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Caspase 1

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Immunopharmacology Ligand target has curated data in GtoImmuPdb

Target id: 1617

Nomenclature: Caspase 1

Family: C14: Caspase

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 404 11q23 CASP1 caspase 1
Mouse - 402 9 A1 Casp1 caspase 1
Rat - 402 8q11 Casp1 caspase 1
Previous and Unofficial Names Click here for help
ICE | IL-1 β-converting enzyme | p45 | interleukin 1 beta-converting enzyme | IL1BC | caspase 1, apoptosis-related cysteine peptidase
Database Links Click here for help
Specialist databases
MEROPS C14.001 (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: 3.4.22.36
Substrates and Reaction Kinetics Click here for help
Substrate Sp. Property Value Units Standard property Standard value Assay description Assay conditions Comments Reference
Rho GDP dissociation inhibitor beta Substrate is endogenous in the given species Hs - -
parkin Substrate is endogenous in the given species Hs - -
pro-caspase 4 Substrate is endogenous in the given species Hs - -
pro-interleukin-1β Substrate is endogenous in the given species Hs - -

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

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
VRT-043198 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 9.1 pKi 6
pKi 9.1 (Ki 8x10-10 M) Derived from pro-drug belnacasan [6]
pralnacasan Small molecule or natural product Primary target of this compound Immunopharmacology Ligand Hs Inhibition 9.0 pKi 5
pKi 9.0 (Ki 1x10-9 M) [5]
uracil 20 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 8.0 pIC50 3
pIC50 8.0 (IC50 9.8x10-9 M) [3]
Description: IC50 in a biochemical assay.
M826 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.3 pIC50 4
pIC50 7.3 (IC50 5x10-8 M) [4]
AS101 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition - - 2
[2]
Z-YVAD-FMK Peptide Hs Inhibition - - 1
[1]
Immunopharmacology Comments
Caspase 1 is also known as interleukin-1beta (IL-1α) converting enzyme (ICE). Amongst its substrates are the precursors of the inflammatory cytokines IL-1β and IL-18, which it proteolytically cleaves into active mature peptides.
Immuno Process Associations
Immuno Process:  Inflammation
GO Annotations:  Associated to 3 GO processes
GO:0001774 microglial cell activation ISO
GO:0050727 regulation of inflammatory response IBA
GO:0071346 cellular response to interferon-gamma IMP
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 7 GO processes, IEA only
GO:0019221 cytokine-mediated signaling pathway TAS
GO:0032611 interleukin-1 beta production IGI
GO:0032731 positive regulation of interleukin-1 beta production IMP
GO:0050715 positive regulation of cytokine secretion IMP
GO:0071345 cellular response to cytokine stimulus TAS
GO:0071346 cellular response to interferon-gamma IMP
GO:1903265 positive regulation of tumor necrosis factor-mediated signaling pathway IMP
Immuno Process:  Immune regulation
GO Annotations:  Associated to 1 GO processes
GO:0050727 regulation of inflammatory response IBA
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 1 GO processes
GO:0001774 microglial cell activation ISO

References

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1. Avivi-Green C, Polak-Charcon S, Madar Z, Schwartz B. (2002) Different molecular events account for butyrate-induced apoptosis in two human colon cancer cell lines. J. Nutr., 132 (7): 1812-8. [PMID:12097652]

2. Brodsky M, Yosef S, Galit R, Albeck M, Longo DL, Albeck A, Sredni B. (2007) The synthetic tellurium compound, AS101, is a novel inhibitor of IL-1beta converting enzyme. J. Interferon Cytokine Res., 27 (6): 453-62. [PMID:17572009]

3. Fournier JF, Clary L, Chambon S, Dumais L, Harris CS, Millois C, Pierre R, Talano S, Thoreau É, Aubert J et al.. (2018) Rational Drug Design of Topically Administered Caspase 1 Inhibitors for the Treatment of Inflammatory Acne. J. Med. Chem., 61 (9): 4030-4051. [PMID:29648825]

4. 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]

5. Linton SD. (2005) Caspase inhibitors: a pharmaceutical industry perspective. Curr Top Med Chem, 5 (16): 1697-717. [PMID:16375749]

6. Wannamaker W, Davies R, Namchuk M, Pollard J, Ford P, Ku G, Decker C, Charifson P, Weber P, Germann UA et al.. (2007) (S)-1-((S)-2-{[1-(4-amino-3-chloro-phenyl)-methanoyl]-amino}-3,3-dimethyl-butanoyl)-pyrrolidine-2-carboxylic acid ((2R,3S)-2-ethoxy-5-oxo-tetrahydro-furan-3-yl)-amide (VX-765), an orally available selective interleukin (IL)-converting enzyme/caspase-1 inhibitor, exhibits potent anti-inflammatory activities by inhibiting the release of IL-1beta and IL-18. J. Pharmacol. Exp. Ther., 321 (2): 509-16. [PMID:17289835]

How to cite this page

C14: Caspase: Caspase 1. Last modified on 13/04/2018. Accessed on 24/10/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1617.