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with NPBWR1 as keyword
Pelosini, C. Maffei, M. Ceccarini, G. Marchi, M. Marsili, A. Galli, G. Scartabelli, G. Tamberi, A. Latrofa, F. Fierabracci, P.
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Published in
Journal of Endocrinological Investigation
Background: GPR7, the endogenous coupled receptor for neuropeptide B and neuropeptide W, is expressed in several regions of the central nervous system, which are involved in the regulation of feeding behavior. GPR7 affects the regulation of energy balance through a mechanism independent of leptin and melanocortin pathways. Aim: Aim of this study wa...
Moningka, Remond Anthony Romero, F Hastings, Nicholas B Guo, Zhiqiang Wang, Ming Di Salvo, Jerry Li, Ying Trusca, Dorina Deng, Qiaoling Tong, Vincent
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Published in
Bioorganic & medicinal chemistry letters
Here, we report the discovery of a new class of NPBWR1 antagonists identified from a fragment-based screen. Compound 1 (cAMP IC50 = 250 µM; LE = 0.29) emerged as an initial hit. Further optimization of 1 by SAR-by-catalogue and chemical modification produced 21a (cAMP IC50 = 30 nM; LE = 0.39) with a 6,700-fold increase in potency from fragment 1. S...
