Caspase 3

Target id: 1619

Nomenclature: Caspase 3

Family: C14: Caspase

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

   GtoImmuPdb view: OFF :     Caspase 3 has curated GtoImmuPdb data

Gene and Protein Information
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
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
Specialist databases
MEROPS C14.003 (Hs)
Other databases
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 3.4.22.56
Substrates and Reaction Kinetics
Substrate Sp. Property Value Units Standard property Standard value Assay description Assay conditions Comments Reference
huntingtin Hs - -
retinoblastoma-associated protein Hs - -
caspase 3 Hs - -
ICAD Hs - -
PARP Hs - -
PKCδ Hs - -
pro-caspase 7 Hs - -
Endogenous activators (Human)
Caspase 8, caspase 9, caspase 10, GrB

Download all structure-activity data for this target as a CSV file

Activators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
PAC1 Hs Activation - - 8
[8]
PETCM Hs Activation - - 5
[5]
Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
M826 Hs Inhibition 8.3 pKi 3
pKi 8.3 (Ki 5x10-9 M) [3]
compound 4 [PMID: 12408711] Hs Inhibition 7.3 pKi 2
pKi 7.3 (Ki 5x10-8 M) [2]
AZ10417808 Hs Inhibition 6.6 pKi 9
pKi 6.6 (Ki 2.47x10-7 M) [9]
Ac-DEVD-CHO Hs Inhibition 9.8 pIC50 6
pIC50 9.8 (IC50 1.6x10-10 M) [6]
Z-DEVD-FMK Hs Inhibition - - 1
[1]
Z-DQMD-FMK Hs Inhibition - - 4
[4]
Immunopharmacology Comments
Defective caspase 3 expression in immune effector cells my 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
Immuno Process ID:  6
Comment: 
GO Annotation:  Associated to GO processes
GO Processes:  B cell homeostasis (GO:0001782) IEA
erythrocyte differentiation (GO:0030218) IDA
negative regulation of B cell proliferation (GO:0030889) IEA
T cell homeostasis (GO:0043029) IEA
negative regulation of activated T cell proliferation (GO:0046007) IEA
References: 
Immuno Process:  Immune system development
Immuno Process ID:  8
Comment: 
GO Annotation:  Associated to GO processes
GO Processes:  erythrocyte differentiation (GO:0030218) IDA
platelet formation (GO:0030220) TAS
References: 
Immuno Process:  Cytokine production & signalling
Immuno Process ID:  9
Comment: 
GO Annotation:  Associated to GO processes
GO Processes:  response to tumor necrosis factor (GO:0034612) TAS
References: 
Immuno Process:  T cell (activation)
Immuno Process ID:  4
Comment: 
GO Annotation:  Associated to GO processes, IEA only
GO Processes:  negative regulation of activated T cell proliferation (GO:0046007) IEA
References: 
Immuno Process:  B cell (activation)
Immuno Process ID:  5
Comment: 
GO Annotation:  Associated to GO processes, IEA only
GO Processes:  negative regulation of B cell proliferation (GO:0030889) IEA
References: 
Immuno Process:  Chemotaxis & migration
Immuno Process ID:  10
Comment: 
GO Annotation:  Associated to GO processes, IEA only
GO Processes:  negative regulation of activated T cell proliferation (GO:0046007) IEA
References: 
Immuno Process:  Cellular signalling
Immuno Process ID:  11
Comment: 
GO Annotation:  Associated to GO processes, IEA only
GO Processes:  negative regulation of B cell proliferation (GO:0030889) IEA
negative regulation of activated T cell proliferation (GO:0046007) IEA
References: 
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. Science299 (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 Chem45 (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 19/04/2017. Accessed on 24/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1619.