Pharmacogenomic and structural analysis of constitutive G protein–coupled receptor activity

MJ Smit, HF Vischer, RA Bakker… - Annu. Rev …, 2007 - annualreviews.org
G protein–coupled receptors (GPCRs) respond to a chemically diverse plethora of signal
transduction molecules. The notion that GPCRs also signal without an external chemical …

Pharmacogenetics of the G protein-coupled receptors

MD Thompson, DEC Cole, V Capra… - … in Drug Discovery and …, 2014 - Springer
Pharmacogenetics investigates the influence of genetic variants on physiological
phenotypes related to drug response and disease, while pharmacogenomics takes a …

[HTML][HTML] Impact of GPCRs in clinical medicine: monogenic diseases, genetic variants and drug targets

PA Insel, CM Tang, I Hahntow, MC Michel - Biochimica et Biophysica Acta …, 2007 - Elsevier
By virtue of their large number, widespread distribution and important roles in cell
physiology and biochemistry, G-protein-coupled receptors (GPCR) play multiple important …

Genetic variations in human G protein-coupled receptors: implications for drug therapy

W Sadee, E Hoeg, J Lucas, D Wang - AAPs PharmSci, 2001 - Springer
Numerous genes encode G protein-coupled receptors (GPCRs)-a main molecular target for
drug therapy. Estimates indicate that the human genome contains approximately 600 GPCR …

Genetic variations and polymorphisms of G protein-coupled receptors: functional and therapeutic implications

BK Rana, T Shiina, PA Insel - Annual review of pharmacology …, 2001 - annualreviews.org
G protein-coupled receptors (GPCRs) represent a major class of proteins in the genome of
many species, including humans. In addition to the mapping of a number of human …

Elucidating the interactome of G protein-coupled receptors and receptor activity-modifying proteins

IB Kotliar, E Lorenzen, JM Schwenk, DL Hay… - Pharmacological …, 2023 - ASPET
G protein-coupled receptors (GPCRs) are known to interact with several other classes of
integral membrane proteins that modulate their biology and pharmacology. However, the …

Constitutive activation of G protein-coupled receptors and diseases: insights into mechanisms of activation and therapeutics

YX Tao - Pharmacology & therapeutics, 2008 - Elsevier
The existence of constitutive activity for G protein-coupled receptors (GPCRs) was first
described in 1980s. In 1991, the first naturally occurring constitutively active mutations in …

Structure-function of the G protein–coupled receptor superfamily

V Katritch, V Cherezov… - Annual review of …, 2013 - annualreviews.org
During the past few years, crystallography of G protein–coupled receptors (GPCRs) has
experienced exponential growth, resulting in the determination of the structures of 16 distinct …

The use of constitutively active GPCRs in drug discovery and functional genomics

DT Chalmers, DP Behan - Nature reviews Drug discovery, 2002 - nature.com
The complete sequencing of the human genome has afforded researchers the opportunity to
identify novel G-protein-coupled receptors (GPCRs) that are expressed in human tissues …

GPCR signaling: understanding the pathway to successful drug discovery

C Williams, SJ Hill - G protein-coupled receptors in drug discovery, 2009 - Springer
Modulators of G protein-coupled receptors (GPCRs) form a key area for the pharmaceutical
industry, representing˜ 27% of all Food and Drug Administration (FDA)-approved drugs …