Details of the Target

General Information of Target

Target ID LDTP09904
Target Name Caspase-10 (CASP10)
Gene Name CASP10
Gene ID 843
Synonyms
MCH4; Caspase-10; CASP-10; EC 3.4.22.63; Apoptotic protease Mch-4; FAS-associated death domain protein interleukin-1B-converting enzyme 2; FLICE2; ICE-like apoptotic protease 4) [Cleaved into: Caspase-10 subunit p23/17; Caspase-10 subunit p12]
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MWNATPSEEPGFNLTLADLDWDASPGNDSLGDELLQLFPAPLLAGVTATCVALFVVGIAG
NLLTMLVVSRFRELRTTTNLYLSSMAFSDLLIFLCMPLDLVRLWQYRPWNFGDLLCKLFQ
FVSESCTYATVLTITALSVERYFAICFPLRAKVVVTKGRVKLVIFVIWAVAFCSAGPIFV
LVGVEHENGTDPWDTNECRPTEFAVRSGLLTVMVWVSSIFFFLPVFCLTVLYSLIGRKLW
RRRRGDAVVGASLRDQNHKQTVKMLAVVVFAFILCWLPFHVGRYLFSKSFEPGSLEIAQI
SQYCNLVSFVLFYLSAAINPILYNIMSKKYRVAVFRLLGFEPFSQRKLSTLKDESSRAWT
ESSINT
Target Type
Patented-recorded
Target Bioclass
Enzyme
Family
Peptidase C14A family
Function
Involved in the activation cascade of caspases responsible for apoptosis execution. Recruited to both Fas- and TNFR-1 receptors in a FADD dependent manner. May participate in the granzyme B apoptotic pathways. Cleaves and activates effector caspases CASP3, CASP4, CASP6, CASP7, CASP8 and CASP9. Hydrolyzes the small- molecule substrates, Tyr-Val-Ala-Asp-|-AMC and Asp-Glu-Val-Asp-|-AMC.; Isoform 7 can enhance NF-kappaB activity but promotes only slight apoptosis.; Isoform C is proteolytically inactive.
TTD ID
T14894
Uniprot ID
Q92851
DrugMap ID
TTX5HEK
Ensemble ID
ENST00000272879.9
HGNC ID
HGNC:1500
ChEMBL ID
CHEMBL5037

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
IPM
 Probe Info  		N.A.  LDD0241  [1]
Johansson_61
 Probe Info  		_(20.00)  LDD1485  [2]
NAIA_5
 Probe Info  		C16(20.00)  LDD2227  [3]
DBIA
 Probe Info  		C97(4.88)  LDD0209  [4]
IA-alkyne
 Probe Info  		C43(0.00); C97(0.00)  LDD0166  [5]
Lodoacetamide azide
 Probe Info  		C97(0.00); C43(0.00)  LDD0037  [6]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0632  CL-Sc Hep-G2 C16(20.00)  LDD2227  [3]
 LDCM0367  CL1 HEK-293T C169(1.21)  LDD1571  [7]
 LDCM0370  CL101 HEK-293T C169(1.09)  LDD1574  [7]
 LDCM0374  CL105 HEK-293T C169(0.92)  LDD1578  [7]
 LDCM0378  CL109 HEK-293T C169(0.96)  LDD1582  [7]
 LDCM0383  CL113 HEK-293T C169(1.00)  LDD1587  [7]
 LDCM0387  CL117 HEK-293T C169(1.11)  LDD1591  [7]
 LDCM0392  CL121 HEK-293T C169(1.23)  LDD1596  [7]
 LDCM0396  CL125 HEK-293T C169(1.16)  LDD1600  [7]
 LDCM0400  CL13 HEK-293T C169(1.43)  LDD1604  [7]
 LDCM0413  CL25 HEK-293T C169(0.97)  LDD1617  [7]
 LDCM0426  CL37 HEK-293T C169(0.97)  LDD1630  [7]
 LDCM0439  CL49 HEK-293T C169(1.01)  LDD1643  [7]
 LDCM0453  CL61 HEK-293T C169(1.09)  LDD1656  [7]
 LDCM0466  CL73 HEK-293T C169(1.20)  LDD1669  [7]
 LDCM0479  CL85 HEK-293T C169(1.09)  LDD1682  [7]
 LDCM0492  CL97 HEK-293T C169(0.87)  LDD1695  [7]
 LDCM0204  EV-97 T cell C16(8.50)  LDD0525  [8]
 LDCM0569  Fragment7 Jurkat _(20.00)  LDD1485  [2]
 LDCM0022  KB02 A3-KAW C97(1.94)  LDD2257  [9]
 LDCM0023  KB03 Jurkat C97(4.88)  LDD0209  [4]
 LDCM0024  KB05 COLO792 C43(2.38)  LDD3310  [9]
 LDCM0131  RA190 MM1.R C16(1.29); C169(1.05)  LDD0304  [10]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 5 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
E3 ubiquitin-protein ligase XIAP (XIAP) IAP family P98170
CASP8 and FADD-like apoptosis regulator (CFLAR) Peptidase C14A family O15519
Caspase-8 (CASP8) Peptidase C14A family Q14790
Serine/threonine-protein kinase RIO3 (RIOK3) RIO-type Ser/Thr kinase family O14730
Receptor-interacting serine/threonine-protein kinase 1 (RIPK1) TKL Ser/Thr protein kinase family Q13546

References

1 Oxidant-Induced Bioconjugation for Protein Labeling in Live Cells. ACS Chem Biol. 2023 Jan 20;18(1):112-122. doi: 10.1021/acschembio.2c00740. Epub 2022 Dec 21.
2 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.
3 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
4 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.
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 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
7 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
8 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.
9 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
10 Physical and Functional Analysis of the Putative Rpn13 Inhibitor RA190. Cell Chem Biol. 2020 Nov 19;27(11):1371-1382.e6. doi: 10.1016/j.chembiol.2020.08.007. Epub 2020 Aug 27.