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Gene and Protein Information | ||||||
Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | - | 377 | 11q22.3 | CASP4 | caspase 4 | |
Mouse | - | 373 | 9 2.46 cM | Casp4 | caspase 4, apoptosis-related cysteine peptidase | |
Rat | - | 373 | 8q11 | Casp4 | caspase 4 |
Previous and Unofficial Names |
TX protease | Casp11 | caspase 11 | ich-3 | ICE(rel)II | ICH-2 | caspase 4, apoptosis-related cysteine peptidase |
Database Links | |
Specialist databases | |
MEROPS | C14.007 (Hs) |
Other databases | |
Alphafold | P49662 (Hs), P70343 (Mm) |
BRENDA | 3.4.22.57 |
ChEMBL Target | CHEMBL2226 (Hs), CHEMBL1075276 (Mm) |
Ensembl Gene | ENSG00000196954 (Hs), ENSMUSG00000033538 (Mm), ENSRNOG00000033697 (Rn) |
Entrez Gene | 837 (Hs), 12363 (Mm), 114555 (Rn) |
Human Protein Atlas | ENSG00000196954 (Hs) |
KEGG Enzyme | 3.4.22.57 |
KEGG Gene | hsa:837 (Hs), mmu:12363 (Mm), rno:114555 (Rn) |
OMIM | 602664 (Hs) |
Pharos | P49662 (Hs) |
RefSeq Nucleotide | NM_001225 (Hs), NM_033306 (Hs), NM_007609 (Mm), NM_053736 (Rn) |
RefSeq Protein | NP_001216 (Hs), NP_150649 (Hs), NP_031635 (Mm), NP_446188 (Rn) |
UniProtKB | P49662 (Hs), P70343 (Mm) |
Wikipedia | CASP4 (Hs) |
Enzyme Reaction | ||||
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Substrates and Reaction Kinetics | ||||||||||||||||||||||||
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Download all structure-activity data for this target as a CSV file
Inhibitors | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Immunopharmacology Comments |
Recognition of cytoplasmic lipopolysaccharide (LPS) by Inflammatory caspases including caspases-4 and -5 leads to pyroptosis and secretion of inflammatory mediators [3-4]. The caspase activation and recruitment domain (CARD) of caspase-4 recognises the lipid A moiety of LPS. Activation of caspase-4 results in pyroptosis, and induction of NLRP3 inflammasome activation which promotes IL-1β and IL-18 maturation and secretion. |
Immuno Process Associations | ||
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1. 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]
2. Lee D, Long SA, Murray JH, Adams JL, Nuttall ME, Nadeau DP, Kikly K, Winkler JD, Sung CM, Ryan MD et al.. (2001) Potent and selective nonpeptide inhibitors of caspases 3 and 7. J Med Chem, 44 (12): 2015-26. [PMID:11384246]
3. Shi J, Gao W, Shao F. (2017) Pyroptosis: Gasdermin-Mediated Programmed Necrotic Cell Death. Trends Biochem Sci, 42 (4): 245-254. [PMID:27932073]
4. 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]
5. 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]
C14: Caspase: Caspase 4. Last modified on 11/02/2019. Accessed on 02/11/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=1620.