General Information of Target

Target ID LDTP07986
Target Name RAS guanyl-releasing protein 2 (RASGRP2)
Gene Name RASGRP2
Gene ID 10235
Synonyms
CDC25L; MCG7; RAS guanyl-releasing protein 2; Calcium and DAG-regulated guanine nucleotide exchange factor I; CalDAG-GEFI; Cdc25-like protein; hCDC25L; F25B3.3 kinase-like protein
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAGTLDLDKGCTVEELLRGCIEAFDDSGKVRDPQLVRMFLMMHPWYIPSSQLAAKLLHIY
QQSRKDNSNSLQVKTCHLVRYWISAFPAEFDLNPELAEQIKELKALLDQEGNRRHSSLID
IDSVPTYKWKRQVTQRNPVGQKKRKMSLLFDHLEPMELAEHLTYLEYRSFCKILFQDYHS
FVTHGCTVDNPVLERFISLFNSVSQWVQLMILSKPTAPQRALVITHFVHVAEKLLQLQNF
NTLMAVVGGLSHSSISRLKETHSHVSPETIKLWEGLTELVTATGNYGNYRRRLAACVGFR
FPILGVHLKDLVALQLALPDWLDPARTRLNGAKMKQLFSILEELAMVTSLRPPVQANPDL
LSLLTVSLDQYQTEDELYQLSLQREPRSKSSPTSPTSCTPPPRPPVLEEWTSAAKPKLDQ
ALVVEHIEKMVESVFRNFDVDGDGHISQEEFQIIRGNFPYLSAFGDLDQNQDGCISREEM
VSYFLRSSSVLGGRMGFVHNFQESNSLRPVACRHCKALILGIYKQGLKCRACGVNCHKQC
KDRLSVECRRRAQSVSLEGSAPSPSPMHSHHHRAFSFSLPRPGRRGSRPPEIREEEVQTV
EDGVFDIHL
Target Bioclass
Other
Family
RASGRP family
Subcellular location
Cytoplasm, cytosol
Function
Functions as a calcium- and DAG-regulated nucleotide exchange factor specifically activating Rap through the exchange of bound GDP for GTP. May also activate other GTPases such as RRAS, RRAS2, NRAS, KRAS but not HRAS. Functions in aggregation of platelets and adhesion of T-lymphocytes and neutrophils probably through inside-out integrin activation. May function in the muscarinic acetylcholine receptor M1/CHRM1 signaling pathway.
Uniprot ID
Q7LDG7
Ensemble ID
ENST00000354024.7
HGNC ID
HGNC:9879

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CAL62 SNV: p.R581H .
CORL88 SNV: p.C398F .
HUPT4 SNV: p.P94L .
KYSE410 Insertion: p.D439Ter .
L428 SNV: p.R508C .
LNCaP clone FGC SNV: p.A245T .
MDAMB453 SNV: p.S563L .
MOLT4 SNV: p.V354L .
NCIH1703 SNV: p.R387L .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 6 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
Johansson_61
 Probe Info 
_(10.57)  LDD1485  [1]
HPAP
 Probe Info 
4.00  LDD0064  [2]
DBIA
 Probe Info 
C296(7.45); C11(19.01); C76(4.10)  LDD0209  [3]
4-Iodoacetamidophenylacetylene
 Probe Info 
N.A.  LDD0038  [4]
IA-alkyne
 Probe Info 
C296(0.00); C20(0.00)  LDD0166  [5]
Lodoacetamide azide
 Probe Info 
C11(0.00); C20(0.00)  LDD0037  [4]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0569  Fragment7 Jurkat _(10.57)  LDD1485  [1]
 LDCM0022  KB02 697 C610(1.21); C73(2.74)  LDD2245  [6]
 LDCM0023  KB03 Jurkat C296(7.45); C11(19.01); C76(4.10)  LDD0209  [3]
 LDCM0024  KB05 MOLM-13 C610(1.23); C76(6.52)  LDD3333  [6]
 LDCM0014  Panhematin hPBMC 4.00  LDD0064  [2]

References

1 Proteome-wide covalent ligand discovery in native biological systems. Nature. 2016 Jun 23;534(7608):570-4. doi: 10.1038/nature18002. Epub 2016 Jun 15.
2 A Chemical Proteomic Map of Heme-Protein Interactions. J Am Chem Soc. 2022 Aug 24;144(33):15013-15019. doi: 10.1021/jacs.2c06104. Epub 2022 Aug 12.
Mass spectrometry data entry: PXD034651
3 Covalent Inhibition by a Natural Product-Inspired Latent Electrophile. J Am Chem Soc. 2023 May 24;145(20):11097-11109. doi: 10.1021/jacs.3c00598. Epub 2023 May 15.
4 Enhancing Cysteine Chemoproteomic Coverage through Systematic Assessment of Click Chemistry Product Fragmentation. Anal Chem. 2022 Mar 8;94(9):3800-3810. doi: 10.1021/acs.analchem.1c04402. Epub 2022 Feb 23.
Mass spectrometry data entry: PXD028853
5 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060
6 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