General Information of Target

Target ID LDTP04047
Target Name Tyrosine-protein kinase ZAP-70 (ZAP70)
Gene Name ZAP70
Gene ID 7535
Synonyms
SRK; Tyrosine-protein kinase ZAP-70; EC 2.7.10.2; 70 kDa zeta-chain associated protein; Syk-related tyrosine kinase
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Sequence
MPDPAAHLPFFYGSISRAEAEEHLKLAGMADGLFLLRQCLRSLGGYVLSLVHDVRFHHFP
IERQLNGTYAIAGGKAHCGPAELCEFYSRDPDGLPCNLRKPCNRPSGLEPQPGVFDCLRD
AMVRDYVRQTWKLEGEALEQAIISQAPQVEKLIATTAHERMPWYHSSLTREEAERKLYSG
AQTDGKFLLRPRKEQGTYALSLIYGKTVYHYLISQDKAGKYCIPEGTKFDTLWQLVEYLK
LKADGLIYCLKEACPNSSASNASGAAAPTLPAHPSTLTHPQRRIDTLNSDGYTPEPARIT
SPDKPRPMPMDTSVYESPYSDPEELKDKKLFLKRDNLLIADIELGCGNFGSVRQGVYRMR
KKQIDVAIKVLKQGTEKADTEEMMREAQIMHQLDNPYIVRLIGVCQAEALMLVMEMAGGG
PLHKFLVGKREEIPVSNVAELLHQVSMGMKYLEEKNFVHRDLAARNVLLVNRHYAKISDF
GLSKALGADDSYYTARSAGKWPLKWYAPECINFRKFSSRSDVWSYGVTMWEALSYGQKPY
KKMKGPEVMAFIEQGKRMECPPECPPELYALMSDCWIYKWEDRPDFLTVEQRMRACYYSL
ASKVEGPPGSTQKAEAACA
Target Type
Patented-recorded
Target Bioclass
Enzyme
Family
Protein kinase superfamily, Tyr protein kinase family, SYK/ZAP-70 subfamily
Subcellular location
Cytoplasm
Function
Tyrosine kinase that plays an essential role in regulation of the adaptive immune response. Regulates motility, adhesion and cytokine expression of mature T-cells, as well as thymocyte development. Contributes also to the development and activation of primary B-lymphocytes. When antigen presenting cells (APC) activate T-cell receptor (TCR), a serie of phosphorylations lead to the recruitment of ZAP70 to the doubly phosphorylated TCR component CD247/CD3Z through ITAM motif at the plasma membrane. This recruitment serves to localization to the stimulated TCR and to relieve its autoinhibited conformation. Release of ZAP70 active conformation is further stabilized by phosphorylation mediated by LCK. Subsequently, ZAP70 phosphorylates at least 2 essential adapter proteins: LAT and LCP2. In turn, a large number of signaling molecules are recruited and ultimately lead to lymphokine production, T-cell proliferation and differentiation. Furthermore, ZAP70 controls cytoskeleton modifications, adhesion and mobility of T-lymphocytes, thus ensuring correct delivery of effectors to the APC. ZAP70 is also required for TCR-CD247/CD3Z internalization and degradation through interaction with the E3 ubiquitin-protein ligase CBL and adapter proteins SLA and SLA2. Thus, ZAP70 regulates both T-cell activation switch on and switch off by modulating TCR expression at the T-cell surface. During thymocyte development, ZAP70 promotes survival and cell-cycle progression of developing thymocytes before positive selection (when cells are still CD4/CD8 double negative). Additionally, ZAP70-dependent signaling pathway may also contribute to primary B-cells formation and activation through B-cell receptor (BCR).
TTD ID
T64553
Uniprot ID
P43403
DrugMap ID
TTUMHT8
Ensemble ID
ENST00000264972.10
HGNC ID
HGNC:12858
ChEMBL ID
CHEMBL2803

