Mas-related Gene Family Related Drug Discovery Products
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MAS-related G protein–coupled receptors (MRGPR) is a new GPCR family. The MRGPR family consists of ∼40 members that are divided into nine separate subfamilies (MRGPRA through -H and -X) and are largely expressed in primary sensory neurons and mast cells. Although the complete range of biological functions for all MRGPR are still unknown, there is evidence that certain MRGPR subtypes play a part in nociception, pruritus, sleep, cell proliferation, circulation, and mast cell degranulation.
Fig.1 MAS-related G protein–coupled receptors. (Solinski, 2014)
With years of experience in the field of drug discovery and development, Creative Biolabs can offer mas-related gene family tools to contribute to the success of your project:
Overview of Mas-related Gene Family
Mrgprs is a subfamily related to the proto-oncogene Mas1. Mrgprs research has been difficult in part because receptor expression varies between species. Humans have eight subfamilies, compared to seven for rodents (A–G), of which only four (MRGPR D–G) clearly share sequences with their rodent counterparts. On the other hand, rodents lack any obvious orthologues of the Mrgprs in the X family (X1-4), which are only found in primates. The rodent A family and the rodent A, B, and C families share functional similarities in the mrgprs of the X family. Although Mrgpr family receptors are orphans, several agonists have been suggested.
- MAS-Related G Protein–Coupled Receptors A
The first MRGPR to be examined in a functional experiment were the mouse MRGPRA members 1 and 4. Both receptors responded to many peptides of the RFamide family proven to influence nociception in vertebrates. By activating MRGPRA1, the mammalian neuropeptide FF (NPFF) boosted intracellular calcium concentrations, and the mammalian neuropeptide AF (NPAF) did the same for the MRGPRA4 subtype.
- MAS-Related G Protein–Coupled Receptors B
None of the rodent MRGPRB members has been attributed to any ligand thus far. The spinal laminaIIo, a region of the substantia gelatinosa that processes spinal pain, is where MRGPRB4-positive neurons project. According to these results, MRGPRB4 may designate C-fiber tactile afferents, which are meant to sense light touching and stroking.
- MAS-Related G Protein–Coupled Receptors C
Rats and mice each have a single gene that codes for a protein of the rodent MRGPRC subfamily, and both receptor subtypes may bind a variety of ligands. A group of various but structurally related peptides were used to activate the MRGPRC from rat and mouse to elicit calcium signals.
- MAS-Related G Protein–Coupled Receptors D
The MRGPRD subfamily consists of only one receptor subtypeper species, which is conserved in rodents and primates. It has been determined that β-alanine is a ligand of MRGPRD and that this may be the cause of their endogenous actions.
- MAS-Related G Protein–Coupled Receptors E to -H
Except for MRGPRH, which is found solely in rodents, all members of the subfamilies MRGPRE through -H have a single receptor per species. No member of these MRGPR has ever been assigned to a ligand.
- MAS-Related G Protein–Coupled Receptors X
MRGPRX1 and -2 function via G protein activation. Both receptors additionally encouraged the release of calcium from internal stores via the PLCb-mediated production of inositol-1,4,5-trisphosphate. According to their expression patterns, MRGPRX1 and MRGPRX2 may be involved in the biology of mast cells, the plasticity of primary sensory neurons, and the functioning of somatosensory detectors. Despite specific expression, data demonstrating MRGPRX2-mediated actions in primary sensory neurons are currently few. MRGPRX2 may also cause hypotension and slow-wave sleep, among other things.
Fig.2 Potential mechanisms of MRGPRX2. (Hawker, 2023)
References
- Solinski, H.J.; et al. Pharmacology and signaling of MAS-related G protein–coupled receptors. Pharmacological reviews. 2014, 66(3): 570-597.
- Hawker, P.; et al. Mas‐Related G Protein‐Coupled Receptors in Gastrointestinal Dysfunction and Inflammatory Bowel Disease: A Review. British Journal of Pharmacology. 2023.
