Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTB6T7O)

DTT Name	Caspase-9 (CASP9)
Synonyms	MCH6; ICE-like apoptotic protease 6; ICE-LAP6; CASP-9; Apoptotic protease-activating factor 3; Apoptotic protease activating factor 3; Apoptotic protease Mch-6; APAF-3
Gene Name	CASP9
DTT Type	Clinical trial target	[1]
BioChemical Class	Peptidase
UniProt ID	CASP9_HUMAN
TTD ID	T93903
3D Structure	Download 2D Sequence (FASTA) Download 3D Structure (PDB) Download
EC Number	EC 3.4.22.62
Sequence	MDEADRRLLRRCRLRLVEELQVDQLWDALLSRELFRPHMIEDIQRAGSGSRRDQARQLII DLETRGSQALPLFISCLEDTGQDMLASFLRTNRQAAKLSKPTLENLTPVVLRPEIRKPEV LRPETPRPVDIGSGGFGDVGALESLRGNADLAYILSMEPCGHCLIINNVNFCRESGLRTR TGSNIDCEKLRRRFSSLHFMVEVKGDLTAKKMVLALLELAQQDHGALDCCVVVILSHGCQ ASHLQFPGAVYGTDGCPVSVEKIVNIFNGTSCPSLGGKPKLFFIQACGGEQKDHGFEVAS TSPEDESPGSNPEPDATPFQEGLRTFDQLDAISSLPTPSDIFVSYSTFPGFVSWRDPKSG SWYVETLDDIFEQWAHSEDLQSLLLRVANAVSVKGIYKQMPGCFNFLRKKLFFKTS
Function	Binding of caspase-9 to Apaf-1 leads to activation of the protease which then cleaves and activates caspase-3. Promotes DNA damage-induced apoptosis in a ABL1/c-Abl-dependent manner. Proteolytically cleaves poly(ADP-ribose) polymerase (PARP). Involved in the activation cascade of caspases responsible for apoptosis execution.
KEGG Pathway	p53 signaling pathway (hsa04115 ) PI3K-Akt signaling pathway (hsa04151 ) Apoptosis (hsa04210 ) VEGF signaling pathway (hsa04370 ) Thyroid hormone signaling pathway (hsa04919 ) Alzheimer's disease (hsa05010 ) Parkinson's disease (hsa05012 ) Amyotrophic lateral sclerosis (ALS) (hsa05014 ) Huntington's disease (hsa05016 ) Legionellosis (hsa05134 ) Toxoplasmosis (hsa05145 ) Tuberculosis (hsa05152 ) Hepatitis B (hsa05161 ) Influenza A (hsa05164 ) Pathways in cancer (hsa05200 ) Colorectal cancer (hsa05210 ) Pancreatic cancer (hsa05212 ) Endometrial cancer (hsa05213 ) Prostate cancer (hsa05215 ) Small cell lung cancer (hsa05222 ) Non-small cell lung cancer (hsa05223 ) Viral myocarditis (hsa05416 )
Reactome Pathway	SMAC-mediated dissociation of IAP (R-HSA-111464 ) NOD1/2 Signaling Pathway (R-HSA-168638 ) AKT phosphorylates targets in the cytosol (R-HSA-198323 ) Constitutive Signaling by AKT1 E17K in Cancer (R-HSA-5674400 ) SMAC binds to IAPs (R-HSA-111463 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA)

MIA Detail

Jump to Detail Molecular Interaction Atlas of This DTT

1 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
isatin sulfonamide 34	DM21Y8J	Cystic fibrosis	CA25	Clinical trial	[1]
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3 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Glionitrin A	DM98CSW	Solid tumour/cancer	2A00-2F9Z	Investigative	[2]
NVX-207	DMBQRA8	Solid tumour/cancer	2A00-2F9Z	Investigative	[3]
Z-LEHD-fmk	DMEFHQI	Discovery agent	N.A.	Investigative	[4]
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References

1	Potent and selective nonpeptide inhibitors of caspases 3 and 7. J Med Chem. 2001 Jun 7;44(12):2015-26.
2	Glionitrin A, a new diketopiperazine disulfide, activates ATM-ATR-Chk1/2 via 53BP1 phosphorylation in DU145 cells and shows antitumor effect in xenograft model. Biol Pharm Bull. 2014;37(3):378-86.
3	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: 1625).
4	The expression of Smac and XIAP in rat hippocampus following limbic seizure induced by kainic acid injection into amygdaloid nucleus. Sheng Li Xue Bao. 2004 Apr 25;56(2):172-7.