Target General Infomation
Target ID
T93903
Former ID
TTDR01006
Target Name
Caspase-9
Gene Name
CASP9
Synonyms
APAF-3; Apoptotic protease Mch-6; Apoptotic protease activating factor 3; CASP-9; ICE-LAP6; ICE-like apoptotic protease 6; CASP9
Target Type
Clinical Trial
Disease Cancer [ICD9: 140-229; ICD10: C00-C96]
Cystic fibrosis [ICD9: 277; ICD10: E84]
Function
Involved in the activation cascade of caspases responsible for apoptosis execution. Binding of caspase-9 to apaf- 1 leads to activation of the protease which then cleaves and activates caspase-3. Proteolytically cleaves poly(adp-ribose) polymerase (parp).
BioChemical Class
Peptidase
UniProt ID
EC Number
EC 3.4.22.62
Sequence
MDEADRRLLRRCRLRLVEELQVDQLWDALLSRELFRPHMIEDIQRAGSGSRRDQARQLII
DLETRGSQALPLFISCLEDTGQDMLASFLRTNRQAAKLSKPTLENLTPVVLRPEIRKPEV
LRPETPRPVDIGSGGFGDVGALESLRGNADLAYILSMEPCGHCLIINNVNFCRESGLRTR
TGSNIDCEKLRRRFSSLHFMVEVKGDLTAKKMVLALLELAQQDHGALDCCVVVILSHGCQ
ASHLQFPGAVYGTDGCPVSVEKIVNIFNGTSCPSLGGKPKLFFIQACGGEQKDHGFEVAS
TSPEDESPGSNPEPDATPFQEGLRTFDQLDAISSLPTPSDIFVSYSTFPGFVSWRDPKSG
SWYVETLDDIFEQWAHSEDLQSLLLRVANAVSVKGIYKQMPGCFNFLRKKLFFKTS
Structure
1JXQ; 1NW9; 2AR9; 3D9T; 3V3K; 3YGS; 4RHW
Drugs and Mode of Action
Drug(s) isatin sulfonamide 34 Drug Info Clinical trial Cystic fibrosis [526075], [541652]
Modulator Glionitrin A Drug Info [532688]
NVX-207 Drug Info [543451]
Inhibitor isatin sulfonamide 34 Drug Info [526075]
Z-LEHD-fmk Drug Info [535959]
Pathways
KEGG Pathway p53 signaling pathway
PI3K-Akt signaling pathway
Apoptosis
VEGF signaling pathway
Thyroid hormone signaling pathway
Alzheimer&#039
s disease
Parkinson&#039
Amyotrophic lateral sclerosis (ALS)
Huntington&#039
Legionellosis
Toxoplasmosis
Tuberculosis
Hepatitis B
Influenza A
Pathways in cancer
Colorectal cancer
Pancreatic cancer
Endometrial cancer
Prostate cancer
Small cell lung cancer
Non-small cell lung cancer
Viral myocarditis
NetPath Pathway IL2 Signaling Pathway
FSH Signaling Pathway
TCR Signaling Pathway
PANTHER Pathway Angiogenesis
Apoptosis signaling pathway
FAS signaling pathway
PI3 kinase pathway
VEGF signaling pathway
Pathway Interaction Database p75(NTR)-mediated signaling
Negative effector of Fas and TNF-alpha
Caspase Cascade in Apoptosis
Class I PI3K signaling events mediated by Akt
Reactome SMAC binds to IAPs
caspase complexes
NOD1/2 Signaling Pathway
AKT phosphorylates targets in the cytosol
Constitutive Signaling by AKT1 E17K in Cancer
WikiPathways DNA Damage Response
Apoptosis Modulation by HSP70
FAS pathway and Stress induction of HSP regulation
PIP3 activates AKT signaling
Apoptosis
Amyotrophic lateral sclerosis (ALS)
Integrated Pancreatic Cancer Pathway
Parkinsons Disease Pathway
Corticotropin-releasing hormone
Allograft Rejection
AGE/RAGE pathway
TNF alpha Signaling Pathway
Prostate Cancer
Alzheimers Disease
Integrated Breast Cancer Pathway
Integrated Cancer pathway
Regulation of Apoptosis
Intrinsic Pathway for Apoptosis
Apoptosis Modulation and Signaling
miRNA Regulation of DNA Damage Response
NOD pathway
References
Ref 526075Potent and selective nonpeptide inhibitors of caspases 3 and 7. J Med Chem. 2001 Jun 7;44(12):2015-26.
Ref 541652(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. (Ligand id: 6515).
Ref 526075Potent and selective nonpeptide inhibitors of caspases 3 and 7. J Med Chem. 2001 Jun 7;44(12):2015-26.
Ref 532688Glionitrin 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.
Ref 535959The 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.
Ref 543451(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).

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