Details of the Target

General Information of Target

Target ID LDTP02295
Target Name Integrin alpha-5 (ITGA5)
Gene Name ITGA5
Gene ID 3678
Synonyms
FNRA; Integrin alpha-5; CD49 antigen-like family member E; Fibronectin receptor subunit alpha; Integrin alpha-F; VLA-5; CD antigen CD49e) [Cleaved into: Integrin alpha-5 heavy chain; Integrin alpha-5 light chain]
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MGSRTPESPLHAVQLRWGPRRRPPLLPLLLLLLPPPPRVGGFNLDAEAPAVLSGPPGSFF
GFSVEFYRPGTDGVSVLVGAPKANTSQPGVLQGGAVYLCPWGASPTQCTPIEFDSKGSRL
LESSLSSSEGEEPVEYKSLQWFGATVRAHGSSILACAPLYSWRTEKEPLSDPVGTCYLST
DNFTRILEYAPCRSDFSWAAGQGYCQGGFSAEFTKTGRVVLGGPGSYFWQGQILSATQEQ
IAESYYPEYLINLVQGQLQTRQASSIYDDSYLGYSVAVGEFSGDDTEDFVAGVPKGNLTY
GYVTILNGSDIRSLYNFSGEQMASYFGYAVAATDVNGDGLDDLLVGAPLLMDRTPDGRPQ
EVGRVYVYLQHPAGIEPTPTLTLTGHDEFGRFGSSLTPLGDLDQDGYNDVAIGAPFGGET
QQGVVFVFPGGPGGLGSKPSQVLQPLWAASHTPDFFGSALRGGRDLDGNGYPDLIVGSFG
VDKAVVYRGRPIVSASASLTIFPAMFNPEERSCSLEGNPVACINLSFCLNASGKHVADSI
GFTVELQLDWQKQKGGVRRALFLASRQATLTQTLLIQNGAREDCREMKIYLRNESEFRDK
LSPIHIALNFSLDPQAPVDSHGLRPALHYQSKSRIEDKAQILLDCGEDNICVPDLQLEVF
GEQNHVYLGDKNALNLTFHAQNVGEGGAYEAELRVTAPPEAEYSGLVRHPGNFSSLSCDY
FAVNQSRLLVCDLGNPMKAGASLWGGLRFTVPHLRDTKKTIQFDFQILSKNLNNSQSDVV
SFRLSVEAQAQVTLNGVSKPEAVLFPVSDWHPRDQPQKEEDLGPAVHHVYELINQGPSSI
SQGVLELSCPQALEGQQLLYVTRVTGLNCTTNHPINPKGLELDPEGSLHHQQKREAPSRS
SASSGPQILKCPEAECFRLRCELGPLHQQESQSLQLHFRVWAKTFLQREHQPFSLQCEAV
YKALKMPYRILPRQLPQKERQVATAVQWTKAEGSYGVPLWIIILAILFGLLLLGLLIYIL
YKLGFFKRSLPYGTAMEKAQLKPPATSDA
Target Type
Clinical trial
Target Bioclass
Transporter and channel
Family
Integrin alpha chain family
Subcellular location
Membrane
Function
Integrin alpha-5/beta-1 (ITGA5:ITGB1) is a receptor for fibronectin and fibrinogen. It recognizes the sequence R-G-D in its ligands. ITGA5:ITGB1 binds to PLA2G2A via a site (site 2) which is distinct from the classical ligand-binding site (site 1) and this induces integrin conformational changes and enhanced ligand binding to site 1. ITGA5:ITGB1 acts as a receptor for fibrillin-1 (FBN1) and mediates R-G-D-dependent cell adhesion to FBN1. ITGA5:ITGB1 acts as a receptor for fibronectin (FN1) and mediates R-G-D-dependent cell adhesion to FN1. ITGA5:ITGB1 is a receptor for IL1B and binding is essential for IL1B signaling. ITGA5:ITGB3 is a receptor for soluble CD40LG and is required for CD40/CD40LG signaling.; (Microbial infection) Integrin ITGA5:ITGB1 acts as a receptor for Human metapneumovirus.; (Microbial infection) Integrin ITGA2:ITGB1 acts as a receptor for Human parvovirus B19.; (Microbial infection) In case of HIV-1 infection, the interaction with extracellular viral Tat protein seems to enhance angiogenesis in Kaposi's sarcoma lesions.
TTD ID
T29879
Uniprot ID
P08648
DrugMap ID
TTHIZP9
Ensemble ID
ENST00000293379.9
HGNC ID
HGNC:6141
ChEMBL ID
CHEMBL3955

