Details of the Target

General Information of Target

Target ID LDTP05544
Target Name Regulator of G-protein signaling 1 (RGS1)
Gene Name RGS1
Gene ID 5996
Synonyms
1R20; BL34; IER1; Regulator of G-protein signaling 1; RGS1; B-cell activation protein BL34; Early response protein 1R20
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MRAAAISTPKLDKMPGMFFSANPKELKGTTHSLLDDKMQKRRPKTFGMDMKAYLRSMIPH
LESGMKSSKSKDVLSAAEVMQWSQSLEKLLANQTGQNVFGSFLKSEFSEENIEFWLACED
YKKTESDLLPCKAEEIYKAFVHSDAAKQINIDFRTRESTAKKIKAPTPTCFDEAQKVIYT
LMEKDSYPRFLKSDIYLNLLNDLQANSLK
Target Bioclass
Other
Subcellular location
Cell membrane
Function
Regulates G protein-coupled receptor signaling cascades, including signaling downstream of the N-formylpeptide chemoattractant receptors and leukotriene receptors. Inhibits B cell chemotaxis toward CXCL12. Inhibits signal transduction by increasing the GTPase activity of G protein alpha subunits thereby driving them into their inactive GDP-bound form.
Uniprot ID
Q08116
Ensemble ID
ENST00000367459.8
HGNC ID
HGNC:9991

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
HCC15 SNV: p.A77D .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C170(1.52)  LDD3419  [1]
BTD
 Probe Info  		C131(1.92)  LDD2102  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 G-361 C170(1.58)  LDD2329  [1]
 LDCM0023  KB03 G-361 C170(1.72)  LDD2746  [1]
 LDCM0024  KB05 SH-4 C170(1.52)  LDD3419  [1]
 LDCM0509  N-(4-bromo-3,5-dimethylphenyl)-2-nitroacetamide MDA-MB-231 C131(1.92)  LDD2102  [2]

References

1 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
2 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761