Top ▲

Caspase 1

Click here for help

Target id: 1617

Nomenclature: Caspase 1

Family: C14: Caspase

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 404 11q22.3 CASP1 caspase 1
Mouse - 402 9 2.46 cM 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
Alphafold P29466 (Hs), P29452 (Mm), P43527 (Rn)
BRENDA 3.4.22.36
ChEMBL Target CHEMBL4801 (Hs), CHEMBL4800 (Mm)
Ensembl Gene ENSG00000137752 (Hs), ENSMUSG00000025888 (Mm), ENSRNOG00000007372 (Rn)
Entrez Gene 834 (Hs), 12362 (Mm), 25166 (Rn)
Human Protein Atlas ENSG00000137752 (Hs)
KEGG Enzyme 3.4.22.36
KEGG Gene hsa:834 (Hs), mmu:12362 (Mm), rno:25166 (Rn)
OMIM 147678 (Hs)
Pharos P29466 (Hs)
RefSeq Nucleotide NM_001223 (Hs), NM_001257119 (Hs), NM_033292 (Hs), NM_033293 (Hs), NM_033294 (Hs), NM_033295 (Hs), NM_001257118 (Hs), NM_009807 (Mm), NM_012762 (Rn)
RefSeq Protein NP_001214 (Hs), NP_001244048 (Hs), NP_150634 (Hs), NP_150635 (Hs), NP_150636 (Hs), NP_150637 (Hs), NP_001244047 (Hs), NP_033937 (Mm), NP_036894 (Rn)
UniProtKB P29466 (Hs), P29452 (Mm), P43527 (Rn)
Wikipedia CASP1 (Hs)
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 Ligand has a PDB structure 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
Immuno Process:  Cytokine production & signalling
Immuno Process:  Immune regulation
Immuno Process:  Cellular signalling

References

Show »

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 11/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=1617.