Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTKEPHX)

DTT Name Granzyme B (GZMB)
Synonyms Tcell serine protease 13E; SECT; Lymphocyte protease; Human lymphocyte protein; Granzyme2; GZMB; Fragmentin2; Cytotoxic Tlymphocyte proteinase 2; Cathepsin Glike 1; CTSGL1; CTLA1; C11
Gene Name GZMB
DTT Type
Literature-reported target
 [1]
BioChemical Class
Peptidase
UniProt ID
GRAB_HUMAN
TTD ID
T08298
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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EC Number
EC 3.4.21.79
Sequence
MQPILLLLAFLLLPRADAGEIIGGHEAKPHSRPYMAYLMIWDQKSLKRCGGFLIRDDFVL
TAAHCWGSSINVTLGAHNIKEQEPTQQFIPVKRPIPHPAYNPKNFSNDIMLLQLERKAKR
TRAVQPLRLPSNKAQVKPGQTCSVAGWGQTAPLGKHSHTLQEVKMTVQEDRKCESDLRHY
YDSTIELCVGDPEIKKTSFKGDSGGPLVCNKVAQGIVSYGRNNGMPPRACTKVSSFVHWI
KKTMKRY
Function
This enzyme is necessary for target cell lysis in cell- mediated immune responses. It cleaves after Asp. Seems to be linked to an activation cascade of caspases (aspartate-specific cysteine proteases) responsible for apoptosis execution. Cleaves caspase-3, -7, -9and 10 to give rise to active enzymes mediating apoptosis.
KEGG Pathway
Natural killer cell mediated cytotoxicity (hsa04650 )
Type I diabetes mellitus (hsa04940 )
Transcriptional misregulation in cancer (hsa05202 )
Autoimmune thyroid disease (hsa05320 )
Allograft rejection (hsa05330 )
Graft-versus-host disease (hsa05332 )
Reactome Pathway
NOTCH2 intracellular domain regulates transcription (R-HSA-2197563 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
2 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
PMID12127536C20 DMY7W2U Discovery agent N.A. Investigative [2]
VDA-1124 DMN62VE Aortic aneurysm BD50 Investigative [1]
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References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2369).
2 Discovery of potent, selective human granzyme B inhibitors that inhibit CTL mediated apoptosis. Bioorg Med Chem Lett. 2002 Aug 19;12(16):2197-200.