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 13 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
FBPP2
 Probe Info  		5.53  LDD0324  [1]
STPyne
 Probe Info  		K943(10.00)  LDD0277  [2]
OPA-S-S-alkyne
 Probe Info  		K965(0.71); K588(1.72); K943(2.54); K910(3.88)  LDD3494  [3]
DBIA
 Probe Info  		C192(3.55); C731(2.99)  LDD3310  [4]
BTD
 Probe Info  		C192(0.99)  LDD2109  [5]
Acrolein
 Probe Info  		C156(0.00); C731(0.00); C192(0.00)  LDD0222  [6]
m-APA
 Probe Info  		N.A.  LDD2231  [7]
4-Iodoacetamidophenylacetylene
 Probe Info  		C192(0.00); C731(0.00)  LDD0038  [8]
IA-alkyne
 Probe Info  		C731(0.00); C156(0.00)  LDD0036  [8]
Lodoacetamide azide
 Probe Info  		C156(0.00); C192(0.00); C731(0.00)  LDD0037  [8]
NAIA_4
 Probe Info  		N.A.  LDD2226  [9]
TFBX
 Probe Info  		N.A.  LDD0148  [10]
NAIA_5
 Probe Info  		C156(0.00); C921(0.00)  LDD2223  [9]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C192(1.32)  LDD2117  [5]
 LDCM0558  2-Cyano-N-phenylacetamide MDA-MB-231 C192(1.42)  LDD2152  [5]
 LDCM0215  AC10 HEK-293T C911(1.05)  LDD1508  [11]
 LDCM0270  AC15 HEK-293T C911(1.25)  LDD1513  [11]
 LDCM0277  AC18 HEK-293T C911(0.90)  LDD1516  [11]
 LDCM0279  AC2 HEK-293T C911(1.13)  LDD1518  [11]
 LDCM0281  AC21 HEK-293T C911(1.08)  LDD1520  [11]
 LDCM0283  AC23 HEK-293T C911(1.32)  LDD1522  [11]
 LDCM0286  AC26 HEK-293T C911(1.17)  LDD1525  [11]
 LDCM0289  AC29 HEK-293T C911(1.27)  LDD1528  [11]
 LDCM0292  AC31 HEK-293T C911(1.31)  LDD1531  [11]
 LDCM0295  AC34 HEK-293T C911(1.30)  LDD1534  [11]
 LDCM0298  AC37 HEK-293T C911(1.31)  LDD1537  [11]
 LDCM0300  AC39 HEK-293T C911(1.10)  LDD1539  [11]
 LDCM0304  AC42 HEK-293T C911(1.10)  LDD1543  [11]
 LDCM0307  AC45 HEK-293T C911(1.12)  LDD1546  [11]
 LDCM0309  AC47 HEK-293T C911(1.08)  LDD1548  [11]
 LDCM0312  AC5 HEK-293T C911(1.17)  LDD1551  [11]
 LDCM0313  AC50 HEK-293T C911(1.13)  LDD1552  [11]
 LDCM0316  AC53 HEK-293T C911(0.98)  LDD1555  [11]
 LDCM0318  AC55 HEK-293T C911(1.15)  LDD1557  [11]
 LDCM0321  AC58 HEK-293T C911(0.97)  LDD1560  [11]
 LDCM0325  AC61 HEK-293T C911(1.14)  LDD1564  [11]
 LDCM0327  AC63 HEK-293T C911(1.09)  LDD1566  [11]
 LDCM0334  AC7 HEK-293T C911(1.07)  LDD1568  [11]
 LDCM0248  AKOS034007472 HEK-293T C911(1.06)  LDD1511  [11]
 LDCM0020  ARS-1620 HCC44 C192(1.06)  LDD2171  [12]
 LDCM0108  Chloroacetamide HeLa C156(0.00); C731(0.00); C192(0.00)  LDD0222  [6]
 LDCM0369  CL100 HEK-293T C911(1.05)  LDD1573  [11]
 LDCM0372  CL103 HEK-293T C911(0.94)  LDD1576  [11]
 LDCM0373  CL104 HEK-293T C911(1.18)  LDD1577  [11]
 LDCM0376  CL107 HEK-293T C911(0.95)  LDD1580  [11]
 LDCM0377  CL108 HEK-293T C911(1.36)  LDD1581  [11]
 LDCM0379  CL11 HEK-293T C911(1.13)  LDD1583  [11]
 LDCM0381  CL111 HEK-293T C911(0.90)  LDD1585  [11]
 LDCM0382  CL112 HEK-293T C911(1.31)  LDD1586  [11]
 LDCM0385  CL115 HEK-293T C911(0.89)  LDD1589  [11]
 LDCM0386  CL116 HEK-293T C911(1.01)  LDD1590  [11]
 LDCM0389  CL119 HEK-293T C911(1.22)  LDD1593  [11]
 LDCM0391  CL120 HEK-293T C911(1.05)  LDD1595  [11]
 LDCM0394  CL123 HEK-293T C911(0.84)  LDD1598  [11]
 LDCM0395  CL124 HEK-293T C911(1.07)  LDD1599  [11]
 LDCM0398  CL127 HEK-293T C911(0.88)  LDD1602  [11]
 LDCM0399  CL128 HEK-293T C911(1.07)  LDD1603  [11]
