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G-Protein-Coupled Receptor/GPCR Ligands as Drug Target

G‐Protein‐Coupled Receptor/GPCR Ligands as Drug Target Background

G-protein-coupled receptor/GPCR ligands are compounds that bind to a GPCRs. These may be conceptualized as "keys" that fit into a specific "lock" on the cell surface, the latter being the receptor, to modify cellular activity at the biophysical, biochemical, and/or genomic level.

The complex signaling pathways modulated by G-protein-coupled receptors/GPCRs offer a variety of potential drug targets. GPCRs are coupled to various members of the G protein superfamily, so named because of their functional dependence on the hydrolysis of the purine nucleotide, GTP, for activity.

GPCRs in mammals are classified into five main families, named Glutamate, Rhodopsin, Adhesion, Frizzled, and Secretin according to the GRAFS classification.

GPCRs regulate physiological responses to a variety of stimuli that include endogenous ligands such as biogenic amines, peptides, glycoproteins, lipids, nucleotides, Ca2+ ions, and various exogenous ligands for sensory perception such as odorants, pheromones, and even photons.

As a consequence, these receptors mediate multiple physiological processes such as neurotransmission, cellular metabolism, secretion, cellular differentiation, growth, inflammatory, and immune responses.

It is estimated that ~50% of clinically prescribed drugs and 25 of the 100 top selling drugs target GPCRs. Yet, only a small fraction of all GPCRs are presently targeted by drugs.

G‐Protein‐Coupled Receptor/GPCR & GPCR Ligands as Drug Target List

Chemokine Receptors Chemokine Ligands
CCR1 CCL3, CCL4, CCL5, CCL7, CCL14, CCL15, CCL16, CCL23
CCR2 CCL2, CCL7, CCL8, CCL12, CCL13
CCR3 CCL5, CCL7, CCL11, CCL13, CCL15, CCL24, CCL26, CCL28
CCR4 CCL2, CCL3, CCL5, CCL17, CCL22
CCR5 CCL3, CCL4, CCL5, CCL8
CCR6 CCL20
CCR7 CCL19, CCL21
CCR8 CCL1, CCL4, CCL17
CCR9 CCL25
CCL27, CCL28 XCL1, XCL2
CX3CR1 CX3CL1
CX3CL1 CXCL6, CXCL8
CXCR2 CXCL1, CXCL2, CXCL3, CXCL5, CXCL6, CXCL7, CXCL8
CXCR3 CXCL9, CXCL10, CXCL11
CXCR4 CXCL12
CXCR5 CXCL13
CXCR6 CXCL16

Other G‐Protein‐Coupled Receptor/GPCR Ligands as Drug Target List

ADM AGRP CALCA CALCB CARTPT CCK
CGA CGB CGB5 CGB7 CORT CRH
GAL GAST GCG GPHA2 GHRH GHRL
GIP GNRH1 GNRH2 GRP HCRT IAPP
MLN NMB NMU NPVF NPY NTS
PDYN PENK NPY NTS PDYN PENK
POMC PPY PTH PTHLH QRFP RLN1
RLN2 RLN3 TSHB TRH UCN2 UCN3
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