GPR20 Membrane Protein Introduction

Introduction of GPR20

GPR20 is encoded by the GPR20 gene. It belongs to the G-protein-coupled receptor (GPCR) family which has been greatly studied during the past few years. GPCRs are potential drug targets of about 34% of all modern clinical drugs because they are involved in many different diseases. GPR20 is one of a class A orphan GPCRs which has a similar structure to other identified GPCRs, whose endogenous ligand has not yet been identified.

Basic Information of GPR20
Protein Name	G-protein coupled receptor 20
Gene Name	GPR20
Aliases	NA
Organism	Homo sapiens (Human)
UniProt ID	Q99678
Transmembrane Times	7
Length (aa)	358
Sequence	MPSVSPAGPSAGAVPNATAVTTVRTNASGLEVPLFHLFARLDEELHGTFPGLWLALMAVHGAIFLAGLVLNGLALYVFCCRTRAKTPSVIYTINLVVTDLLVGLSLPTRFAVYYGARGCLRCAFPHVLGYFLNMHCSILFLTCICVDRYLAIVRPEGSRRCRQPACARAVCAFVWLAAGAVTLSVLGVTGSPCCRVFALTVLEFRLLPLLVISVFTGRIMCALSRPGLLHQGRQRRVRAMQLLLTVLIIFLVCFTPFHARQVAVALWPDMPHHTSLVVYHVAVTLSSLNSCMDPIVYCFVTSGFQATVRGLFGQHGEREPSSGDVVSMHRSSKGSGRHHILSAGPHALTQALANGPEA

Function of GPR20 Membrane Protein

The activity of GPR20 is regulated by G proteins, leading in the constitutive activation of its coupled G proteins in the absence of ligand. The basal level and the prostaglandin E2-induced production of cAMP were significantly decreased in HEK293 cell expressed GPR20 exogenously. A few studies also reported that the expression of GPR20 evaluates in the gastrointestinal tract such as the small intestine and the large intestine. The high expression of GPR20 can activate Gi proteins constitutively even through the absence of its ligand stimulation. Although the biological role of GPR20, as well as its endogenous ligand remain unclear, GPR20 is reported to be involved in many different cellular signaling processes, including control of intracellular cAMP levels and mitogenic signaling. Besides, a few studies reveal that GRP20 is closely related to nucleotide or lipid receptors and may have an important role in regulating the intestinal lipid transport.

Fig.1 Functional diagram of GPR20. (Hase, 2008)

Application of GPR20 Membrane Protein in Literature

Hase M., et al. Characterization of an Orphan G Protein-coupled Receptor, GPR20, That Constitutively Activates Gi Proteins. J Biol Chem. 2008, 283, 12747-12755. PubMed ID: 18347022

This article reports that GPR20 is involved in activation of Gi proteins and inhibition of the prostaglandin E(2)-induced cAMP production without its ligand stimulation.
O'Dowd B.F., et al. Cloning and chromosomal mapping of four putative novel human G-protein-coupled receptor genes. Gene. 1997, 187, 75-81. PubMed ID: 9073069

This article reveals that the gene of GPR20 was isolated by screening of a genomic library. The expression of GPR20 is detected in several human brain regions and also in liver by northern blot analysis.
Martin A.L., et al. Constitutive Activity among Orphan Class-A G Protein Coupled Receptors. PLoS ONE. 2015, 10(9): 451-463. PubMed ID: 26384023

This article focuses on evaluating the biological function of orphan class-A G-protein coupled receptors in the cAMP signaling pathway. It shows that GPR20 can inhibit the expression of CRE-mediated gene in GPR20 transiently expressed CHO-K1 cells.
Vélez J.I., et al. APOE*E2 allele delays age of onset in PSEN1 E280A Alzheimer's disease. Mol Psychiatry. 2016, 21, 916-924. PubMed ID: 26619808

Authors in this group analyzed about 50,000 genomic variants of 71 people from 'Paisa' pedigree and some GPR20 functional variants are involved in the Alzheimer's disease (AD). These variants of GPR20 are useful for finding the potential treatments for Alzheimer's disease.

GPR20 Preparation Options

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Reference

Hase M., et.al. (2008). Characterization of an Orphan G Protein-coupled Receptor, GPR20, That Constitutively Activates Gi Proteins. J Biol Chem. 283, 12747-12755.

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