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A structural chemogenomics analysis of aminergic GPCRs : lessons for histamine receptor ligand design
Author(s) -
Kooistra A J,
Kuhne S,
Esch I J P,
Leurs R,
Graaf C
Publication year - 2013
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/bph.12248
Subject(s) - g protein coupled receptor , ligand (biochemistry) , pharmacophore , drug discovery , biology , receptor , structural similarity , binding site , computational biology , chemistry , biochemistry
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.