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Caspase 5

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Target id: 1621

Nomenclature: Caspase 5

Family: C14: Caspase

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 434 11q22.3 CASP5 caspase 5
Previous and Unofficial Names Click here for help
ICH-3 protease | TY protease | ICE(rel)III | caspase 5, apoptosis-related cysteine peptidase
Database Links Click here for help
Specialist databases
MEROPS C14.008 (Hs)
Other databases
Alphafold P51878 (Hs)
BRENDA 3.4.22.58
ChEMBL Target CHEMBL3131 (Hs)
Ensembl Gene ENSG00000137757 (Hs)
Entrez Gene 838 (Hs)
Human Protein Atlas ENSG00000137757 (Hs)
KEGG Enzyme 3.4.22.58
KEGG Gene hsa:838 (Hs)
OMIM 602665 (Hs)
Pharos P51878 (Hs)
RefSeq Nucleotide NM_001136110 (Hs), NM_001136109 (Hs), NM_001136112 (Hs), NM_004347 (Hs)
RefSeq Protein NP_001129581 (Hs), NP_001129584 (Hs), NP_004338 (Hs), NP_001129582 (Hs)
UniProtKB P51878 (Hs)
Wikipedia CASP5 (Hs)
Enzyme Reaction Click here for help
EC Number: 3.4.22.58

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
M826 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.7 pIC50 2
⤷ pIC50 6.7 (IC50 2x10-7 M) [2]
uracil 20 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 5.5 pIC50 1
⤷ pIC50 5.5 (IC50 2.98x10-6 M) [1]
Description: IC50 in a biochemical assay.
Z-WEHD-FMK Peptide Hs Inhibition - - 3
⤷ [3]
Immunopharmacology Comments
Recognition of cytoplasmic lipopolysaccharide (LPS) by Inflammatory caspases including caspases-4 and -5 leads to pyroptosis and secretion of inflammatory mediators [4-5].
Immuno Process Associations
Immuno Process:  Immune regulation
Immuno Process:  Inflammation

References

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1. 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]

2. 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]

3. Naito T, Yokogawa T, Kim HS, Futagami M, Wataya Y, Matsuda A, Fukushima M, Kitade Y, Sasaki T. (2002) Anticancer mechanisms of 1-(3-C-ethynyl-beta-D-ribo-pentofuranosyl) cytosine (ECyd, TAS-106). Nucleic Acids Res Suppl, (2): 241-2. [PMID:12903195]

4. Shi J, Gao W, Shao F. (2017) Pyroptosis: Gasdermin-Mediated Programmed Necrotic Cell Death. Trends Biochem Sci, 42 (4): 245-254. [PMID:27932073]

5. Shi J, Zhao Y, Wang Y, Gao W, Ding J, Li P, Hu L, Shao F. (2014) Inflammatory caspases are innate immune receptors for intracellular LPS. Nature, 514 (7521): 187-92. [PMID:25119034]

How to cite this page

C14: Caspase: Caspase 5. Last modified on 11/02/2019. Accessed on 16/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=1621.