Target Information
| Target General Information | Top | |||||
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| Target ID |
T57253
(Former ID: TTDI01728)
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| Target Name |
Mas-related G protein-coupled receptor X1 (MRGX1)
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| Synonyms |
Sensory neuron-specific G-protein coupled receptor 3/4; SNSR4; SNSR3; Mas-related G-protein coupled receptor member X1; MRGX1
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| Gene Name |
MRGPRX1
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| Target Type |
Literature-reported target
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[1] | ||||
| Function |
Orphan receptor. Probably involved in the function of nociceptive neurons. May regulate nociceptor function and/or development, including the sensation or modulation of pain. Potently activated by enkephalins including BAM22 (bovine adrenal medulla peptide 22) and BAM (8-22). BAM22 is the most potent compound and evoked a large and dose-dependent release of intracellular calcium in stably transfected cells. G(alpha)q proteins are involved in the calcium-signaling pathway. Activated by the antimalarial drug, chloroquine. May mediate chloroquine-induced itch, in a histamine-independent manner.
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| UniProt ID | ||||||
| Sequence |
MDPTISTLDTELTPINGTEETLCYKQTLSLTVLTCIVSLVGLTGNAVVLWLLGCRMRRNA
FSIYILNLAAADFLFLSGRLIYSLLSFISIPHTISKILYPVMMFSYFAGLSFLSAVSTER CLSVLWPIWYRCHRPTHLSAVVCVLLWALSLLRSILEWMLCGFLFSGADSAWCQTSDFIT VAWLIFLCVVLCGSSLVLLIRILCGSRKIPLTRLYVTILLTVLVFLLCGLPFGIQFFLFL WIHVDREVLFCHVHLVSIFLSALNSSANPIIYFFVGSFRQRQNRQNLKLVLQRALQDASE VDEGGGQLPEEILELSGSRLEQ 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: 2-(Cyclopropanesulfonamido)-N-(2-ethoxyphenyl)benzamide | Ligand Info | |||||
| Structure Description | CryoEM structure of Gq-coupled MRGPRX1 with peptide ligand BAM8-22 and positive allosteric modulator ML382 | PDB:8DWG | ||||
| Method | Electron microscopy | Resolution | 2.71 Å | Mutation | No | [2] |
| PDB Sequence |
CYKQTLSLTV
32 LTCIVSLVGL42 TGNAVVLWLL52 GCRMRRNAFS62 IYILNLAAAD72 FLFLSGRLIY 82 SLLSFISIPH92 TISKILYPVM102 MFSYFAGLSF112 LSAVSTERCL122 SVLWPIWYRC 132 HRPTHLSAVV142 CVLLWALSLL152 RSILEWMLCG162 FLFSGADSAW172 CQTSDFITVA 182 WLIFLCVVLC192 GSSLVLLIRI202 LCLTRLYVTI218 LLTVLVFLLC228 GLPFGIQFFL 238 FLWIHVDREV248 LFCHVHLVSI258 FLSALNSSAN268 PIIYFFV
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| Ligand Name: MRGPRX1 agonist 1 | Ligand Info | |||||
| Structure Description | CryoEM structure of Gq-coupled MRGPRX1 with ligand Compound-16 | PDB:8DWH | ||||
| Method | Electron microscopy | Resolution | 3.25 Å | Mutation | No | [2] |
| PDB Sequence |
KQTLSLTVLT
34 CIVSLVGLTG44 NAVVLWLLGC54 RMRRNAFSIY64 ILNLAAADFL74 FLSGRLIYSL 84 LSFISIPHTI94 SKILYPVMMF104 SYFAGLSFLS114 AVSTERCLSV124 LWPIWYRCHR 134 PTHLSAVVCV144 LLWALSLLRS154 ILEWMLCGFL164 FSGADSAWCQ174 TSDFITVAWL 184 IFLCVVLCGS194 SLVLLIRILC204 LTRLYVTILL220 TVLVFLLCGL230 PFGIQFFLFL 240 WIHVDREVLF250 CHVHLVSIFL260 SALNSSANPI270 IYFFVGSF
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| 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 Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| References | Top | |||||
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| REF 1 | Targeting human Mas-related G protein-coupled receptor X1 to inhibit persistent pain. Proc Natl Acad Sci U S A. 2017 Mar 7;114(10):E1996-E2005. | |||||
| REF 2 | Ligand recognition and allosteric modulation of the human MRGPRX1 receptor. Nat Chem Biol. 2023 Apr;19(4):416-422. | |||||
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