Miltz, Wolfgang, Velcicky, Juraj, Dawson King, Janet, Littlewood-Evans, Amanda, Ludwig, Marie-Gabrielle, Seuwen, Klaus, Feifel, Roland, Oberhauser, Berndt, Meyer, Arndt, Gabriel, Daniela and Loetscher, Pius (2017) Design and synthesis of potent and orally active GPR4 antagonists with modulatory effects on nociception, inflammation, and angiogenesis. Bioorganic & Medicinal Chemistry, 25 (16). pp. 4512-4525. ISSN 0968-0896

Abstract

The G-protein-coupled receptor GPR4 functions as a proton sensor activated by extracellular acidic pH and has been implicated in playing a key role in acidosis associated with a variety of inflammatory conditions. A selective GPR4 antagonist 2 was developed, starting from a high throughput screening hit 1. The compound showed potent cellular activity and was efficacious in animal models of angiogenesis, inflammation, and pain.

Item Type:	Article
Keywords:	GPR4; Amino-pyrimidine derivatives; Imidazo-pyridine derivatives; Angiogenesis; Inflammation; Pain
Date Deposited:	09 Aug 2017 00:45
Last Modified:	09 Aug 2017 00:45
URI:	https://oak.novartis.com/id/eprint/31037