G-Protein-Coupled Receptors/GPCRs as Drug Target

G‐Protein‐Coupled Receptors/GPCRs as Drug Target Background

G protein-coupled receptors (GPCRs), which include ~900 members, represent the most leading family of validated drug targets in biomedicine. G protein-coupled receptors (GPCRs) have an important role in multiple diseases, including the development of cancer and cancer metastasis, and that's what makes GPCRs perfect drug targets for modern medicinal drugs.

When some GPCRs ligands such as chemokine, thrombin, lysophosphatidic acid (LPA), gastrin-releasing peptide and endothelin bind to their receptors, it causes a comformational change in G protein-coupled receptors (GPCRs) , which are involved in two signal transduction pathways: cAMP signaling pathway and phosphatidylinositol signaling pathway.

Recently, G protein-coupled receptors (GPCRs) have been an uprising star in drug therapy. One example of such GPCRs is chemokine receptor type 4 (CXCR4) which has great potential in drug target research. CXCR4 is thought to be involved in many disease states including more than 23 types of cancer and several immunodeficiency disorders, including head and neck cancer, breast cancer, small-cell lung cancer, non-small-cell lung cancer and Acquired Immune Deficiency Syndrome (AIDS).

G‐Protein‐Coupled Receptors/GPCRs Class A as Drug Target List

HTR2A HTR2B HTR4 HTR5A HTR6 HTR7
CHRM1 CHRM2 CHRM4 CHRM5 ADORA1 ADORA2A
ADORA2B ADORA3 ADRA1A ADRA1B ADRA2A ADRA2B
ADRB2 AGTR1 AGTR2 APLNR GPBAR1 GRPR
BDKRB1 BDKRB2 CNR1 CNR2 CMKLR1 CCR1
CCR2 CCR3 CCR4 CCR5 CCR6 CCR7
CCR8 CCR9 CXCR1 CXCR2 CXCR3 CXCR4
CXCR5 CXCR6 CX3CR1 ACKR1 ACKR2 ACKR3
C3AR1 C5AR1 C5AR2 DRD1 DRD2 DRD5
EDNRA EDNRB GPER1 RAMP3 FPR1 FPR2
FPR3 FFAR1 FFAR4 GALR2 FSHR HRH1
HCAR1 HCAR2 LTB4R CYSLTR1 OXGR1 OXER1
LPAR1 LPAR2 LPAR3 LPAR6 S1PR1 S1PR2
S1PR3 MCHR1 MC3R NMUR2 NPSR1 NPBWR2
NPY1R NPY2R NPY4R OPRD1 OPRK1 OPRL1
HCRTR2 P2RY1 P2RY2 P2RY6 P2RY8 P2RY12
PTAFR PROKR2 PRLHR PTGDR PTGDR2 PTGER1
PTGER3 PTGER4 PTGIR TBXA2R F2R F2RL1
F2RL3 RXFP2 RXFP3 SSTR1 SSTR2 TACR2
TSHR AVPR1A AVPR2      

G‐Protein‐Coupled Receptors/GPCRs Class A Orphan as Drug Target List

GPR6 GPR17 GPR19 GPR20 GPR25 GPR26
GPR27 GPR37 GPR37L1 GPR39 GPR45 GPR52
GPR61 GPR75 GPR83 GPR84 GPR85 GPR141
GPR155 GPR160 GPR161 GPR176 GPR182 GPR183
LGR4 LGR5        

G‐Protein‐Coupled Receptors/GPCRs Class B Orphan as Drug Target List

CALCR CALCRL RAMP1 RAMP2 CRHR1 SCTR
GCGR GLP1R GLP2R PTH1R ADCYAP1R1 VIPR1
VIPR2          

G‐Protein‐Coupled Receptors/GPCRs Adhesion Class Orphan as Drug Target List

ADGRE5 EMR1 EMR2 EMR3 GPR56 GPR64
GPR110 GPR113 GPR114 GPR116 GPR133  

Other G‐Protein‐Coupled Receptors/GPCRs as Drug Target List

GPRC6A GRM2 GRM3 GRM4 GPRC5B GPRC5D
FZD1 FZD2 FZD3 FZD4 FZD5 FZD6
FZD9 FZD10 GPR107 GPR137 GPR137B GPR143
GPR180          
Receptors
Receptors Classification
Receptors by Differentiation Cells
Receptors by Drug Target
GPCRs as Drug Target
GPCR Ligands as Drug Target
Nuclear Hormone Receptors as Drug Target
Cell Adhesion Receptors as Drug Target
Host Defense Receptors as Drug Target
Enzyme-Linked Receptors as Drug Target+
- Receptor Tyrosine Kinases as Drug Target
- Receptor Serine/Threonine Kinases as Drug Target
- Receptor Tyrosine Phosphatases as Drug Target
Other Receptors as Drug Target
Receptors by Functions
Receptors Reagent Products
Receptors by Species