Details of the Target

General Information of Target

Target ID LDTP02277
Target Name Integrin alpha-IIb (ITGA2B)
Gene Name ITGA2B
Gene ID 3674
Synonyms
GP2B; ITGAB; Integrin alpha-IIb; GPalpha IIb; GPIIb; Platelet membrane glycoprotein IIb; CD antigen CD41) [Cleaved into: Integrin alpha-IIb heavy chain; Integrin alpha-IIb light chain, form 1; Integrin alpha-IIb light chain, form 2]
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MARALCPLQALWLLEWVLLLLGPCAAPPAWALNLDPVQLTFYAGPNGSQFGFSLDFHKDS
HGRVAIVVGAPRTLGPSQEETGGVFLCPWRAEGGQCPSLLFDLRDETRNVGSQTLQTFKA
RQGLGASVVSWSDVIVACAPWQHWNVLEKTEEAEKTPVGSCFLAQPESGRRAEYSPCRGN
TLSRIYVENDFSWDKRYCEAGFSSVVTQAGELVLGAPGGYYFLGLLAQAPVADIFSSYRP
GILLWHVSSQSLSFDSSNPEYFDGYWGYSVAVGEFDGDLNTTEYVVGAPTWSWTLGAVEI
LDSYYQRLHRLRGEQMASYFGHSVAVTDVNGDGRHDLLVGAPLYMESRADRKLAEVGRVY
LFLQPRGPHALGAPSLLLTGTQLYGRFGSAIAPLGDLDRDGYNDIAVAAPYGGPSGRGQV
LVFLGQSEGLRSRPSQVLDSPFPTGSAFGFSLRGAVDIDDNGYPDLIVGAYGANQVAVYR
AQPVVKASVQLLVQDSLNPAVKSCVLPQTKTPVSCFNIQMCVGATGHNIPQKLSLNAELQ
LDRQKPRQGRRVLLLGSQQAGTTLNLDLGGKHSPICHTTMAFLRDEADFRDKLSPIVLSL
NVSLPPTEAGMAPAVVLHGDTHVQEQTRIVLDCGEDDVCVPQLQLTASVTGSPLLVGADN
VLELQMDAANEGEGAYEAELAVHLPQGAHYMRALSNVEGFERLICNQKKENETRVVLCEL
GNPMKKNAQIGIAMLVSVGNLEEAGESVSFQLQIRSKNSQNPNSKIVLLDVPVRAEAQVE
LRGNSFPASLVVAAEEGEREQNSLDSWGPKVEHTYELHNNGPGTVNGLHLSIHLPGQSQP
SDLLYILDIQPQGGLQCFPQPPVNPLKVDWGLPIPSPSPIHPAHHKRDRRQIFLPEPEQP
SRLQDPVLVSCDSAPCTVVQCDLQEMARGQRAMVTVLAFLWLPSLYQRPLDQFVLQSHAW
FNVSSLPYAVPPLSLPRGEAQVWTQLLRALEERAIPIWWVLVGVLGGLLLLTILVLAMWK
VGFFKRNRPPLEEDDEEGE
Target Bioclass
Other
Family
Integrin alpha chain family
Subcellular location
Membrane
Function
Integrin alpha-IIb/beta-3 is a receptor for fibronectin, fibrinogen, plasminogen, prothrombin, thrombospondin and vitronectin. It recognizes the sequence R-G-D in a wide array of ligands. It recognizes the sequence H-H-L-G-G-G-A-K-Q-A-G-D-V in fibrinogen gamma chain. Following activation integrin alpha-IIb/beta-3 brings about platelet/platelet interaction through binding of soluble fibrinogen. This step leads to rapid platelet aggregation which physically plugs ruptured endothelial cell surface.
Uniprot ID
P08514
Ensemble ID
ENST00000262407.6
HGNC ID
HGNC:6138
ChEMBL ID
CHEMBL212

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
COLO800 SNV: p.L18V .
HCC1954 SNV: p.Y186Ter .
HCC44 SNV: p.D848Y .
HCT15 SNV: p.E428D; p.E719Ter .
HEC1 SNV: p.T525I .
HEC1B SNV: p.W16L .
HT115 SNV: p.R358C; p.L908I .
J82 SNV: p.L940M .
MCC13 Substitution: p.Q475Ter .
MEWO SNV: p.R351Q .
MOLT4 SNV: p.D636V .
NALM6 SNV: p.R351Q .
NCIH2286 SNV: p.A4P .
NCIH661 SNV: p.V484A .
NCIH82 Deletion: p.L940CfsTer? .
P31FUJ SNV: p.E635Ter .
SKMEL3 SNV: p.G853A .
SKMEL30 SNV: p.P972S; p.G1038R .
TOV21G SNV: p.E1037Ter .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C87(2.12); C161(2.99)  LDD3334  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 CMK C96(3.24); C504(3.43); C87(3.41); C161(2.98)  LDD2302  [1]
 LDCM0023  KB03 CMK C96(3.99); C504(7.73); C87(3.90); C161(4.48)  LDD2719  [1]
 LDCM0024  KB05 MOLM-16 C87(2.12); C161(2.99)  LDD3334  [1]

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