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
A101D Substitution: p.V470F .
A3KAW SNV: p.R358C .
CCK81 SNV: p.V149A .
HT115 SNV: p.A218V .
IGROV1 SNV: p.V127M .
KYSE510 SNV: p.I577M .
LNCaP clone FGC SNV: p.R353C; p.L371Q .
MEWO SNV: p.G291E .
NCIH1993 SNV: p.H52Q .
NCIH2286 SNV: p.Y474Ter .
NCIH23 SNV: p.S602R .
RL952 SNV: p.L270P .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 10 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
TH211
 Probe Info 
Y164(17.05); Y506(10.38); Y292(5.83)  LDD0260  [1]
STPyne
 Probe Info 
K504(1.02)  LDD2219  [2]
DBIA
 Probe Info 
CAmbiguous(4.71); C346(8.77); C84(4.06); C249(9.48)  LDD0209  [3]
4-Iodoacetamidophenylacetylene
 Probe Info 
C596(0.00); C249(0.00); C346(0.00); C96(0.00)  LDD0038  [4]
IA-alkyne
 Probe Info 
C596(0.00); C249(0.00); C78(0.00); C84(0.00)  LDD0036  [4]
IPIAA_H
 Probe Info 
C96(0.00); C405(0.00); C222(0.00)  LDD0030  [5]
IPIAA_L
 Probe Info 
C102(0.00); C78(0.00); C222(0.00); C405(0.00)  LDD0031  [5]
Lodoacetamide azide
 Probe Info 
C596(0.00); C249(0.00); C346(0.00); C96(0.00)  LDD0037  [4]
Compound 10
 Probe Info 
C117(0.00); C249(0.00); C254(0.00); C510(0.00)  LDD2216  [6]
Compound 11
 Probe Info 
C117(0.00); C254(0.00); C510(0.00); C84(0.00)  LDD2213  [6]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 T cell C346(9.32)  LDD1703  [7]
 LDCM0023  KB03 Jurkat CAmbiguous(4.71); C346(8.77); C84(4.06); C249(9.48)  LDD0209  [3]
 LDCM0024  KB05 MONO-MAC-6 C596(1.69)  LDD3335  [8]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 6 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Hepatocyte growth factor receptor (MET) Tyr protein kinase family P08581
Mast/stem cell growth factor receptor Kit (KIT) Tyr protein kinase family P10721
Epidermal growth factor receptor (EGFR) Tyr protein kinase family P00533
Tyrosine-protein kinase Lck (LCK) Tyr protein kinase family P06239
Tyrosine-protein phosphatase non-receptor type 22 (PTPN22) Protein-tyrosine phosphatase family Q9Y2R2
E3 ubiquitin-protein ligase CBL (CBL) . P22681
Transporter and channel
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
T-cell surface glycoprotein CD3 zeta chain (CD247) CD3Z/FCER1G family P20963
T-cell surface glycoprotein CD3 epsilon chain (CD3E) . P07766

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
Fostamatinib Small molecular drug DB12010
Investigative
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Aloisine Small molecular drug D00SEC
K00592a Small molecular drug D0T4MJ
Staurosporine Small molecular drug DB02010
Patented
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Us8546370, 102 Small molecular drug D00HGD
Us8546370, 11 Small molecular drug D09OGH
Us8546370, 17 Small molecular drug D0VE2A

References

1 Chemoproteomic profiling of kinases in live cells using electrophilic sulfonyl triazole probes. Chem Sci. 2021 Jan 21;12(9):3295-3307. doi: 10.1039/d0sc06623k.
2 Global profiling of lysine reactivity and ligandability in the human proteome. Nat Chem. 2017 Dec;9(12):1181-1190. doi: 10.1038/nchem.2826. Epub 2017 Jul 31.
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-Enabled Rapid and High Coverage Chemoproteomic Identification of Cell-State-Dependent Redox-Sensitive Cysteines. Mol Cell Proteomics. 2022 Apr;21(4):100218. doi: 10.1016/j.mcpro.2022.100218. Epub 2022 Feb 25.
Mass spectrometry data entry: PXD029500 , PXD031647
6 Multiplexed CuAAC Suzuki-Miyaura Labeling for Tandem Activity-Based Chemoproteomic Profiling. Anal Chem. 2021 Feb 2;93(4):2610-2618. doi: 10.1021/acs.analchem.0c04726. Epub 2021 Jan 20.
Mass spectrometry data entry: PXD022279
7 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.
8 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