Target Information
| Target General Information | Top | |||||
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| Target ID |
T38187
(Former ID: TTDI02127)
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| Target Name |
Mas-related gene 2 (MRGX2)
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| Synonyms |
Masrelated Gprotein coupled receptormember X2; MRGPRX2
Click to Show/Hide
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| Gene Name |
MRGPRX2
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| Target Type |
Literature-reported target
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[1] | ||||
| Function |
Mast cell-specific receptor for basic secretagogues (PubMed:25517090). Basic secretagogues are a set of cationic amphiphilic drugs, as well as endo- and exogenous peptides, which share basic head group combined with a hydrophobic core of the molecule. Recognizes and binds small molecules containing a cyclized a tetrahydroisoquinoline (THIQ), such as non-steroidal neuromuscular blocking drugs (NMBDs), including tubocurarine and atracurium. Mediates mast cell responsiveness and side effects of small-molecule therapeutic drugs by acting as a specific receptor for basic secretagogues drugs in mast cells: binding to drugs induces pseudo-allergic reactions characterized by histamine release, inflammation and airway contraction. Acts as a receptor for a number of ligands, including peptides: acts as a receptor of cortistatin-14, a regulator of sleep regulation locomotor activity, and cortical function (PubMed:12915402). Acts as a receptor for proadrenomedullin N- terminal peptides PAMP-12, and atlower extent PAMP-20 (PubMed:15823563). Acts as a receptor for antibacterial protein LL-37, promoting chemotaxis, degranulation and chemokine production in mast cells (PubMed:22069323). Acts as a receptor for PMX-53 peptide, a potent antagonist of C5AR1/CD88 (PubMed:21441599). Acts as a receptor for beta-defensins (PubMed:23698749). Acts as a receptor for complanadine A, an alkaloid (PubMed:24930830). {ECO:0000250|UniProtKB:Q3UG50, 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:0000305|PubMed:12915402}.
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| BioChemical Class |
GPCR rhodopsin
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| UniProt ID | ||||||
| Sequence |
MDPTTPAWGTESTTVNGNDQALLLLCGKETLIPVFLILFIALVGLVGNGFVLWLLGFRMR
RNAFSVYVLSLAGADFLFLCFQIINCLVYLSNFFCSISINFPSFFTTVMTCAYLAGLSML STVSTERCLSVLWPIWYRCRRPRHLSAVVCVLLWALSLLLSILEGKFCGFLFSDGDSGWC QTFDFITAAWLIFLFMVLCGSSLALLVRILCGSRGLPLTRLYLTILLTVLVFLLCGLPFG IQWFLILWIWKDSDVLFCHIHPVSVVLSSLNSSANPIIYFFVGSFRKQWRLQQPILKLAL QRALQDIAEVDHSEGCFRQGTPEMSRSSLV Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
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| Ligand Name: Cholesterol | Ligand Info | |||||
| Structure Description | Cryo-EM structure of pseudoallergen receptor MRGPRX2 complex with C48/80, state1 | PDB:7VV5 | ||||
| Method | Electron microscopy | Resolution | 2.76 Å | Mutation | No | [2] |
| PDB Sequence |
LLLLCGKETL
31 IPVFLILFIA41 LVGLVGNGFV51 LWLLGFRMRR61 NAFSVYVLSL71 AGADFLFLCF 81 QIINCLVYLS91 NFFCSISINF101 PSFFTTVMTC111 AYLAGLSMLS121 TVSTERCLSV 131 LWPIWYRCRR141 PRHLSAVVCV151 LLWALSLLLS161 ILEGKFCGFL171 FSDGDSGWCQ 181 TFDFITAAWL191 IFLFMVLCGS201 SLALLVRILC211 GSRGLPLTRL221 YLTILLTVLV 231 FLLCGLPFGI241 QWFLILWIWK251 DSDVLFCHIH261 PVSVVLSSLN271 SSANPIIYFF 281 VGSFRKQW
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Ligand Name: 2-[4-methoxy-3-[[2-methoxy-3-[[2-methoxy-5-[2-(methylamino)ethyl]phenyl]methyl]-5-[2-(methylamino)ethyl]phenyl]methyl]phenyl]-~{N}-methyl-ethanamine | Ligand Info | |||||
| Structure Description | Cryo-EM structure of pseudoallergen receptor MRGPRX2 complex with C48/80, state1 | PDB:7VV5 | ||||
| Method | Electron microscopy | Resolution | 2.76 Å | Mutation | No | [2] |
| PDB Sequence |
LLLLCGKETL
31 IPVFLILFIA41 LVGLVGNGFV51 LWLLGFRMRR61 NAFSVYVLSL71 AGADFLFLCF 81 QIINCLVYLS91 NFFCSISINF101 PSFFTTVMTC111 AYLAGLSMLS121 TVSTERCLSV 131 LWPIWYRCRR141 PRHLSAVVCV151 LLWALSLLLS161 ILEGKFCGFL171 FSDGDSGWCQ 181 TFDFITAAWL191 IFLFMVLCGS201 SLALLVRILC211 GSRGLPLTRL221 YLTILLTVLV 231 FLLCGLPFGI241 QWFLILWIWK251 DSDVLFCHIH261 PVSVVLSSLN271 SSANPIIYFF 281 VGSFRKQW
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Similarity Proteins
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| Chemical Structure based Activity Landscape of Target | Top |
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| Target Profiles in Patients | Top | |||||
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| Target Expression Profile (TEP) | ||||||
| References | Top | |||||
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| REF 1 | NCBI GEO: archive for functional genomics data sets--update. Nucleic Acids Res. 2013 Jan;41(Database issue):D991-5. | |||||
| REF 2 | Structure, function and pharmacology of human itch receptor complexes. Nature. 2021 Dec;600(7887):164-169. | |||||
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