Mas-Related G-Protein Coupled Receptor Family

The Mas-related G protein-coupled receptors (MRGPRs) comprise a subfamily of GPCRs. MRGPRs family comprises almost 40 members which can be grouped into nine distinct subfamilies (MRGPRA to -H and -X) and almost all the members are still considered "orphan" with no endogenous ligands identified. However, several distinct peptides and amino acids are evaluated as potential ligands, including β-alanine, angiotensin-(1-7), alamandine, GABA, cortistatin-14, and cleavage products of proenkephalin, pro-opiomelanocortin, prodynorphin, or pro-neuropeptide-FF-A.

Most MRGPRs, including all MRGPRA, MRGPRB, and part of MRGPRC and MRGPRD subfamily members, are nearly and exclusively expressed in specific dorsal root and trigeminal ganglia neurons and play important roles in nociception, itch, or pruritus, and thermosensation. Some MRGPRs, such as human MRGPRX2 and rat MRGPRB3, are probably the long-sought low-affinity, low-selectivity receptors on mast cells that mediate IgE-independent degranulating actions. In vitro overexpression cells, MRGPRs present tumorigenic and proliferative actions when the accumulation exceeds a certain threshold, which is normally not reached in vivo. Some MRGPRs have been shown to be expressed in cardiovascular organs and exploited its protective actions in cardiovascular and metabolic diseases. The further investigations on MRGPRs reveal their physiologic and pathophysiologic functions with great therapeutic potency.

Here shows a part of members of MRGPRs, including MRGPRD to -G and MRGPRX1 to -X4. MRGPRD is the first identified non-orphan receptor that recognizes β-alanine as a ligand and its activation is transmitted by both G_q and G_i proteins onto changes of intracellular Ca²⁺ and cAMP. MRGPRE most likely binds MRGPRD to form heterodimers. MRGPRX1 can be activated by BAM22, a product of proenkephalin A metabolism. β-defensins (e.g., hBD2 and hBD3) and cathelicidines (e.g., LL-37), are ligands for MRGPRX2 receptor on human mast cells. For MRGPRF, MRGPRG, MRGPRX3 and MRGPRX4, no ligand has been described yet.

Human Mas-related G-protein Coupled Receptor Members
MRGPRD	MRGPRX2

Aided by cutting-edge Magic™ membrane protein production platform, Creative Biolabs is proud to offer the preparation of these targets in required formats using various strategies, such as detergent micelles, proteoliposomes, nanodiscs, lipoparticles, polymers, stable cell line.

Magic™ membrane protein production platform – Creative Biolabs

Meanwhile, our Magic™ membrane protein antibody discovery platform can help to discover antibodies against these targets, even fully humanized antibodies, by various approaches including hybridoma technology, phage display technology, etc. We also present DNA immunization service for anti-membrane protein antibody development. Please feel free to contact us for more information.

All listed services and products are For Research Use Only. Do Not use in any diagnostic or therapeutic applications.

Online Inquiry

	USA: Europe: Germany:
	Call us at: USA: UK: Germany:
	Fax:
	Email: