemMedChem (04.11.2011)
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Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799
Ohwada, Jun, Ebiike, Hirosato, Kawada, Hatsuo, Tsukazaki, Masao, Nakamura, Mitsuaki, Miyazaki, Takuya, Morikami, Kenji, Yoshinari, Kiyoshi, Yoshida, Miyuki, Kondoh, Osamu, Kuramoto, Shino, Ogawa, Kotaro, Aoki, Yuko, Shimma, Nobuo
Published in Bioorganic & medicinal chemistry letters (15.03.2011)
Published in Bioorganic & medicinal chemistry letters (15.03.2011)
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Development of a Method for Converting a TAK1 Type I Inhibitor into a Type II or c-Helix-Out Inhibitor by Structure-Based Drug Design (SBDD)
Muraoka, Terushige, Ide, Mitsuaki, Irie, Machiko, Morikami, Kenji, Miura, Takaaki, Nishihara, Masamichi, Kashiwagi, Hirotaka
Published in Chemical & pharmaceutical bulletin (2016)
Published in Chemical & pharmaceutical bulletin (2016)
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Monte Carlo Simulations on Atropisomerism of Thienotriazolodiazepines Applicable to Slow Transition Phenomena Using Potential Energy Surfaces by ab initio Molecular Orbital Calculations
Morikami, Kenji, Itezono, Yoshiko, Nishimoto, Masahiro, Ohta, Masateru
Published in Chemical & pharmaceutical bulletin (2014)
Published in Chemical & pharmaceutical bulletin (2014)
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Effects of fluorines on nonsecosteroidal vitamin D receptor agonists
Kashiwagi, Hirotaka, Ohta, Masateru, Ono, Yoshiyuki, Morikami, Kenji, Itoh, Susumu, Sato, Hideki, Takahashi, Tadakatsu
Published in Bioorganic & medicinal chemistry (01.02.2013)
Published in Bioorganic & medicinal chemistry (01.02.2013)
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Synthesis and biological activities of benzofuran antifungal agents targeting fungal N-myristoyltransferase
Masubuchi, Miyako, Ebiike, Hirosato, Kawasaki, Ken-ichi, Sogabe, Satoshi, Morikami, Kenji, Shiratori, Yasuhiko, Tsujii, Shinji, Fujii, Toshihiko, Sakata, Kiyoaki, Hayase, Michiko, Shindoh, Hidetoshi, Aoki, Yuko, Ohtsuka, Tatsuo, Shimma, Nobuo
Published in Bioorganic & medicinal chemistry (01.10.2003)
Published in Bioorganic & medicinal chemistry (01.10.2003)
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Optimizing the Physicochemical Properties of Raf/MEK Inhibitors by Nitrogen Scanning
Aoki, Toshihiro, Hyohdoh, Ikumi, Furuichi, Noriyuki, Ozawa, Sawako, Watanabe, Fumio, Matsushita, Masayuki, Sakaitani, Masahiro, Morikami, Kenji, Takanashi, Kenji, Harada, Naoki, Tomii, Yasushi, Shiraki, Koji, Furumoto, Kentaro, Tabo, Mitsuyasu, Yoshinari, Kiyoshi, Ori, Kazutomo, Aoki, Yuko, Shimma, Nobuo, Iikura, Hitoshi
Published in ACS medicinal chemistry letters (10.04.2014)
Published in ACS medicinal chemistry letters (10.04.2014)
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Design and synthesis of novel benzofurans as a new class of antifungal agents targeting fungal N-myristoyltransferase. Part 3
Kawasaki, Ken-ichi, Masubuchi, Miyako, Morikami, Kenji, Sogabe, Satoshi, Aoyama, Tsunehisa, Ebiike, Hirosato, Niizuma, Satoshi, Hayase, Michiko, Fujii, Toshihiko, Sakata, Kiyoaki, Shindoh, Hidetoshi, Shiratori, Yasuhiko, Aoki, Yuko, Ohtsuka, Tatsuo, Shimma, Nobuo
Published in Bioorganic & medicinal chemistry letters (06.01.2003)
Published in Bioorganic & medicinal chemistry letters (06.01.2003)
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Development of a Method for Converting a TAK1 Type I Inhibitor into a Type II or c-Helix-Out Inhibitor by Structure-Based Drug Design (SBDD)
Terushige Muraokaa, Mitsuaki Idea, Machiko Irieb, Kenji Morikamia, Takaaki Miurab, Masamichi Nishiharaa, Hirotaka Kashiwagia
Published in Chemical and Pharmaceutical Bulletin (01.11.2016)
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Published in Chemical and Pharmaceutical Bulletin (01.11.2016)
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The fibroblast growth factor receptor genetic status as a potential predictor of the sensitivity to CH5183284/Debio 1347, a novel selective FGFR inhibitor
Nakanishi, Yoshito, Akiyama, Nukinori, Tsukaguchi, Toshiyuki, Fujii, Toshihiko, Sakata, Kiyoaki, Sase, Hitoshi, Isobe, Takehito, Morikami, Kenji, Shindoh, Hidetoshi, Mio, Toshiyuki, Ebiike, Hirosato, Taka, Naoki, Aoki, Yuko, Ishii, Nobuya
