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Identification of piperazine-bisamide GHSR antagonists for the treatment of obesity |
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| Authors: | Ming Yu Mike Lizarzaburu Holger Beckmann Richard Connors Kang Dai Katrin Haller Cong Li Lingming Liang Michelle Lindstrom Ji Ma Alykhan Motani Malgorzata Wanska Alex Zhang Leping Li Julio C Medina |
| Institution: | 1. Amgen Inc. 1120 Veterans Boulevard, South San Francisco, CA 94080, USA;2. Syntacoll Gmbh, Donaustr. 24, 93342 Saal/Donau, Germany;3. Presidio Pharmaceuticals, Inc. 1700 Owens Street, Suite 585, San Francisco, CA 94158, USA |
| Abstract: | Piperazine-bisamide analogs were discovered as partial agonists of human growth hormone secretagogue receptor (GHSR) in a high throughput screen. The partial agonists were optimized for potency and converted into antagonists through structure–activity relationship (SAR) studies. The efforts also led to the identification of potent antagonist with favorable PK profile suitable as a tool compound for in vivo studies. |
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