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Št. zadetkov: 4
Discovery of immunoproteasome inhibitors using large-scale covalent virtual screening
Andrea Scarpino, Dávid Bajusz, Matic Proj, Martina Gobec, Izidor Sosič, Stanislav Gobec, György G. Ferenczy, György Keserü M.
Izvirni znanstveni članek
Oznake: immunoproteasome;covalent inhibitor;virtual screening;beta5i selective inhibitor;
Large-scale virtual screening of boronic acid derivatives was performed to identify nonpeptidic covalent inhibitors of the %5i subunit of the immunoproteasome. A hierarchical virtual screening cascade including noncovalent and covalent docking steps was applied to a virtual library of over 104,000 c ...
Leto: 2019 Vir: Fakulteta za farmacijo (UL FFA)
Covalent inhibitors of bacterial peptidoglycan biosynthesis enzyme MurA with chloroacetamide warhead
Katarina Grabrijan, Martina Hrast, Matic Proj, Ana Dolšak, Irena Zdovc, Tímea Imre, László Petri, Péter Ábrányi-Balogh, György Keserü M., Stanislav Gobec
Izvirni znanstveni članek
Oznake: antibakterijska sredstva;UDP-N-acetilglukozamin enolpiruvil transferaza;tiolna reaktivnost;antibacterial agents;UDP-N-Acetylglucosamine enolpyruvyl transferase;thiol reactivity;
MurA (UDP-N-acetylglucosamine enolpyruvyl transferase) catalyzes the first committed step in the cytoplasmic part of peptidoglycan biosynthesis and is a validated target enzyme for antibacterial drug discovery; the inhibitor fosfomycin has been used clinically for decades. Like fosfomycin, most MurA ...
Leto: 2022 Vir: Fakulteta za farmacijo (UL FFA)
Next-generation heterocyclic electrophiles as small-molecule covalent MurA inhibitors
Péter Ábrányi-Balogh, Aaron Keeley, György G. Ferenczy, László Petri, Tímea Imre, Katarina Grabrijan, Martina Hrast, Damijan Knez, Janez Ilaš, Stanislav Gobec, György Keserü M.
Izvirni znanstveni članek
Oznake: kovalentni inhibitor;heterociklični elektrofili;označevanje cisteina;kvaternizacija;MurA;covalent inhibitor;heterocyclic electrophiles;cysteine labelling;quaternization;
Heterocyclic electrophiles as small covalent fragments showed promising inhibitory activity on the antibacterial target MurA (UDP-N-acetylglucosamine 1-carboxyvinyltransferase, EC:2.5.1.7). Here, we report the second generation of heterocyclic electrophiles: the quaternized analogue of the heterocyc ...
Leto: 2022 Vir: Fakulteta za farmacijo (UL FFA)
Bromo-cyclobutenaminones as new covalent UDP-N-acetylglucosamine enolpyruvyl transferase (murA) inhibitors
David J. Hamilton, Péter Ábrányi-Balogh, Aaron Keeley, László Petri, Martina Hrast, Tímea Imre, Maikel Wijtmans, Stanislav Gobec, Iwan J. P. de Esch, György Keserü M.
Izvirni znanstveni članek
Oznake: covalent inhibitor;MurA;cyclobutenaminone;antibacterial;irreversible;
Drug discovery programs against the antibacterial target UDP-N-acetylglucosamine enolpyruvyl transferase (MurA) have already resulted in covalent inhibitors having small three- and five-membered heterocyclic rings. In the current study, the reactivity of four-membered rings was carefully modulated t ...
Leto: 2020 Vir: Fakulteta za farmacijo (UL FFA)
Št. zadetkov: 4
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