Published in Molecular cancer therapeutics (01.11.2014)
Published in Molecular cancer therapeutics (01.11.2014)
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Discovery of [5-Amino-1-(2-methyl‑3H‑benzimidazol-5-yl)pyrazol-4-yl]-(1H‑indol-2-yl)methanone (CH5183284/Debio 1347), An Orally Available and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor
Ebiike, Hirosato, Taka, Naoki, Matsushita, Masayuki, Ohmori, Masayuki, Takami, Kyoko, Hyohdoh, Ikumi, Kohchi, Masami, Hayase, Tadakatsu, Nishii, Hiroki, Morikami, Kenji, Nakanishi, Yoshito, Akiyama, Nukinori, Shindoh, Hidetoshi, Ishii, Nobuya, Isobe, Takehito, Matsuoka, Hiroharu
Published in Journal of medicinal chemistry (08.12.2016)
Published in Journal of medicinal chemistry (08.12.2016)
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Discovery of a potent and highly selective transforming growth factor β receptor-associated kinase 1 (TAK1) inhibitor by structure based drug design (SBDD)
Muraoka, Terushige, Ide, Mitsuaki, Morikami, Kenji, Irie, Machiko, Nakamura, Mitsuaki, Miura, Takaaki, Kamikawa, Takayuki, Nishihara, Masamichi, Kashiwagi, Hirotaka
Published in Bioorganic & medicinal chemistry (15.09.2016)
Published in Bioorganic & medicinal chemistry (15.09.2016)
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Identification of a selective inhibitor of transforming growth factor β-activated kinase 1 by biosensor-based screening of focused libraries
Miura, Takaaki, Matsuo, Atsushi, Muraoka, Terushige, Ide, Mitsuaki, Morikami, Kenji, Kamikawa, Takayuki, Nishihara, Masamichi, Kashiwagi, Hirotaka
Published in Bioorganic & medicinal chemistry letters (15.02.2017)
Published in Bioorganic & medicinal chemistry letters (15.02.2017)
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Modification of a dihydropyrrolopyrimidine phosphoinositide 3-kinase (PI3K) inhibitor to improve oral bioavailability
Kawada, Hatsuo, Ebiike, Hirosato, Tsukazaki, Masao, Yamamoto, Shun, Koyama, Kohei, Nakamura, Mitsuaki, Morikami, Kenji, Yoshinari, Kiyoshi, Yoshida, Miyuki, Ogawa, Kotaro, Shinma, Nobuo, Tsukuda, Takuo, Ohwada, Jun
Published in Bioorganic & medicinal chemistry (15.12.2015)
Published in Bioorganic & medicinal chemistry (15.12.2015)
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Systematic SAR study of the side chain of nonsecosteroidal vitamin D3 analogs
Kashiwagi, Hirotaka, Ono, Yoshiyuki, Ohta, Masateru, Morikami, Kenji, Takahashi, Tadakatsu
Published in Bioorganic & medicinal chemistry (15.07.2012)
Published in Bioorganic & medicinal chemistry (15.07.2012)
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Discovery of novel tetracyclic compounds as anaplastic lymphoma kinase inhibitors
Kinoshita, Kazutomo, Ono, Yoshiyuki, Emura, Takashi, Asoh, Kohsuke, Furuichi, Noriyuki, Ito, Toshiya, Kawada, Hatsuo, Tanaka, Shota, Morikami, Kenji, Tsukaguchi, Toshiyuki, Sakamoto, Hiroshi, Tsukuda, Takuo, Oikawa, Nobuhiro
Published in Bioorganic & medicinal chemistry letters (15.06.2011)
Published in Bioorganic & medicinal chemistry letters (15.06.2011)
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Optimization of the phenylurea moiety in a phosphoinositide 3-kinase (PI3K) inhibitor to improve water solubility and the PK profile by introducing a solubilizing group and ortho substituents
Kawada, Hatsuo, Ebiike, Hirosato, Tsukazaki, Masao, Yamamoto, Shun, Koyama, Kohei, Nakamura, Mitsuaki, Morikami, Kenji, Yoshinari, Kiyoshi, Yoshida, Miyuki, Ogawa, Kotaro, Shimma, Nobuo, Tsukuda, Takuo, Ohwada, Jun
Published in Bioorganic & medicinal chemistry (01.07.2016)
Published in Bioorganic & medicinal chemistry (01.07.2016)
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Abstract 4758: Disruption of CRAF-mediated MEK activation is required for effective MEK inhibition in KRAS mutant tumors
Lito, Piro, Saborowski, Anna, Yue, Jingyin, Solomon, Martha, Joseph, Eric, Fellman, Christof, Ohara, Kazuhiro, Morikami, Kenji, Miura, Takaaki, Lucas, Christine, Ishii, Nobuya, Lowe, Scott, Rosen, Neal
Published in Cancer research (Chicago, Ill.) (01.10.2014)
Published in Cancer research (Chicago, Ill.) (01.10.2014)
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