WebbThis review summarizes the development of peptidic and peptidomimetic compounds with an electrophilic nitrile 'warhead' as inhibitors of the cysteine cathepsins B, S, L, C, and … Webb13 apr. 2024 · They are designed to covalently bind the catalytically active amino acids through electrophilic groups called warheads. Covalent inhibition has an advantage in terms of pharmacodynamic properties but can also bear toxicity risks due to non-selective off-target protein binding.
Peptidomimetic nitrile warheads as SARS-CoV-2 3CL protease …
Webb15 apr. 2024 · Abstract. In the field of drug discovery, the nitrile group is well represented among drugs and biologically active compounds. It can form both non-covalent and … Webb15 maj 2024 · The irreversible warheads are the β-lactams ( 2, 4, 6), where hydrolysis of the inhibitor from the amino acid residue could potentially happen, but would produce a … locality boa breeders
Covalent narlaprevir- and boceprevir-derived hybrid inhibitors of …
Webb20 aug. 2024 · Some reactive warheads are susceptible to reaction with glutathione (GSH) and so we decided to test if GSH sequesters these nitrile inhibitors. We incubated 18a … Webb15 apr. 2024 · In the field of drug discovery, the nitrile group is well represented among drugs and biologically active compounds. It can form both non-covalent and covalent … WebbThe covalent screen discovered an electrophilic serine warhead that can inhibit LexA proteolysis, reacting with Ser-119 via a nitrile moiety. This research presents a starting point for... indian dietetic association membership