A structural chemogenomics analysis of aminergic GPCRs: lessons for histamine receptor ligand design.

ABSTRACT:

Background and purpose

Chemogenomics focuses on the discovery of new connections between chemical and biological space leading to the discovery of new protein targets and biologically active molecules. G-protein coupled receptors (GPCRs) are a particularly interesting protein family for chemogenomics studies because there is an overwhelming amount of ligand binding affinity data available. The increasing number of aminergic GPCR crystal structures now for the first time allows the integration of chemogenomics studies with high-resolution structural analyses of GPCR-ligand complexes.

Experimental approach

In this study, we have combined ligand affinity data, receptor mutagenesis studies, and amino acid sequence analyses to high-resolution structural analyses of (hist)aminergi

SUBMITTER: Kooistra AJ 

PROVIDER: S-EPMC3764853 | biostudies-literature | 2013 Sep

REPOSITORIES: biostudies-literature