Zobrazeno 1 - 10
of 23
pro vyhledávání: '"Yasutaka Nagisa"'
Autor:
Shoki Okuda, Yasuyoshi Arikawa, Tomohiro Okawa, Junichi Sakamoto, Nobuyuki Amano, Shinobu Sasaki, Masanori Nakakariya, Yugo Habata, Shizuo Kasai, Natsu Hotta, Kenichi Hamagami, Masaaki Funata, Yasutaka Nagisa, Minoru Maruyama, Toshimi Nagi, Yasunori Nio
Publikováno v:
Endocrinology. 158:1298-1313
Bombesin receptor subtype 3 (BRS-3) is an orphan G protein-coupled receptor. Based on the obese phenotype of male BRS-3-deficient mice, BRS-3 has been considered an attractive target for obesity treatment. Here, we developed a selective BRS-3 agonist
Autor:
Uttam Khamrai, Jumpei Aida, Mrinalkanti Kundu, Tsuneo Yasuma, Mikio Shirasaki, Shoki Okuda, Shizuo Kasai, Syunsuke Yamamoto, Asato Kina, Masashi Takahashi, Toshihiro Noguchi, Yasutaka Nagisa, Yayoi Kawata, Hideyuki Igawa, Minoru Ikoma, Yasushi Fujioka, Keiko Kakegawa, Tsuyoshi Maekawa, Masaharu Nakayama
Publikováno v:
Bioorganic & Medicinal Chemistry. 24:2486-2503
Melanin-concentrating hormone (MCH) is an attractive target for antiobesity agents, and numerous drug discovery programs are dedicated to finding small-molecule MCH receptor 1 (MCHR1) antagonists. We recently reported novel pyridine-2(1 H )-ones as a
Autor:
Shoki Okuda, Minoru Ikoma, Masashi Takahashi, Shizuo Kasai, Yasutaka Nagisa, Hiromi Kaku, Syunsuke Yamamoto, Tsuyoshi Maekawa, Toshihiro Noguchi, Asato Kina, Keiko Kakegawa, Natsu Hotta, Yayoi Kawata, Hideyuki Igawa, Jumpei Aida, Masaharu Nakayama
Publikováno v:
Bioorganic & Medicinal Chemistry. 24:2504-2518
To develop non-basic melanin-concentrating hormone receptor 1 (MCHR1) antagonists with a high probability of target selectivity and therapeutic window, we explored neutral bicyclic motifs that could replace the previously reported imidazo[1,2-a]pyrid
Autor:
Mayumi Nishida, Natsu Hotta, Kenichi Hamagami, Masaaki Mori, Nobuyuki Amano, Masaaki Funata, Tomohiro Okawa, Shinobu Sasaki, Yasunori Nio, Junichi Sakamoto, Yasutaka Nagisa, Masanori Nakakariya, Yasuyoshi Arikawa, Minoru Maruyama, Toshimi Nagi, Shizuo Kasai, Yugo Habata
Publikováno v:
Brain and Behavior
Objectives Bombesin receptor subtype‐3 (BRS‐3) has been suggested to play a potential role in energy homeostasis. However, the physiological mechanism of BRS‐3 on energy homeostasis remains unknown. Thus, we investigated the BRS‐3‐mediated
Publikováno v:
Proceedings for Annual Meeting of The Japanese Pharmacological Society. 92:1-YIA
Autor:
Lenke Tari, Hideyuki Igawa, Akihiro Takano, Miklós Tóth, Jenny Häggkvist, Christer Halldin, Shoki Okuda, Shizuo Kasai, Vladimir Stepanov, Syunsuke Yamamoto, Yasutaka Nagisa, Marie Svedberg
Publikováno v:
Current radiopharmaceuticals. 10(1)
Background and Objective: Melanin-concentrating hormone (MCH) is an attractive target for antiobesity agents and many drug discovery programs have been dedicated to identify smallmolecule antagonists of melanin-concentrating hormone receptor 1 (MCHR1
Autor:
Hideyuki Igawa, Masashi Takahashi, Minoru Ikoma, Shiro Takekawa, Ayumi Ando, Shizuo Kasai, Natsu Hotta, Masaharu Nakayama, Mayumi Nishida, Shoki Okuda, Yoshinori Satomi, Yasutaka Nagisa, Syunsuke Yamamoto, Yayoi Kawata
Publikováno v:
European journal of pharmacology. 796
Melanin-concentrating hormone (MCH), a cyclic neuropeptide expressed predominantly in the lateral hypothalamus, plays an important role in the control of feeding behavior and energy homeostasis. Mice lacking MCH or MCH1 receptor are resistant to diet
Autor:
Uttam Khamrai, Shizuo Kasai, Minoru Ikoma, Asato Kina, Masaharu Nakayama, Jumpei Aida, Keiko Kakegawa, Yasutaka Nagisa, Masashi Takahashi, Syunsuke Yamamoto, Hideki Hirabayashi, Tsuneo Yasuma, Hideyuki Igawa, Mrinalkanti Kundu, Yayoi Kawata, Tsuyoshi Maekawa, Shuntaro Ashina
Publikováno v:
Journal of medicinal chemistry. 59(3)
Aiming to discover melanin-concentrating hormone receptor 1 (MCHR1) antagonists with improved safety profiles, we hypothesized that the aliphatic amine employed in most antagonists reported to date could be removed if the bicyclic motif of the compou
Autor:
Yuji Ishihara, Ryoma Hara, Kaneyoshi Kato, Asano Asami, Toshiro Yamashita, Shigekazu Sasaki, Shiro Takekawa, Hitomi Ogino, Nobuhiro Suzuki, Shuntaro Ashina, Yoshihide Nakano, Masahiro Kamaura, Tomoko Kaisho, Shizuo Kasai, Toshio Tanaka, Koki Kato, Shinichi Masada, Toshihiro Imaeda, Yasutaka Nagisa, Makoto Kamata
Publikováno v:
Journal of Medicinal Chemistry. 55:2353-2366
It was found that 3-(aminomethyl)quinoline derivatives showed high binding affinities for melanin-concentrating hormone receptor 1 (MCHR1) with reduced affinity for serotonin receptor 2c (5-HT2c) when the dihydronaphthalene nucleus of compound 1 (hum
Autor:
Toshio Tanaka, Satoshi Endo, Nobuhiro Suzuki, Jun Terauchi, Yoshihide Nakano, Maki Miyamoto, Kaoru Watanabe, Makoto Kamata, Hitomi Ogino, Shiro Takekawa, Asano Asami, Toshiro Yamashita, Michiko Tawada, Koki Kato, Yasutaka Nagisa, Kaneyoshi Kato, Yuji Ishihara, Toshihiro Imaeda, Taiichi Ora
Publikováno v:
Bioorganic & Medicinal Chemistry. 19:5539-5552
Human melanin-concentrating hormone receptor 1 (hMCHR1) antagonists are promising targets for obesity treatment. We identified the tetrahydronaphthalene derivative 1a with modest binding affinity for hMCHR1 by screening an in-house G protein-coupled