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6. Discovery and pharmacological effects of a novel GPR142 antagonist.

Author

Murakoshi, Michiko, Kuwabara, Harumi, Nagasaki, Miyuki, Xiong, Yu Mei, Reagan, Jeff D., Maeda, Hiroaki, and Nara, Futoshi

Abstract

GPR142 is a G-protein-coupled receptor (GPCR), whose most potent and efficacious ligand has been reported as being the natural amino acidl-tryptophan. GPR142 is highly expressed in pancreatic β-cells and immune cells, suggesting the receptor may play a role in the pathogenesis and development of diabetes or inflammatory diseases. In a previous report, we developed GPR142 agonists as insulin secretagogues. In this report, we show the discovery of a selective, potent small-molecule GPR142 antagonist, CLP-3094, and its pharmacological characteristics. These data support targeting this receptor for the treatment of chronic inflammatory diseases. [ABSTRACT FROM PUBLISHER]

Published
2017
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7. Potent and Orally Bioavailable GPR142 Agonists as Novel Insulin Secretagogues for the Treatment of Type 2 Diabetes

Author

Toda, Narihiro, primary, Hao, Xiaolin, additional, Ogawa, Yasuyuki, additional, Oda, Kozo, additional, Yu, Ming, additional, Fu, Zice, additional, Chen, Yi, additional, Kim, Yongjae, additional, Lizarzaburu, Mike, additional, Lively, Sarah, additional, Lawlis, Shauna, additional, Murakoshi, Michiko, additional, Nara, Futoshi, additional, Watanabe, Nobuaki, additional, Reagan, Jeff D., additional, Tian, Hui, additional, Fu, Angela, additional, Motani, Alykhan, additional, Liu, Qingxiang, additional, Lin, Yi-Jyun, additional, Zhuang, Run, additional, Xiong, Yumei, additional, Fan, Peter, additional, Medina, Julio, additional, Li, Leping, additional, Izumi, Masanori, additional, Okuyama, Ryo, additional, and Shibuya, Satoshi, additional

Published
2013
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8. Aminopyrazole–Phenylalanine Based GPR142 Agonists: Discovery of Tool Compound and in Vivo Efficacy Studies

Author

Yu, Ming, primary, Lizarzaburu, Mike, additional, Motani, Alykhan, additional, Fu, Zice, additional, Du, Xiaohui, additional, Liu, Jiwen (Jim), additional, Jiao, Xianyun, additional, Lai, SuJen, additional, Fan, Peter, additional, Fu, Angela, additional, Liu, Qingxiang, additional, Murakoshi, Michiko, additional, Nara, Futoshi, additional, Oda, Kozo, additional, Okuyama, Ryo, additional, Reagan, Jeff D., additional, Watanabe, Nobuaki, additional, Yamazaki, Mami, additional, Xiong, Yumei, additional, Zhang, Ying, additional, Zhuang, Run, additional, Lin, Daniel C.-H., additional, Houze, Jonathan B., additional, Medina, Julio C., additional, and Li, Leping, additional

Published
2013
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9. Corrigendum to “Phenylalanine derivatives as GPR142 agonists for the treatment of Type II diabetes” [Bioorg. Med. Chem. Lett. 22 (2012) 6218–6223]

Author

Du, Xiaohui, primary, Kim, Yong-Jae, additional, Lai, SuJen, additional, Chen, Xi, additional, Lizarzaburu, Mike, additional, Turcotte, Simon, additional, Fu, Zice, additional, Liu, Qingxiang, additional, Zhang, Ying, additional, Motani, Alykhan, additional, Oda, Kozo, additional, Okuyama, Ryo, additional, Nara, Futoshi, additional, Murakoshi, Michiko, additional, Fu, Angela, additional, Reagan, Jeff D., additional, Fan, Peter, additional, Xiong, Yumei, additional, Shen, Wang, additional, Li, Leping, additional, Houze, Jonathan, additional, and Medina, Julio C., additional

Published
2012
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