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Št. zadetkov: 3
Fragment-based design of targeted covalent inhibitors
Levente Kollár, Levente M. Mihalovits, Dávid Bajusz, Damijan Knez, József Simon, Blake H. Balcomb, Daren Fearon, Stanislav Gobec, György Keserü M., György Keserü M.
Izvirni znanstveni članek
Oznake: 3CLpro inhibitors;covalent inhibitors;fragment linking;fragment-based drug discovery;
Linking of fragments in neighboring binding sites is one of the optimization strategies in fragment-based drug discovery, where additive or even more substantial bioactivity improvements can be realized. However, such efforts present a considerable challenge when one fragment binds covalently to the ...
Leto: 2026 Vir: Fakulteta za farmacijo (UL FFA)
Fragment-sized and bidentate (immuno)proteasome inhibitors derived from cysteine and threonine targeting warheads
Levente Kollár, Martina Gobec, Matic Proj, Lara Smrdel, Damijan Knez, Tímea Imre, Ágnes Gömöry, László Petri, Stanislav Gobec, Izidor Sosič
Izvirni znanstveni članek
Oznake: immunoproteasome;benzoxazole-2-carbonitriles;bidentate covalent inhibitors;fragments;non-covalent recognition;
Constitutive- and immunoproteasomes are part of the ubiquitin–proteasome system (UPS), which is responsible for the protein homeostasis. Selective inhibition of the immunoproteasome offers opportunities for the treatment of numerous diseases, including inflammation, autoimmune diseases, and hematolo ...
Leto: 2021 Vir: Fakulteta za farmacijo (UL FFA)
Mapping functionally relevant tractable lysines of challenging protein targets by covalent fragment screening
Noémi Csorba, Péter Ábrányi-Balogh, Zoltán Orgován, Tibor Viktor Szalai, György G. Ferenczy, Levente Kollár, Nikolett Péczka, Tímea Imre, József Simon, Martina Hrast, Stanislav Gobec
Izvirni znanstveni članek
Oznake: allosteric sites;covalent fragment;electrophilic warhead;lysine labelling;protein–protein interaction;
Covalent fragment screening has become an established strategy for identifying targetable amino acid residues or viable chemical starting points against challenging protein targets. In recent years, lysine has received growing interest as a nucleophilic residue suitable for covalent labelling. Herei ...
Leto: 2026 Vir: Fakulteta za farmacijo (UL FFA)
Št. zadetkov: 3
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