73746-45-9Relevant articles and documents
Important Hydrogen Bond Networks in Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitor Design Revealed by Crystal Structures of Imidazoleisoindole Derivatives with IDO1
Peng, Yi-Hui,Ueng, Shau-Hua,Tseng, Chen-Tso,Hung, Ming-Shiu,Song, Jen-Shin,Wu, Jian-Sung,Liao, Fang-Yu,Fan, Yu-Shiou,Wu, Mine-Hsine,Hsiao, Wen-Chi,Hsueh, Ching-Cheng,Lin, Shu-Yu,Cheng, Chia-Yi,Tu, Chih-Hsiang,Lee, Lung-Chun,Cheng, Ming-Fu,Shia, Kak-Shan,Shih, Chuan,Wu, Su-Ying
, p. 282 - 293 (2016/01/29)
Indoleamine 2,3-dioxygenase 1 (IDO1), promoting immune escape of tumors, is a therapeutic target for the cancer immunotherapy. A number of IDO1 inhibitors have been identified, but only limited structural biology studies of IDO1 inhibitors are available t
Discovery of MK-5046, a potent, selective bombesin receptor subtype-3 agonist for the treatment of obesity
Sebhat, Iyassu K.,Franklin, Christopher,Lo, Michael M.-C.,Chen, David,Jewell, James P.,Miller, Randy,Pang, Jianmei,Palyha, Oksana,Kan, Yanqing,Kelly, Theresa M.,Guan, Xiao-Ming,Marsh, Donald J.,Kosinski, Jennifer A.,Metzger, Joseph M.,Lyons, Kathryn,Dragovic, Jasminka,Guzzo, Peter R.,Henderson, Alan J.,Reitman, Marc L.,Nargund, Ravi P.,Wyvratt, Matthew J.,Lin, Linus S.
supporting information; experimental part, p. 43 - 47 (2011/04/17)
We report the development and characterization of compound 22 (MK-5046), a potent, selective small molecule agonist of BRS-3 (bombesin receptor subtype-3). In pharmacological testing using diet-induced obese mice, compound 22 caused mechanism-based, dose-
Substituted inmidazoles as bombesin receptor subtype-3 modulators
-
Page/Page column 27-28, (2010/02/17)
Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.