Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T57943
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| Former ID |
TTDR00440
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| Target Name |
Apopain
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| Gene Name |
CASP3
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| Synonyms |
CASP-3; CPP-32; Caspase 3; Caspase-3; Cysteine protease CPP32; SCA-1; SREBP cleavage activity 1; Yama protein; CASP3
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| Target Type |
Research
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| 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.
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| BioChemical Class |
Peptidase
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| Target Validation |
T57943
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| UniProt ID | |||||
| EC Number |
EC 3.4.22.56
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| Sequence |
MENTENSVDSKSIKNLEPKIIHGSESMDSGISLDNSYKMDYPEMGLCIIINNKNFHKSTG
MTSRSGTDVDAANLRETFRNLKYEVRNKNDLTREEIVELMRDVSKEDHSKRSSFVCVLLS HGEEGIIFGTNGPVDLKKITNFFRGDRCRSLTGKPKLFIIQACRGTELDCGIETDSGVDD DMACHKIPVEADFLYAYSTAPGYYSWRNSKDGSWFIQSLCAMLKQYADKLEFMHILTRVN RKVATEFESFSFDATFHAKKQIPCIVSMLTKELYFYH |
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| 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. | ||||
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