Mas-related Gene GPCR Assays
Background of Mas-related Gene Receptors
Mas-related gene (Mrg), also known as Mas-related G protein-coupled receptors (Mrgprs), are a class of G-protein coupled receptors (GPCRs) encoded by the Mrgpr gene family. More than 50 members in rodents and humans have been identified as belonging to the Mrgpr family, which are grouped into 9 subfamilies (MRGPRA to -H and -X). Mrgprs are described to be predominantly expressed in dorsal root ganglia (DRG) and trigeminal ganglia (TG) neurons, which establishes significant roles of Mrgprs in the nociceptive signaling pathway and itch sensation.
Fig.1. Ligands for the Mas-related G protein-coupled receptor X2. (Quan, 2021)
Important Functions of Mas-related Gene Receptors
- Role of Mrgprs in the nociception: Mrgpr proteins, mainly MrgprD, MrgprC, and MRGPRX1, are important regulators in neuropathic pain behavior as well as somatic and visceral nociception. These Mrgprs have emerged as potential targets for nociception remission.
- Role of Mrgprs in the itch sensation: MrgprA3 or MRGPRX1 (the human ortholog of mouse MrgprA3), MrgprC11, and MrgprD proteins can be activated by pruritogens resulting in itch sensation in a non-histaminergic dependent manner.
- Role of Mrgprs in the immune defense: MrgprB2 (or MRGPRX2 in humans) was the first Mrgpr identified in the immune system, which was mainly expressed by mast cells and implicated in a series of pathophysiological pathways, including neuroimmunity, inflammatory reactions, and host defenses.
Fig.2 The expressions and functions of Mrgprs. (Serhan, 2021)
Subtypes and Mechanisms of Mas-related Gene Receptors
Human Mrgprs consist of MRGPRX1, MRGPRX2, MRGPRX3, and MRGPRX4, of which MRGPRX1, MRGPRX3, and MRGPRX4 are important receptors in the nociception and itch sensation while MRGPRX2 is identified as a regulator in the immune system.
| Receptor | Gene | Mechanism | Agonists | Antagonists |
| MRGPRX1 | MRGPRX1 |
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| MRGPRX2 | MRGPRX2 |
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| MRGPRX3 | MRGPRX3 |
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| MRGPRX4 | MRGPRX4 |
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Assay List of Mas-related Gene Receptors
Creative Biolabs can provide a range of assays of mas-related gene receptors. You can choose the assay in the list or contact us for more information:
| Assay No. | Assay Name | Host Cell | Assay Type | Datasheet |
|---|---|---|---|---|
| Calcium Flux Assay | ||||
| S01YF-1122-KX589 | Magic™ Human MRGPRE In Vitro Calcium Flux Assay | CHO-K1-Gα16 | Calcium Flux Assay | |
| Assay No. | Assay Name | Host Cell | Assay Type | Datasheet |
|---|---|---|---|---|
| Calcium Flux Assay | ||||
| S01YF-1122-KX590 | Magic™ Human MRGPRF In Vitro Calcium Flux Assay | CHO-K1-Gα16 | Calcium Flux Assay | |
| Assay No. | Assay Name | Host Cell | Assay Type | Datasheet |
|---|---|---|---|---|
| Calcium Flux Assay | ||||
| S01YF-1122-KX591 | Magic™ Human MRGPRX1 In Vitro Calcium Flux Assay | CHO-K1 | Calcium Flux Assay | |
Published Data
| Paper Title | MRGPRX2 activation as a rapid, high-throughput mechanistic-based approach for detecting peptide-mediated human mast cell degranulation liabilities |
| Journal | Journal of Immunotoxicology |
| Published | 2020 |
| Abstract | In addition to the IgE-dependent manner, mast cell degranulation (MCD) also can be induced by a non-IgE manner, that is MRGPRX2. Cell-based MRGPRX2 activation assay has been conducted to determine and assess the release of histamine, including both G protein-dependent and independent pathways, to screen peptides for MCD. |
| Result |
Cell-based MRGPRX2 activation assay can be used for effective peptide candidate screening and safety evaluation for MCD in time-saving and high-throughput manners.
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Fig.3. Peptide responses in the MRGPRX2 activation assay. (Lafleur, 2020)
References
- Quan, P. L.; et al. The Multifaceted Mas-Related G Protein-Coupled Receptor Member X2 in Allergic Diseases and Beyond. International Journal of Molecular Sciences. 2021, 22(9): 4421.
- Serhan, N.; et al. Mas-related G protein-coupled receptors (Mrgprs) – Key regulators of neuroimmune interactions. Neuroscience Letters. 2021, 749: 135724.
- Lafleur, M.A.; et al. MRGPRX2 activation as a rapid, high-throughput mechanistic-based approach for detecting peptide-mediated human mast cell degranulation liabilities. Journal of Immunotoxicology. 2020, 17(1): 110-121.
