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Literature summary for 3.4.22.43 extracted from

  • Pribis, J.P.; Al-Abed, Y.; Yang, H.; Gero, D.; Xu, H.; Montenegro, M.F.; Bauer, E.M.; Kim, S.; Chavan, S.S.; Cai, C.; Li, T.; Szoleczky, P.; Szabo, C.; Tracey, K.J.; Billiar, T.R.
    The HIV protease inhibitor saquinavir inhibits HMGB1-driven inflammation by targeting the interaction of cathepsin V with TLR4/MyD88 (2015), Mol. Med., 21, 749-757 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.22.43

Application

Application Comment Organism
medicine mammalian protease cathepsin V is a therapeutic target to inhibit TLR4-mediated inflammation induced by extracellular high-mobility group box 1 (HMGB1) (disulfide form). HMGB1 (disulfide form), via activation of toll-like receptor 4 (TLR4)-dependent signaling, is a strong driver of pathologic inflammation in both acute and chronic conditions. The mechanism of action involves a direct interaction between cathepsin V with TLR4 and its adaptor protein MyD88 Homo sapiens

Protein Variants

Protein Variants Comment Organism
additional information cathepsin V enzyme knockout by siRNA transfection of THP-1 cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
E-64
-
 Homo sapiens
additional information inhibitor screening, overview Homo sapiens
N-[(1,1-dimethylethoxy)carbonyl]-L-tryptophan-2-[[[2-[(2-ethylphenyl)amino]-2-oxoethyl]thio]carbonyl]hydrazide SID, inhibits the enzyme and also blocks HMGB1-induced TNF-alpha production Homo sapiens
saquinavir SQV, the HIV protease inhibitor Inhibits the interaction between cathepsin V and the TLR4-MyD88 receptor complex, also blocks disulfide HMGB1-induced TLR4 activation Homo sapiens
STO33438 334, a mammalian protease inhibitor, inhibits cathepsin V, also blocks disulfide HMGB1-induced TLR4 activation Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
lysosome
-
 Homo sapiens 5764
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Homo sapiens direct interaction of cathepsin V with TLR4 and its adaptor protein MyD88 ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens O60911
-
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
 Homo sapiens
-
THP-1 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
benzyloxycarbonyl-Leu-Arg-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens benzyloxycarbonyl-Leu-Arg + 7-amino-4-methylcoumarin
-
 ?
additional information direct interaction of cathepsin V with TLR4 and its adaptor protein MyD88 Homo sapiens ?
-
 ?

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
5.5
-
 assay at Homo sapiens

General Information

General Information Comment Organism
physiological function HIV protease inhibitor saquinavir targets the interaction of cathepsin V with TLR4/MyD88 Homo sapiens