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GPCRs: The most promiscuous druggable receptor of the mankind
- Source :
- Saudi Pharmaceutical Journal : SPJ, Saudi Pharmaceutical Journal, Vol 29, Iss 6, Pp 539-551 (2021)
- Publication Year :
- 2021
- Publisher :
- Elsevier BV, 2021.
-
Abstract
- All physiological events in living organisms originated as specific chemical/biochemical signals on the cell surface and transmitted into the cytoplasm. This signal is translated within milliseconds–hours to a specific and unique order required to maintain optimum performance and homeostasis of living organisms. Examples of daily biological functions include neuronal communication and neurotransmission in the process of learning and memory, secretion (hormones, sweat, and saliva), muscle contraction, cellular growth, differentiation and migration during wound healing, and immunity to fight infections. Among the different transducers for such life-dependent signals is the large family of G protein-coupled receptors (GPCRs). GPCRs constitute roughly 800 genes, corresponding to 2% of the human genome. While GPCRs control a plethora of pathophysiological disorders, only approximately one-third of GPCR families have been deorphanized and characterized. Recent drug data show that around 40% of the recommended drugs available in the market target mainly GPCRs. In this review, we presented how such system signals, either through G protein or via other players, independent of G protein, function within the biological system. We also discussed drugs in the market or clinical trials targeting mainly GPCRs in various diseases, including cancer.
- Subjects :
- 0301 basic medicine
ERK, Extracellular signal-Regulated Kinase
cAMP, cyclic AMP
G protein
CCR, Chemokine Receptor
GLP1R, Glucagon-Like Peptide-1 Receptor
Druggability
Heterodimerization
Pharmaceutical Science
RM1-950
Review
Computational biology
COX, Cyclooxygenase
Biology
GRKs
AC, Adenylyl Cyclase
03 medical and health sciences
GPCR
0302 clinical medicine
DAG, Diacylglycerol
Arrestin
PKA, Protein Kinase A
PIP2, Phosphatidylinositol-4,5-bisphosphate
Receptor
Gene
GRKs, G protein-coupled Receptor Kinases
G protein-coupled receptor
Pharmacology
G protein-coupled receptor kinase
NMDA, N-Methyl D-Aspartate
Drugs
Nbs, Nanobodies
MAPK, Mitogen-Activated Protein Kinase
Signaling
030104 developmental biology
PAR-1, Protease Activated Receptor 1
Therapeutics. Pharmacology
IP3, Inositol 1,4,5-triphosphate
GIP, Gastric Inhibitory Peptide
030217 neurology & neurosurgery
Function (biology)
G proteins
Subjects
Details
- ISSN :
- 13190164
- Volume :
- 29
- Database :
- OpenAIRE
- Journal :
- Saudi Pharmaceutical Journal
- Accession number :
- edsair.doi.dedup.....14339e0def5699befb4d16ab07f7bd41