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Caspase 3

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Immunopharmacology Ligand target has curated data in GtoImmuPdb

Target id: 1619

Nomenclature: Caspase 3

Family: C14: Caspase

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 277 4q34 CASP3 caspase 3
Mouse - 277 8 B1.1 Casp3 caspase 3
Rat - 277 16q11 Casp3 caspase 3
Previous and Unofficial Names Click here for help
apopain | cysteine protease CPP32 | SCA-1 | SREBP cleavage activity 1 | Caspase 3 apoptosis related cysteine protease (ICE-like cysteine protease) | IRP | Lice | AC-3 | CC3 | mldy | CPP32 | Yama | caspase 3, apoptosis-related cysteine peptidase
Database Links Click here for help
Specialist databases
MEROPS C14.003 (Hs)
Other databases
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction Click here for help
EC Number: 3.4.22.56
Substrates and Reaction Kinetics Click here for help
Substrate Sp. Property Value Units Standard property Standard value Assay description Assay conditions Comments Reference
huntingtin Substrate is endogenous in the given species Hs - -
retinoblastoma-associated protein Substrate is endogenous in the given species Hs - -
caspase 3 Substrate is endogenous in the given species Hs - -
ICAD Substrate is endogenous in the given species Hs - -
PARP Substrate is endogenous in the given species Hs - -
PKCδ Substrate is endogenous in the given species Hs - -
pro-caspase 7 Substrate is endogenous in the given species Hs - -
Endogenous activators (Human)
Caspase 8, caspase 9, caspase 10, GrB

Download all structure-activity data for this target as a CSV file go icon to follow link

Activators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
PAC1 Small molecule or natural product Hs Activation - - 8
[8]
PETCM Small molecule or natural product Hs Activation - - 5
[5]
Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
M826 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.3 pKi 3
pKi 8.3 (Ki 5x10-9 M) [3]
compound 4 [PMID: 12408711] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.3 pKi 2
pKi 7.3 (Ki 5x10-8 M) [2]
AZ10417808 Small molecule or natural product Hs Inhibition 6.6 pKi 9
pKi 6.6 (Ki 2.47x10-7 M) [9]
Ac-DEVD-CHO Small molecule or natural product Hs Inhibition 9.8 pIC50 6
pIC50 9.8 (IC50 1.6x10-10 M) [6]
Z-DEVD-FMK Peptide Hs Inhibition - - 1
[1]
Z-DQMD-FMK Peptide Hs Inhibition - - 4
[4]
Immunopharmacology Comments
Defective caspase 3 expression in immune effector cells may influence susceptibility to Kawasaki disease, an acute vasculitis syndrome affecting small- and medium-sized arteries of infants and children [7].
Immuno Process Associations
Immuno Process:  Immune regulation
GO Annotations:  Associated to 5 GO processes
GO:0030218 erythrocyte differentiation IDA
click arrow to show/hide IEA associations
GO:0001782 B cell homeostasis IEA
GO:0030889 negative regulation of B cell proliferation IEA
GO:0043029 T cell homeostasis IEA
GO:0046007 negative regulation of activated T cell proliferation IEA
Immuno Process:  Immune system development
GO Annotations:  Associated to 2 GO processes
GO:0030218 erythrocyte differentiation IDA
GO:0030220 platelet formation TAS
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 2 GO processes
GO:0019221 cytokine-mediated signaling pathway TAS
GO:0034612 response to tumor necrosis factor TAS
Immuno Process:  T cell (activation)
GO Annotations:  Associated to 1 GO processes, IEA only
click arrow to show/hide IEA associations
GO:0046007 negative regulation of activated T cell proliferation IEA
Immuno Process:  B cell (activation)
GO Annotations:  Associated to 1 GO processes, IEA only
click arrow to show/hide IEA associations
GO:0030889 negative regulation of B cell proliferation IEA
Immuno Process:  Chemotaxis & migration
GO Annotations:  Associated to 1 GO processes, IEA only
click arrow to show/hide IEA associations
GO:0046007 negative regulation of activated T cell proliferation IEA
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 2 GO processes, IEA only
click arrow to show/hide IEA associations
GO:0030889 negative regulation of B cell proliferation IEA
GO:0046007 negative regulation of activated T cell proliferation IEA
Immuno Disease Associations
Disease Name:  Kawasaki disease
Disease Synonyms:  no synonynms
Comment:  Caspase 3 mutations confer susceptibility to KD.
Disease X-refs:  OMIM: 611775
References:  7

