irreversible inhibition

(redirected from irreversible inhibitor)

irreversible inhibition

the action of an inhibitor such that, once bound to a protein, it cannot dissociate.
References in periodicals archive ?
Verdiperstat is a potential first-in-class, oral, brain-penetrant, irreversible inhibitor of myeloperoxidase, an enzyme that acts as a key driver of pathological oxidative stress and inflammation in the brain.
Verdiperstat is first-in-class, oral, irreversible inhibitor of myeloperoxidase, an enzyme that acts as a key driver of pathological oxidative stress and inflammation in the brain.
Trapoxin, an antitumor cyclic tetrapeptide, is an irreversible inhibitor of mammalian histone deacetylase.
The company added that BLU-554 (CS3008) is an oral, potent highly selective and irreversible inhibitor of FGFR4, with a precise selectivity for FGFR4 that spares the paralog kinases FGFR1, FGFR2 and FGFR3.
Canertinib is an irreversible inhibitor that binds covalently to specific cysteine residues in the ATP-binding pocket such as cysteine 773 of EGFR, cysteine 784 of ErbB2, and cysteine 778 of ErbB4 thereby blocking the ATP-binding site in the kinase domain of ErbB proteins, preventing their kinase activity and downstream signaling, and additionally, it also prevents transmodulation of ErbB2 [7].
Afatinib is a potent irreversible inhibitor of all members of the ERBB family of receptor tyrosine kinases.
The assays were also performed in the presence of the following inhibitors: 1 mM phenylmethylsulfonyl fluoride (PMSF; inhibitor of serine proteases), 5 [micro]M E64 (irreversible inhibitor of cysteine proteases), and 1 [micro]M CA074 (irreversible inhibitor of cathepsin B).
Moreover, thapsigargin, a specific irreversible inhibitor of ER calcium-ATPase, has been used to investigate the effect of a disturbed endoplasmic reticulum (ER) calcium homeostasis on different processes of cells, including cytoskeleton dynamics.
E-64 isolated from cultures of Aspergillus japonicus is a very strong and irreversible inhibitor of cysteine proteases [30, 31].
Steroidal sulfamate-based inhibitors Initial search for STS inhibitors centred around trying to modify the structure of E1S to create analogues, ajustified approach as E1S is the substrate for STS.23 The first breakthrough in the design process came when the sulfate group of E1S was replaced by a sulfamate moiety (- OSO2NH2), creating the compound estrone 3-O- sulfamate (EMATE) in 1998.23 EMATE (Figure-2), was found to be an irreversible inhibitor, inhibiting STS in a time- and concentration-dependent fashion.
Neratinib is an oral, irreversible inhibitor of HER1, HER2 and HER4.