[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 …

Mutations in G protein–coupled receptors: mechanisms, pathophysiology and potential therapeutic approaches

T Schöneberg, I Liebscher - Pharmacological reviews, 2021 - ASPET
There are approximately 800 annotated G protein–coupled receptor (GPCR) genes, making
these membrane receptors members of the most abundant gene family in the human …

The structural basis of G-protein-coupled receptor function and dysfunction in human diseases

T Schöneberg, A Schulz, T Gudermann - Reviews of physiology …, 2007 - Springer
Among the different families of transmembrane receptors, G-proteincoupled receptors
(GPCR) form the largest superfamily being present in yeast, plants, protozoa and metazoa …

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 …

Mutant G-protein-coupled receptors as a cause of human diseases

T Schöneberg, A Schulz, H Biebermann… - Pharmacology & …, 2004 - Elsevier
G-protein-coupled receptors (GPCR) are involved in directly and indirectly controlling an
extraordinary variety of physiological functions. Their key roles in cellular communication …

Molecular Manipulation of G Protein coupled Receptors A New Avenue into Drug Discovery

M Sautel, G Milligan - Current medicinal chemistry, 2000 - ingentaconnect.com
During the past 10 years or so, associated with the introduction of molecular biology
techniques to G protein coupled receptor (GPCR) research, outstanding progress has been …

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 …

[HTML][HTML] How genetic errors in GPCRs affect their function: possible therapeutic strategies

H Stoy, VV Gurevich - Genes & diseases, 2015 - Elsevier
Activating and inactivating mutations in numerous human G protein-coupled receptors
(GPCRs) are associated with a wide range of disease phenotypes. Here we use several …

orphan GPCRs as emerging drug targets

Y Fang, T Kenakin, C Liu - Frontiers in pharmacology, 2015 - frontiersin.org
G protein coupled-receptors (GPCRs) have been proven to be the most successful class of
druggable targets in the human genome. In fact, 30–50% of marketed drugs are estimated to …

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 …