MRGPRX2
entrez
117194
canonical
uniprot
Q96LB1
canonical
ensembl
ENSG00000183695
resolver
ensp
ENSP00000333800
resolver
enst
ENST00000329773
resolver
genesymbol
MRGPRX2
resolver
genesymbol_syn
MRGX2
resolver
hgnc
HGNC:17983
resolver
uniprot
B5B0C7
resolver
uniprot
Q4QXW4
resolver
uniprot
Q4QXW7
resolver
uniprot
Q4QXX0
resolver
uniprot
Q4QXX2
resolver
uniprot
Q4QXX3
resolver
uniprot
Q4QXX4
resolver
uniprot
Q4QXX6
resolver
uniprot
Q4QXX7
resolver
uniprot
W8W3L5
resolver
uniprot_entry
MRGX2_HUMAN
resolver
uniprot_sec
B5B0C7
resolver
uniprot_sec
Q4QXW4
resolver
uniprot_sec
Q4QXW7
resolver
uniprot_sec
Q4QXX0
resolver
uniprot_sec
Q4QXX2
resolver
uniprot_sec
Q4QXX3
resolver
uniprot_sec
Q4QXX4
resolver
uniprot_sec
Q4QXX6
resolver
uniprot_sec
Q4QXX7
resolver
uniprot_sec
W8W3L5
resolver
activity_regulation
ACTIVITY REGULATION: Activated by the selective small-molecule agonist ZINC-3573 (PubMed:28288109, PubMed:34789874). Inhibited by the selective small-molecule antagonist ZINC16991592 (PubMed:34789874). Activated by the basic secretagogue compound 48/80 (C48/80) (PubMed:34789875). {ECO:0000269|PubMed:28288109, ECO:0000269|PubMed:34789874, ECO:0000269|PubMed:34789875}.
uniprot
proteins
amino_acid_sequence
MDPTTPAWGTESTTVNGNDQALLLLCGKETLIPVFLILFIALVGLVGNGFVLWLLGFRMRRNAFSVYVLSLAGADFLFLCFQIINCLVYLSNFFCSISINFPSFFTTVMTCAYLAGLSMLSTVSTERCLSVLWPIWYRCRRPRHLSAVVCVLLWALSLLLSILEGKFCGFLFSDGDSGWCQTFDFITAAWLIFLFMVLCGSSLALLVRILCGSRGLPLTRLYLTILLTVLVFLLCGLPFGIQWFLILWIWKDSDVLFCHIHPVSVVLSSLNSSANPIIYFFVGSFRKQWRLQQPILKLALQRALQDIAEVDHSEGCFRQGTPEMSRSSLV
uniprot
proteins
function
FUNCTION: Mast cell-specific G protein-coupled receptor for basic secretagogues, which regulates mast cell degranulation and itch-related hypersensitivity reactions (PubMed:22069323, PubMed:25517090, PubMed:28288109, PubMed:34789874, PubMed:34789875). A secretagogue is an agent that promotes the secretion of hormones, neurohormones, chemical neurotransmitters or other compounds synthesized and secreted by cells (PubMed:25517090). Basic secretagogues comprise a set of cationic amphiphilic drugs, as well as endo- or exogenous peptides, consisting of a basic head group and a hydrophobic core (PubMed:25517090). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of downstream effectors, such as adenylate cyclase (PubMed:28288109, PubMed:34789874, PubMed:34789875). MRGPRX2 is both coupled to G(q) and G(i) G proteins: G(q) coupling activates phospholipase C-beta, releasing diacylglycerol (DAG) and inositol 1,4,5-trisphosphate (IP3) second messengers, while G(i) coupling mediates inhibition of adenylate cyclase activity (PubMed:28288109, PubMed:34789874, PubMed:34789875). Recognizes and binds small molecules containing a cyclized tetrahydroisoquinoline (THIQ), such as non-steroidal neuromuscular blocking drugs (NMBDs), including tubocurarine and atracurium (By similarity). In response to these compounds, mediates pseudo-allergic reactions characterized by histamine release, inflammation and airway contraction (By similarity). Acts as a receptor for substance P, a basic secretagogue neuropeptide released from the terminals of specific sensory nerves, initiating a signaling that mediates neurogenic inflammation and pain (PubMed:30686732, PubMed:34789875). Neurogenic inflammation includes mast cell activation, recruitment of immune cells and release of inflammatory mediators, such as cytokines and chemokines (By similarity). The inflammatory response can then activate or sensitize nociceptors, promoting pain (By similarity). Acts as a receptor for a number of other ligands, including peptides and alkaloids, such as cortistatin-14, proadrenomedullin peptides PAMP-12 and, at lower extent, PAMP-20, antibacterial protein LL-37, PMX-53 peptide, beta-defensins, complanadine A and CXCL17 (PubMed:12915402, PubMed:15823563, PubMed:21441599, PubMed:22069323, PubMed:23698749, PubMed:24930830, PubMed:34789874, PubMed:34789875). Also acts as a receptor for opioids, such as (-)- and (+)-morphine, hydrocodone, sinomenine, dextromethorphan, dynorphin A, dynorphin B, and alpha- and beta-neoendorphin, promoting mast cell degranulation (PubMed:28288109). {ECO:0000250|UniProtKB:Q3KNA1, ECO:0000269|PubMed:12915402, ECO:0000269|PubMed:15823563, ECO:0000269|PubMed:21441599, ECO:0000269|PubMed:22069323, ECO:0000269|PubMed:23698749, ECO:0000269|PubMed:24930830, ECO:0000269|PubMed:25517090, ECO:0000269|PubMed:28288109, ECO:0000269|PubMed:30686732, ECO:0000269|PubMed:34789874, ECO:0000269|PubMed:34789875, ECO:0000269|PubMed:41167449}.
