Michael acceptor containing drugs are a novel class of 5‐lipoxygenase inhibitor targeting the surface cysteines C416 and C418
Sign Up to like & getrecommendations! Published in 2017 at "Biochemical Pharmacology"
DOI: 10.1016/j.bcp.2016.11.004
Abstract: Graphical abstract Figure. No Caption available. ABSTRACT Recently, we published that nitro‐fatty acids (NFA) are potent electrophilic molecules which inhibit 5‐lipoxygenase (5‐LO) by interacting catalytically with cysteine residues next to a substrate entry channel. The… read more here.
Keywords: containing drugs; acceptor containing; michael acceptor; acceptor ... See more keywords
Discovery of Michael acceptor containing 1,4-dihydropyridines as first covalent inhibitors of L-/T-type calcium channels.
Sign Up to like & getrecommendations! Published in 2019 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2019.103187
Abstract: 1,4-Dihydropyridines (DHPs) are an important class of blockers targeting different calcium channel subtypes and have great therapeutic value against cardiovascular and neurophysiologic conditions. Here, we present the design of DHP-based hexahydroquinoline derivatives as either selective… read more here.
Keywords: covalent inhibitors; calcium channels; type calcium; michael acceptor ... See more keywords
Glutathione Adduct Patterns of Michael-Acceptor Carbonyls.
Sign Up to like & getrecommendations! Published in 2017 at "Environmental science & technology"
DOI: 10.1021/acs.est.6b04981
Abstract: Glutathione (GSH) has so far been considered to facilitate detoxification of soft organic electrophiles through covalent binding at its cysteine (Cys) thiol group, followed by stepwise catalyzed degradation and eventual elimination along the mercapturic acid… read more here.
Keywords: acceptor carbonyls; adduct; michael acceptor; acceptor ... See more keywords
Mechanism of inhibition of SARS-CoV-2 Mpro by N3 peptidyl Michael acceptor explained by QM/MM simulations and design of new derivatives with tunable chemical reactivity†
Sign Up to like & getrecommendations! Published in 2020 at "Chemical Science"
DOI: 10.1039/d0sc06195f
Abstract: The SARS-CoV-2 main protease (Mpro) is essential for replication of the virus responsible for the COVID-19 pandemic, and one of the main targets for drug design. Here, we simulate the inhibition process of SARS-CoV-2 Mpro… read more here.
Keywords: mechanism; cov mpro; michael acceptor; sars cov ... See more keywords
Improvement of the Chemical Reactivity of Michael Acceptor of Ethacrynic Acid Correlates with Antiproliferative Activities
Sign Up to like & getrecommendations! Published in 2023 at "Molecules"
DOI: 10.3390/molecules28020910
Abstract: The present study aims to report the design, synthesis, and biological activity of new ethacrynic acid (EA) analogs (6–10) obtained by the double modulation of the carboxylic acid moiety and the aromatic ring with the… read more here.
Keywords: reactivity michael; michael acceptor; acid; activity ... See more keywords