Details of the Target

General Information of Target

Target ID LDTP00661
Target Name CASP8 and FADD-like apoptosis regulator (CFLAR)
Gene Name CFLAR
Gene ID 8837
Synonyms
CASH; CASP8AP1; CLARP; MRIT; CASP8 and FADD-like apoptosis regulator; Caspase homolog; CASH; Caspase-eight-related protein; Casper; Caspase-like apoptosis regulatory protein; CLARP; Cellular FLICE-like inhibitory protein; c-FLIP; FADD-like antiapoptotic molecule 1; FLAME-1; Inhibitor of FLICE; I-FLICE; MACH-related inducer of toxicity; MRIT; Usurpin) [Cleaved into: CASP8 and FADD-like apoptosis regulator subunit p43; CASP8 and FADD-like apoptosis regulator subunit p12]
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSAEVIHQVEEALDTDEKEMLLFLCRDVAIDVVPPNVRDLLDILRERGKLSVGDLAELLY
RVRRFDLLKRILKMDRKAVETHLLRNPHLVSDYRVLMAEIGEDLDKSDVSSLIFLMKDYM
GRGKISKEKSFLDLVVELEKLNLVAPDQLDLLEKCLKNIHRIDLKTKIQKYKQSVQGAGT
SYRNVLQAAIQKSLKDPSNNFRLHNGRSKEQRLKEQLGAQQEPVKKSIQESEAFLPQSIP
EERYKMKSKPLGICLIIDCIGNETELLRDTFTSLGYEVQKFLHLSMHGISQILGQFACMP
EHRDYDSFVCVLVSRGGSQSVYGVDQTHSGLPLHHIRRMFMGDSCPYLAGKPKMFFIQNY
VVSEGQLEDSSLLEVDGPAMKNVEFKAQKRGLCTVHREADFFWSLCTADMSLLEQSHSSP
SLYLQCLSQKLRQERKRPLLDLHIELNGYMYDWNSRVSAKEKYYVWLQHTLRKKLILSYT
Target Type
Literature-reported
Target Bioclass
Enzyme
Family
Peptidase C14A family
Function
Apoptosis regulator protein which may function as a crucial link between cell survival and cell death pathways in mammalian cells. Acts as an inhibitor of TNFRSF6 mediated apoptosis. A proteolytic fragment (p43) is likely retained in the death-inducing signaling complex (DISC) thereby blocking further recruitment and processing of caspase-8 at the complex. Full length and shorter isoforms have been shown either to induce apoptosis or to reduce TNFRSF-triggered apoptosis. Lacks enzymatic (caspase) activity.
TTD ID
T14306
Uniprot ID
O15519
DrugMap ID
TTJZQYH
Ensemble ID
ENST00000309955.8
HGNC ID
HGNC:1876
ChEMBL ID
CHEMBL1955713

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
786O SNV: p.M299I .
CHL1 SNV: p.P236L .
FTC133 SNV: p.S320G .
HEC1 SNV: p.K127N .
HT SNV: p.L431P .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 3 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
IPM
 Probe Info  		N.A.  LDD0241  [1]
IA-alkyne
 Probe Info  		C393(5.94)  LDD1703  [2]
Acrolein
 Probe Info  		N.A.  LDD0233  [3]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 T cell C393(5.94)  LDD1703  [2]
 LDCM0109  NEM HeLa N.A.  LDD0233  [3]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Caspase-10 (CASP10) Peptidase C14A family Q92851
Caspase-8 (CASP8) Peptidase C14A family Q14790
Dual specificity mitogen-activated protein kinase kinase 1 (MAP2K1) STE Ser/Thr protein kinase family Q02750
Dual specificity mitogen-activated protein kinase kinase 7 (MAP2K7) STE Ser/Thr protein kinase family O14733
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
TNF receptor-associated factor 1 (TRAF1) . Q13077

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 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.
3 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.