Referenced in: none

Automatically associated channels: Kv11.1

Title: Melanin concentrating hormone receptor 1 (MCHR1) antagonists-Still a viable approach for obesity treatment?

Authors: Thomas Högberg, Thomas M Frimurer, Pradip K Sasmal

Journal, date & volume: Bioorg. Med. Chem. Lett., 2012 Oct 1 , 22, 6039-47

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/22954736

Abstract
Obesity is a global epidemic associated with multiple severe diseases. Several pharmacotherapies have been investigated including the melanin concentrating hormone (MCH) and its receptor 1. The development of MCHR1 antagonists are described with a specific perspective on different chemotypes investigated in efforts to overcome hERG liabilities while having orally active, potent and selective compounds with sufficient brain penetration. A chemometric comparison of ∼2000 diverse MCHR1 and ∼1000 diverse hERG ligands underline the structural similarities. A binding pocket analysis of a MCHR1 model and recent X-ray structures of GPCRs invoked in selectivity issues indicate a way to support future drug design.