Details of the Target

General Information of Target

Target ID LDTP04484
Target Name Caspase-5 (CASP5)
Gene Name CASP5
Gene ID 838
Synonyms
ICH3; Caspase-5; CASP-5; EC 3.4.22.58; ICE(rel)-III; Protease ICH-3; Protease TY) [Cleaved into: Caspase-5 subunit p20; Caspase-5 subunit p10]
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAEDSGKKKRRKNFEAMFKGILQSGLDNFVINHMLKNNVAGQTSIQTLVPNTDQKSTSVK
KDNHKKKTVKMLEYLGKDVLHGVFNYLAKHDVLTLKEEEKKKYYDTKIEDKALILVDSLR
KNRVAHQMFTQTLLNMDQKITSVKPLLQIEAGPPESAESTNILKLCPREEFLRLCKKNHD
EIYPIKKREDRRRLALIICNTKFDHLPARNGAHYDIVGMKRLLQGLGYTVVDEKNLTARD
MESVLRAFAARPEHKSSDSTFLVLMSHGILEGICGTAHKKKKPDVLLYDTIFQIFNNRNC
LSLKDKPKVIIVQACRGEKHGELWVRDSPASLALISSQSSENLEADSVCKIHEEKDFIAF
CSSTPHNVSWRDRTRGSIFITELITCFQKYSCCCHLMEIFRKVQKSFEVPQAKAQMPTIE
RATLTRDFYLFPGN
Target Type
Patented-recorded
Target Bioclass
Enzyme
Family
Peptidase C14A family
Function
Thiol protease that acts as a mediator of programmed cell death. Initiates pyroptosis, a programmed lytic cell death pathway through cleavage of Gasdermin-D (GSDMD): cleavage releases the N-terminal gasdermin moiety (Gasdermin-D, N-terminal) that binds to membranes and forms pores, triggering pyroptosis. Also mediates cleavage and maturation of IL18. Cleavage of GSDMD and IL18 is not strictly dependent on the consensus cleavage site but depends on an exosite interface on CASP4. During non-canonical inflammasome activation, cuts CGAS and may play a role in the regulation of antiviral innate immune activation.
TTD ID
T89565
Uniprot ID
P51878
DrugMap ID
TTWR48J
Ensemble ID
ENST00000260315.8
HGNC ID
HGNC:1506
ChEMBL ID
CHEMBL3131

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
A673 SNV: p.I114T DBIA    Probe Info 
MEWO SNV: p.D53N DBIA    Probe Info 
ONS76 SNV: p.A208E .
SW480 SNV: p.T364K .
SW620 SNV: p.T364K .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 4 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C328(2.46)  LDD3310  [1]
BTD
 Probe Info  		C300(0.81)  LDD2091  [2]
Acrolein
 Probe Info  		N.A.  LDD0217  [3]
Methacrolein
 Probe Info  		N.A.  LDD0218  [3]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0502  1-(Cyanoacetyl)piperidine MDA-MB-231 C315(0.92); C300(0.79)  LDD2095  [2]
 LDCM0558  2-Cyano-N-phenylacetamide MDA-MB-231 C315(1.37)  LDD2152  [2]
 LDCM0538  4-(Cyanoacetyl)morpholine MDA-MB-231 C315(0.85); C300(0.48)  LDD2131  [2]
 LDCM0498  BS-3668 MDA-MB-231 C300(0.81)  LDD2091  [2]
 LDCM0108  Chloroacetamide HeLa N.A.  LDD0222  [3]
 LDCM0107  IAA HeLa N.A.  LDD0221  [3]
 LDCM0022  KB02 42-MG-BA C328(2.75)  LDD2244  [1]
 LDCM0023  KB03 42-MG-BA C328(2.71)  LDD2661  [1]
 LDCM0024  KB05 COLO792 C328(2.46)  LDD3310  [1]
 LDCM0528  N-(4-bromophenyl)-2-cyano-N-phenylacetamide MDA-MB-231 C315(0.63)  LDD2121  [2]
 LDCM0109  NEM HeLa N.A.  LDD0223  [3]
 LDCM0500  Nucleophilic fragment 13a MDA-MB-231 C315(0.91)  LDD2093  [2]
 LDCM0506  Nucleophilic fragment 16a MDA-MB-231 C315(1.06); C300(1.29)  LDD2099  [2]
 LDCM0508  Nucleophilic fragment 17a MDA-MB-231 C300(0.70)  LDD2101  [2]
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C315(0.90)  LDD2107  [2]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C315(0.40); C300(0.78)  LDD2109  [2]
 LDCM0518  Nucleophilic fragment 22a MDA-MB-231 C315(1.05)  LDD2111  [2]
 LDCM0526  Nucleophilic fragment 26a MDA-MB-231 C300(1.20)  LDD2119  [2]
 LDCM0530  Nucleophilic fragment 28a MDA-MB-231 C300(1.00)  LDD2123  [2]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C300(0.93)  LDD2125  [2]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C300(1.12)  LDD2127  [2]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C315(1.02)  LDD2136  [2]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C315(0.89)  LDD2137  [2]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C300(0.79)  LDD2140  [2]
 LDCM0550  Nucleophilic fragment 5a MDA-MB-231 C315(1.80)  LDD2144  [2]
 LDCM0552  Nucleophilic fragment 6a MDA-MB-231 C315(0.79); C300(0.88)  LDD2146  [2]
 LDCM0554  Nucleophilic fragment 7a MDA-MB-231 C315(0.68); C300(0.39)  LDD2148  [2]
 LDCM0556  Nucleophilic fragment 8a MDA-MB-231 C315(0.39); C300(0.70)  LDD2150  [2]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
M826 Small molecular drug D00YNW

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
2 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
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.