 LDCM0402  CL15 HEK-293T C911(0.86)  LDD1606  [11]
 LDCM0403  CL16 HEK-293T C911(0.97)  LDD1607  [11]
 LDCM0405  CL18 HEK-293T C911(0.97)  LDD1609  [11]
 LDCM0409  CL21 HEK-293T C911(1.16)  LDD1613  [11]
 LDCM0411  CL23 HEK-293T C911(1.22)  LDD1615  [11]
 LDCM0415  CL27 HEK-293T C911(0.97)  LDD1619  [11]
 LDCM0416  CL28 HEK-293T C911(1.15)  LDD1620  [11]
 LDCM0418  CL3 HEK-293T C911(0.89)  LDD1622  [11]
 LDCM0419  CL30 HEK-293T C911(1.05)  LDD1623  [11]
 LDCM0422  CL33 HEK-293T C911(1.22)  LDD1626  [11]
 LDCM0424  CL35 HEK-293T C911(1.35)  LDD1628  [11]
 LDCM0428  CL39 HEK-293T C911(0.88)  LDD1632  [11]
 LDCM0429  CL4 HEK-293T C911(1.25)  LDD1633  [11]
 LDCM0430  CL40 HEK-293T C911(1.28)  LDD1634  [11]
 LDCM0432  CL42 HEK-293T C911(1.15)  LDD1636  [11]
 LDCM0435  CL45 HEK-293T C911(1.12)  LDD1639  [11]
 LDCM0437  CL47 HEK-293T C911(1.40)  LDD1641  [11]
 LDCM0443  CL52 HEK-293T C911(1.14)  LDD1646  [11]
 LDCM0445  CL54 HEK-293T C911(1.21)  LDD1648  [11]
 LDCM0448  CL57 HEK-293T C911(1.51)  LDD1651  [11]
 LDCM0450  CL59 HEK-293T C911(1.38)  LDD1653  [11]
 LDCM0451  CL6 HEK-293T C911(0.95)  LDD1654  [11]
 LDCM0455  CL63 HEK-293T C911(1.15)  LDD1658  [11]
 LDCM0456  CL64 HEK-293T C911(1.05)  LDD1659  [11]
 LDCM0458  CL66 HEK-293T C911(1.51)  LDD1661  [11]
 LDCM0461  CL69 HEK-293T C911(1.28)  LDD1664  [11]
 LDCM0464  CL71 HEK-293T C911(1.38)  LDD1667  [11]
 LDCM0469  CL76 HEK-293T C911(1.12)  LDD1672  [11]
 LDCM0471  CL78 HEK-293T C911(1.07)  LDD1674  [11]
 LDCM0475  CL81 HEK-293T C911(1.14)  LDD1678  [11]
 LDCM0477  CL83 HEK-293T C911(1.23)  LDD1680  [11]
 LDCM0481  CL87 HEK-293T C911(0.95)  LDD1684  [11]
 LDCM0482  CL88 HEK-293T C911(1.03)  LDD1685  [11]
 LDCM0484  CL9 HEK-293T C911(1.34)  LDD1687  [11]
 LDCM0485  CL90 HEK-293T C911(1.13)  LDD1688  [11]
 LDCM0488  CL93 HEK-293T C911(1.49)  LDD1691  [11]
 LDCM0490  CL95 HEK-293T C911(0.95)  LDD1693  [11]
 LDCM0494  CL99 HEK-293T C911(0.83)  LDD1697  [11]
 LDCM0495  E2913 HEK-293T C911(0.85)  LDD1698  [11]
 LDCM0468  Fragment33 HEK-293T C911(0.85)  LDD1671  [11]
 LDCM0022  KB02 T cell-activated C205(15.82)  LDD1704  [13]
 LDCM0023  KB03 42-MG-BA C192(1.95)  LDD2661  [4]
 LDCM0024  KB05 COLO792 C192(3.55); C731(2.99)  LDD3310  [4]
 LDCM0109  NEM HeLa N.A.  LDD0223  [6]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C192(0.99)  LDD2109  [5]
 LDCM0526  Nucleophilic fragment 26a MDA-MB-231 C192(1.06)  LDD2119  [5]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C192(1.11)  LDD2125  [5]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C192(1.40)  LDD2136  [5]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C192(1.08)  LDD2137  [5]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C192(1.32)  LDD2140  [5]
 LDCM0021  THZ1 HCT 116 C192(1.06)  LDD2173  [12]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Transporter and channel
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Integrin beta-1 (ITGB1) Integrin beta chain family P05556
Neuropilin-1 (NRP1) Neuropilin family O14786
Cytokine and receptor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Endoglin (ENG) . P17813
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Sharpin (SHARPIN) . Q9H0F6