uniprot
proteins
mass_dalton
37099
uniprot
proteins
mutagenesis
MUTAGEN 94; /note="F->I: Abolished G protein-coupled receptor signaling in response to Substance P-binding."; /evidence="ECO:0000269|PubMed:39725036"; MUTAGEN 127; /note="R->A: Decreased G(i)-coupled signaling."; /evidence="ECO:0000269|PubMed:34789875"; MUTAGEN 138; /note="R->A: Decreased G(i)-coupled signaling."; /evidence="ECO:0000269|PubMed:34789875"; MUTAGEN 164; /note="E->A: Decreased G protein-coupled receptor signaling."; /evidence="ECO:0000269|PubMed:34789874"; MUTAGEN 165; /note="G->W: Abolished G protein-coupled receptor signaling in response to Substance P-binding."; /evidence="ECO:0000269|PubMed:39725036"; MUTAGEN 168; /note="C->A: Abolished G protein-coupled receptor signaling."; /evidence="ECO:0000269|PubMed:34789874, ECO:0000269|PubMed:34789875"; MUTAGEN 170; /note="F->A: Decreased G protein-coupled receptor signaling in response to cortistatin-14 binding."; /evidence="ECO:0000269|PubMed:34789874, ECO:0000269|PubMed:34789875"; MUTAGEN 180; /note="C->A: Abolished G protein-coupled receptor signaling."; /evidence="ECO:0000269|PubMed:34789874"; MUTAGEN 184; /note="D->A: Decreased G protein-coupled receptor signaling."; /evidence="ECO:0000269|PubMed:34789874"; MUTAGEN 214; /note="R->A: Decreased G(i)-coupled signaling."; /evidence="ECO:0000269|PubMed:34789875"; MUTAGEN 243; /note="W->A: Abolished G protein-coupled receptor signaling in response to cortistatin-14 binding."; /evidence="ECO:0000269|PubMed:34789874
uniprot
proteins
protein_family
G protein-coupled receptor 1 family
uniprot
proteins
protein_family
Mas subfamily
uniprot
proteins
pubmed
11551509
uniprot
proteins
pubmed
12044878
uniprot
proteins
pubmed
12915402
uniprot
proteins
pubmed
15489334
uniprot
proteins
pubmed
15823563
uniprot
proteins
pubmed
15862286
uniprot
proteins
pubmed
16161007
uniprot
proteins
pubmed
21441599
uniprot
proteins
pubmed
22069323
uniprot
proteins
pubmed
23698749
uniprot
proteins
pubmed
24583173
uniprot
proteins
pubmed
24930830
uniprot
proteins
pubmed
25517090
uniprot
proteins
pubmed
28288109
uniprot
proteins
pubmed
30686732
uniprot
proteins
pubmed
34789874
uniprot
proteins
pubmed
34789875
uniprot
proteins
pubmed
39725036
uniprot
proteins
pubmed
41167449
uniprot
proteins
sequence_length
330
uniprot
proteins
subcellular_location
SUBCELLULAR LOCATION: Cell membrane {ECO:0000305|PubMed:34789875}; Multi-pass membrane protein {ECO:0000269|PubMed:34789874, ECO:0000269|PubMed:34789875}.
