Details of the Target

General Information of Target

Target ID LDTP02476
Target Name Granzyme B (GZMB)
Gene Name GZMB
Gene ID 3002
Synonyms
CGL1; CSPB; CTLA1; GRB; Granzyme B; EC 3.4.21.79; C11; CTLA-1; Cathepsin G-like 1; CTSGL1; Cytotoxic T-lymphocyte proteinase 2; Lymphocyte protease; Fragmentin-2; Granzyme-2; Human lymphocyte protein; HLP; SECT; T-cell serine protease 1-3E
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MQPILLLLAFLLLPRADAGEIIGGHEAKPHSRPYMAYLMIWDQKSLKRCGGFLIRDDFVL
TAAHCWGSSINVTLGAHNIKEQEPTQQFIPVKRPIPHPAYNPKNFSNDIMLLQLERKAKR
TRAVQPLRLPSNKAQVKPGQTCSVAGWGQTAPLGKHSHTLQEVKMTVQEDRKCESDLRHY
YDSTIELCVGDPEIKKTSFKGDSGGPLVCNKVAQGIVSYGRNNGMPPRACTKVSSFVHWI
KKTMKRY
Target Type
Literature-reported
Target Bioclass
Enzyme
Family
Peptidase S1 family, Granzyme subfamily
Subcellular location
Secreted
Function
Abundant protease in the cytosolic granules of cytotoxic T-cells and NK-cells which activates caspase-independent pyroptosis when delivered into the target cell through the immunological synapse. It cleaves after Asp. Once delivered into the target cell, acts by catalyzing cleavage of gasdermin-E (GSDME), releasing the pore-forming moiety of GSDME, thereby triggering pyroptosis and target cell death. Seems to be linked to an activation cascade of caspases (aspartate-specific cysteine proteases) responsible for apoptosis execution. Cleaves caspase-3, -9 and -10 (CASP3, CASP9 and CASP10, respectively) to give rise to active enzymes mediating apoptosis. Cleaves and activates CASP7 in response to bacterial infection, promoting plasma membrane repair.
TTD ID
T08298
Uniprot ID
P10144
DrugMap ID
TTKEPHX
Ensemble ID
ENST00000216341.9
HGNC ID
HGNC:4709
ChEMBL ID
CHEMBL2316

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C209(2.75)  LDD2412  [1]
IA-alkyne
 Probe Info  		C142(8.21); C209(5.39)  LDD1704  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 T cell-activated C142(8.21); C209(5.39)  LDD1704  [2]
 LDCM0023  KB03 Karpas-299 C209(4.46)  LDD2829  [1]
 LDCM0024  KB05 T cell-activated C142(17.96); C173(8.98); C209(10.35); C188(5.04)  LDD1706  [2]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Perforin-1 (PRF1) Complement C6/C7/C8/C9 family P14222
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Serglycin (SRGN) Serglycin family P10124

The Drug(s) Related To This Target

Investigative
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pmid12127536c20 Small molecular drug D0Y7HC
Vda-1124 . D06UZS

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 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.