The Drug(s) Related To This Target

Approved
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Tauroursodeoxycholic Acid Small molecular drug DB08834
Phase 1
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Jsm 6427 . D0ZT4J
Investigative
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
C(-grgdfl-) Small molecular drug D0B4JU
Resveratrol Small molecular drug DB02709
Discontinued
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Dw-908e . D0I5PM
Gw-559090 . D0F9QP
Tr-14531 . D01VSK
Zd-7349 . D03EIC

References

1 Tranylcypromine specificity for monoamine oxidase is limited by promiscuous protein labelling and lysosomal trapping. RSC Chem Biol. 2020 Aug 12;1(4):209-213. doi: 10.1039/d0cb00048e. eCollection 2020 Oct 1.
Mass spectrometry data entry: PXD018580
2 A Paal-Knorr agent for chemoproteomic profiling of targets of isoketals in cells. Chem Sci. 2021 Oct 15;12(43):14557-14563. doi: 10.1039/d1sc02230j. eCollection 2021 Nov 10.
Mass spectrometry data entry: PXD028270
3 A chemical proteomics approach for global mapping of functional lysines on cell surface of living cell. Nat Commun. 2024 Apr 8;15(1):2997. doi: 10.1038/s41467-024-47033-w.
Mass spectrometry data entry: PXD042888
4 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
5 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
6 ACR-Based Probe for the Quantitative Profiling of Histidine Reactivity in the Human Proteome. J Am Chem Soc. 2023 Mar 8;145(9):5252-5260. doi: 10.1021/jacs.2c12653. Epub 2023 Feb 27.
7 Global profiling of functional histidines in live cells using small-molecule photosensitizer and chemical probe relay labelling. Nat Chem. 2024 Jun 4. doi: 10.1038/s41557-024-01545-6. Online ahead of print.
Mass spectrometry data entry: PXD042377
8 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
9 N-Acryloylindole-alkyne (NAIA) enables imaging and profiling new ligandable cysteines and oxidized thiols by chemoproteomics. Nat Commun. 2023 Jun 15;14(1):3564. doi: 10.1038/s41467-023-39268-w.
Mass spectrometry data entry: PXD041264
10 Chemoproteomic Profiling by Cysteine Fluoroalkylation Reveals Myrocin G as an Inhibitor of the Nonhomologous End Joining DNA Repair Pathway. J Am Chem Soc. 2021 Dec 8;143(48):20332-20342. doi: 10.1021/jacs.1c09724. Epub 2021 Nov 24.
Mass spectrometry data entry: PXD029255
11 Accelerating multiplexed profiling of protein-ligand interactions: High-throughput plate-based reactive cysteine profiling with minimal input. Cell Chem Biol. 2024 Mar 21;31(3):565-576.e4. doi: 10.1016/j.chembiol.2023.11.015. Epub 2023 Dec 19.
Mass spectrometry data entry: PXD044402
12 Reimagining high-throughput profiling of reactive cysteines for cell-based screening of large electrophile libraries. Nat Biotechnol. 2021 May;39(5):630-641. doi: 10.1038/s41587-020-00778-3. Epub 2021 Jan 4.
13 An Activity-Guided Map of Electrophile-Cysteine Interactions in Primary Human T Cells. Cell. 2020 Aug 20;182(4):1009-1026.e29. doi: 10.1016/j.cell.2020.07.001. Epub 2020 Jul 29.