Target General Infomation
Target ID
T57943
Former ID
TTDR00440
Target Name
Apopain
Gene Name
CASP3
Synonyms
CASP-3; CPP-32; Caspase 3; Caspase-3; Cysteine protease CPP32; SCA-1; SREBP cleavage activity 1; Yama protein; CASP3
Target Type
Research
Disease Cancer [ICD9: 140-229; ICD10: C00-C96]
Function
Involved in the activation cascade of caspases responsible for apoptosis execution. At the onset of apoptosis it proteolytically cleaves poly(ADP-ribose) polymerase (PARP) at a '216-Asp-|-Gly-217' bond. Cleaves and activates sterol regulatory element binding proteins (SREBPs) between the basic helix-loop- helix leucine zipper domain and the membrane attachment domain. Cleaves and activates caspase-6, -7 and -9. Involved in the cleavage of huntingtin. Triggers cell adhesion in sympathetic neurons through RET cleavage.
BioChemical Class
Peptidase
Target Validation
T57943
UniProt ID
EC Number
EC 3.4.22.56
Sequence
MENTENSVDSKSIKNLEPKIIHGSESMDSGISLDNSYKMDYPEMGLCIIINNKNFHKSTG
MTSRSGTDVDAANLRETFRNLKYEVRNKNDLTREEIVELMRDVSKEDHSKRSSFVCVLLS
HGEEGIIFGTNGPVDLKKITNFFRGDRCRSLTGKPKLFIIQACRGTELDCGIETDSGVDD
DMACHKIPVEADFLYAYSTAPGYYSWRNSKDGSWFIQSLCAMLKQYADKLEFMHILTRVN
RKVATEFESFSFDATFHAKKQIPCIVSMLTKELYFYH
Inhibitor 2-(4-fluoro-benzyl)isoquinoline-1,3,4-trione Drug Info [528057]
2-(4-methoxy-benzyl)isoquinoline-1,3,4-trione Drug Info [528057]
2-allylisoquinoline-1,3,4-trione Drug Info [528057]
2-benzylisoquinoline-1,3,4-trione Drug Info [528057]
2-methylisoquinoline-1,3,4-trione Drug Info [528057]
2-phenethylisoquinoline-1,3,4-trione Drug Info [528057]
5-(azepan-1-ylsulfonyl)indoline-2,3-dione Drug Info [530274]
5-(azetidin-1-ylsulfonyl)indoline-2,3-dione Drug Info [530274]
5-(piperidin-1-ylsulfonyl)indoline-2,3-dione Drug Info [530274]
5-(pyrrolidin-1-ylsulfonyl)indoline-2,3-dione Drug Info [530274]
Ac-Asp-Glu-Val-Asp-CHO Drug Info [527329]
Ac-DEVD-CHO Drug Info [530969]
AZ10417808 Drug Info [535636]
compound 4 Drug Info [526447]
Isoquinoline-1,3,4(2H)-trione Drug Info [528057]
M826 Drug Info [527416]
SJ-8002 Drug Info [543450]
Modulator Glionitrin A Drug Info [532688]
Activator PAC1 Drug Info [528397]
PETCM Drug Info [526509]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway MAPK signaling pathway
p53 signaling pathway
Apoptosis
Natural killer cell mediated cytotoxicity
TNF signaling pathway
Serotonergic synapse
Non-alcoholic fatty liver disease (NAFLD)
Alzheimer&#039
s disease
Parkinson&#039
Amyotrophic lateral sclerosis (ALS)
Huntington&#039
Epithelial cell signaling in Helicobacter pylori infection
Pertussis
Legionellosis
Toxoplasmosis
Amoebiasis
Tuberculosis
Hepatitis B
Herpes simplex infection
Pathways in cancer
Viral carcinogenesis
Proteoglycans in cancer
MicroRNAs in cancer
Colorectal cancer
Viral myocarditis
NetPath Pathway TCR Signaling Pathway
IL2 Signaling Pathway
IL4 Signaling Pathway
PANTHER Pathway Apoptosis signaling pathway
FAS signaling pathway
Huntington disease
CCKR signaling map ST
Pathway Interaction Database LPA receptor mediated events
Calcineurin-regulated NFAT-dependent transcription in lymphocytes
FAS (CD95) signaling pathway
Role of Calcineurin-dependent NFAT signaling in lymphocytes
Posttranslational regulation of adherens junction stability and dissassembly
p75(NTR)-mediated signaling
Negative effector of Fas and TNF-alpha
Caspase Cascade in Apoptosis
Syndecan-2-mediated signaling events
Reactome SMAC binds to IAPs
caspase complexes
Apoptotic cleavage of cellular proteins
Degradation of the extracellular matrix
NADE modulates death signalling
Activation of DNA fragmentation factor
Caspase-mediated cleavage of cytoskeletal proteins
WikiPathways DNA Damage Response
SIDS Susceptibility Pathways
Apoptosis Modulation by HSP70
MAPK Signaling Pathway
Copper homeostasis
FAS pathway and Stress induction of HSP regulation
Signaling by Hippo
Apoptosis
Amyotrophic lateral sclerosis (ALS)
Spinal Cord Injury
BDNF signaling pathway
Integrated Pancreatic Cancer Pathway
Oncostatin M Signaling Pathway
Parkinsons Disease Pathway
Corticotropin-releasing hormone
Allograft Rejection
AGE/RAGE pathway
TNF alpha Signaling Pathway
Prostate Cancer
Alzheimers Disease
TWEAK Signaling Pathway
Integrated Breast Cancer Pathway
Signalling by NGF
Integrated Cancer pathway
Regulation of Apoptosis
Intrinsic Pathway for Apoptosis
Apoptotic execution phase
Apoptosis Modulation and Signaling
miRNA Regulation of DNA Damage Response
References
Ref 526447Identification of potent and selective small-molecule inhibitors of caspase-3 through the use of extended tethering and structure-based drug design. J Med Chem. 2002 Nov 7;45(23):5005-22.
Ref 526509Distinctive roles of PHAP proteins and prothymosin-alpha in a death regulatory pathway. Science. 2003 Jan 10;299(5604):223-6.
Ref 527329J Med Chem. 2004 Dec 16;47(26):6455-8.Design and synthesis of a potent and selective peptidomimetic inhibitor of caspase-3.
Ref 527416Novel pyrazinone mono-amides as potent and reversible caspase-3 inhibitors. Bioorg Med Chem Lett. 2005 Feb 15;15(4):1173-80.
Ref 528057J Med Chem. 2006 Mar 9;49(5):1613-23.Design, synthesis, and biological evaluation of isoquinoline-1,3,4-trione derivatives as potent caspase-3 inhibitors.
Ref 528397Small-molecule activation of procaspase-3 to caspase-3 as a personalized anticancer strategy. Nat Chem Biol. 2006 Oct;2(10):543-50. Epub 2006 Aug 27.
Ref 530274Bioorg Med Chem. 2009 Aug 15;17(16):6040-7. Epub 2009 Jul 7.Design, synthesis, and discovery of novel non-peptide inhibitor of Caspase-3 using ligand based and structure based virtual screening approach.
Ref 530969Eur J Med Chem. 2010 Sep;45(9):3858-63. Epub 2010 May 24.Synthesis and evaluation of vinyl sulfones as caspase-3 inhibitors. A structure-activity study.
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 535636Novel small molecule inhibitors of caspase-3 block cellular and biochemical features of apoptosis. J Pharmacol Exp Ther. 2003 Jan;304(1):433-40.
Ref 543450(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: 1619).

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.