Target Information
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' | |||||
s disease | |||||
Parkinson' | |||||
Amyotrophic lateral sclerosis (ALS) | |||||
Huntington' | |||||
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 526447 | Identification 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 526509 | Distinctive roles of PHAP proteins and prothymosin-alpha in a death regulatory pathway. Science. 2003 Jan 10;299(5604):223-6. | ||||
Ref 527329 | J Med Chem. 2004 Dec 16;47(26):6455-8.Design and synthesis of a potent and selective peptidomimetic inhibitor of caspase-3. | ||||
Ref 527416 | Novel pyrazinone mono-amides as potent and reversible caspase-3 inhibitors. Bioorg Med Chem Lett. 2005 Feb 15;15(4):1173-80. | ||||
Ref 528057 | J 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 528397 | Small-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 530274 | Bioorg 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 530969 | Eur 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 532688 | 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. |
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.