uniprot
proteins
transmembrane_region
TRANSMEM 29..56; /note="Helical; Name=1"; /evidence="ECO:0000269|PubMed:34789874, ECO:0000269|PubMed:34789875, ECO:0007744|PDB:7S8L, ECO:0007744|PDB:7S8M, ECO:0007744|PDB:7S8N, ECO:0007744|PDB:7S8O, ECO:0007744|PDB:7VDH, ECO:0007744|PDB:7VDL, ECO:0007744|PDB:7VDM, ECO:0007744|PDB:7VUY, ECO:0007744|PDB:7VUZ, ECO:0007744|PDB:7VV0, ECO:0007744|PDB:7VV3, ECO:0007744|PDB:7VV4, ECO:0007744|PDB:7VV5, ECO:0007744|PDB:7VV6"; TRANSMEM 64..93; /note="Helical; Name=2"; /evidence="ECO:0000269|PubMed:34789874, ECO:0000269|PubMed:34789875, ECO:0007744|PDB:7S8L, ECO:0007744|PDB:7S8M, ECO:0007744|PDB:7S8N, ECO:0007744|PDB:7S8O, ECO:0007744|PDB:7VDH, ECO:0007744|PDB:7VDL, ECO:0007744|PDB:7VDM, ECO:0007744|PDB:7VUY, ECO:0007744|PDB:7VUZ, ECO:0007744|PDB:7VV0, ECO:0007744|PDB:7VV3, ECO:0007744|PDB:7VV4, ECO:0007744|PDB:7VV5, ECO:0007744|PDB:7VV6"; TRANSMEM 103..129; /note="Helical; Name=3"; /evidence="ECO:0000269|PubMed:34789874, ECO:0000269|PubMed:34789875, ECO:0007744|PDB:7S8L, ECO:0007744|PDB:7S8M, ECO:0007744|PDB:7S8N, ECO:0007744|PDB:7S8O, ECO:0007744|PDB:7VDH, ECO:0007744|PDB:7VDL, ECO:0007744|PDB:7VDM, ECO:0007744|PDB:7VUY, ECO:0007744|PDB:7VUZ, ECO:0007744|PDB:7VV0, ECO:0007744|PDB:7VV3, ECO:0007744|PDB:7VV4, ECO:0007744|PDB:7VV5, ECO:0007744|PDB:7VV6"; TRANSMEM 145..170; /note="Helical; Name=4"; /evidence="ECO:0000269|PubMed:34789874, ECO:0000269|PubMed:34789875, ECO:0007744|PDB:7S8L, ECO:0007744|PDB:7S8M, ECO:0007744|PDB:7S8N, ECO:0007744|PDB:7S8O, ECO:0007744|PDB:7VDH, ECO:0007744|PDB:7VDL, ECO:0007744|PDB:7VDM, ECO:0007744|PDB:7VUY, ECO:0007744|PDB:7VUZ, ECO:0007744|PDB:7VV0, ECO:0007744|PDB:7VV3, ECO:0007744|PDB:7VV4, ECO:0007744|PDB:7VV5, ECO:0007744|PDB:7VV6"; TRANSMEM 179..207; /note="Helical; Name=5"; /evidence="ECO:0000269|PubMed:34789874, ECO:0000269|PubMed:34789875, ECO:0007744|PDB:7S8L, ECO:0007744|PDB:7S8M, ECO:0007744|PDB:7S8N, ECO:0007744|PDB:7S8O, ECO:0007744|PDB:7VDH, ECO:0007744|PDB:7VDL, ECO:0007744|PDB:7VDM, ECO:0007744|PDB:7VUY, ECO:0007744|PDB:7VUZ, ECO:0007744|PDB:7VV0, ECO:0007744|PDB:7VV3, ECO:0007744|PDB:7VV4, ECO:0007744|PDB:7VV5, ECO:0007744|PDB:7VV6"; TRANSMEM 221..250; /note="Helical; Name=6"; /evidence="ECO:0000269|PubMed:34789874, ECO:0000269|PubMed:34789875, ECO:0007744|PDB:7S8L, ECO:0007744|PDB:7S8M, ECO:0007744|PDB:7S8N, ECO:0007744|PDB:7S8O, ECO:0007744|PDB:7VDH, ECO:0007744|PDB:7VDL, ECO:0007744|PDB:7VDM, ECO:0007744|PDB:7VUY, ECO:0007744|PDB:7VUZ, ECO:0007744|PDB:7VV0, ECO:0007744|PDB:7VV3, ECO:0007744|PDB:7VV4, ECO:0007744|PDB:7VV5, ECO:0007744|PDB:7VV6"; TRANSMEM 257..283; /note="Helical; Name=7"; /evidence="ECO:0000269|PubMed:34789874, ECO:0000269|PubMed:34789875, ECO:0007744|PDB:7S8L, ECO:0007744|PDB:7S8M, ECO:0007744|PDB:7S8N, ECO:0007744|PDB:7S8O, ECO:0007744|PDB:7VDH, ECO:0007744|PDB:7VDL, ECO:0007744|PDB:7VDM, ECO:0007744|PDB:7VUY, ECO:0007744|PDB:7VUZ, ECO:0007744|PDB:7VV0, ECO:0007744|PDB:7VV3, ECO:0007744|PDB:7VV4, ECO:0007744|PDB:7VV5, ECO:0007744|PDB:7VV6
uniprot
proteins