References

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1. Brockstedt E, Rickers A, Kostka S, Laubersheimer A, Dörken B, Wittmann-Liebold B, Bommert K, Otto A. (1998) Identification of apoptosis-associated proteins in a human Burkitt lymphoma cell line. Cleavage of heterogeneous nuclear ribonucleoprotein A1 by caspase 3. J. Biol. Chem., 273 (43): 28057-64. [PMID:9774422]

2. Choong IC, Lew W, Lee D, Pham P, Burdett MT, Lam JW, Wiesmann C, Luong TN, Fahr B, DeLano WL et al.. (2002) 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., 45 (23): 5005-22. [PMID:12408711]

3. Han Y, Giroux A, Colucci J, Bayly CI, Mckay DJ, Roy S, Xanthoudakis S, Vaillancourt J, Rasper DM, Tam J et al.. (2005) Novel pyrazinone mono-amides as potent and reversible caspase-3 inhibitors. Bioorg. Med. Chem. Lett., 15 (4): 1173-80. [PMID:15686936]

4. Izban KF, Ergin M, Huang Q, Qin JZ, Martinez RL, Schnitzer B, Ni H, Nickoloff BJ, Alkan S. (2001) Characterization of NF-kappaB expression in Hodgkin's disease: inhibition of constitutively expressed NF-kappaB results in spontaneous caspase-independent apoptosis in Hodgkin and Reed-Sternberg cells. Mod. Pathol., 14 (4): 297-310. [PMID:11301346]

5. Jiang X, Kim HE, Shu H, Zhao Y, Zhang H, Kofron J, Donnelly J, Burns D, Ng SC, Rosenberg S et al.. (2003) Distinctive roles of PHAP proteins and prothymosin-alpha in a death regulatory pathway. Science, 299 (5604): 223-6. [PMID:12522243]

6. Newton AS, Glória PM, Gonçalves LM, dos Santos DJ, Moreira R, Guedes RC, Santos MM. (2010) Synthesis and evaluation of vinyl sulfones as caspase-3 inhibitors. A structure-activity study. Eur J Med Chem, 45 (9): 3858-63. [PMID:20541849]

7. Onouchi Y, Ozaki K, Buns JC, Shimizu C, Hamada H, Honda T, Terai M, Honda A, Takeuchi T, Shibuta S et al.. (2010) Common variants in CASP3 confer susceptibility to Kawasaki disease. Hum. Mol. Genet., 19 (14): 2898-906. [PMID:20423928]

8. Putt KS, Chen GW, Pearson JM, Sandhorst JS, Hoagland MS, Kwon JT, Hwang SK, Jin H, Churchwell MI, Cho MH et al.. (2006) Small-molecule activation of procaspase-3 to caspase-3 as a personalized anticancer strategy. Nat. Chem. Biol., 2 (10): 543-50. [PMID:16936720]

9. Scott CW, Sobotka-Briner C, Wilkins DE, Jacobs RT, Folmer JJ, Frazee WJ, Bhat RV, Ghanekar SV, Aharony D. (2003) Novel small molecule inhibitors of caspase-3 block cellular and biochemical features of apoptosis. J. Pharmacol. Exp. Ther., 304 (1): 433-40. [PMID:12490620]

How to cite this page

C14: Caspase: Caspase 3. Last modified on 25/09/2018. Accessed on 24/10/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1619.