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The Magic of Crystal Structure-Based Inhibitor Optimization: Development of a Butyrylcholinesterase Inhibitor with Picomolar Affinity and in Vivo Activity.
Košak U, Brus B, Knez D, Žakelj S, Trontelj J, Pišlar A, Šink R, Jukič M, Živin M, Podkowa A, Nachon F, Brazzolotto X, Stojan J, Kos J, Coquelle N, Sałat K, Colletier JP, Gobec S. Košak U, et al. J Med Chem. 2018 Jan 11;61(1):119-139. doi: 10.1021/acs.jmedchem.7b01086. Epub 2017 Dec 22. J Med Chem. 2018. PMID: 29227101
Development of an in-vivo active reversible butyrylcholinesterase inhibitor.
Košak U, Brus B, Knez D, Šink R, Žakelj S, Trontelj J, Pišlar A, Šlenc J, Gobec M, Živin M, Tratnjek L, Perše M, Sałat K, Podkowa A, Filipek B, Nachon F, Brazzolotto X, Więckowska A, Malawska B, Stojan J, Raščan IM, Kos J, Coquelle N, Colletier JP, Gobec S. Košak U, et al. Sci Rep. 2016 Dec 21;6:39495. doi: 10.1038/srep39495. Sci Rep. 2016. PMID: 28000737 Free PMC article.
N-alkylpiperidine carbamates as potential anti-Alzheimer's agents.
Košak U, Strašek N, Knez D, Jukič M, Žakelj S, Zahirović A, Pišlar A, Brazzolotto X, Nachon F, Kos J, Gobec S. Košak U, et al. Eur J Med Chem. 2020 Jul 1;197:112282. doi: 10.1016/j.ejmech.2020.112282. Epub 2020 Apr 15. Eur J Med Chem. 2020. PMID: 32380361
Repurposing of 8-Hydroxyquinoline-Based Butyrylcholinesterase and Cathepsin B Ligands as Potent Nonpeptidic Deoxyribonuclease I Inhibitors.
Gajic M, Knez D, Sosič I, Mravljak J, Meden A, Košak U, Leitzbach L, George S, Hofmann B, Zivkovic A, Steinhilber D, Stark H, Gobec S, Smelcerovic A, Anderluh M. Gajic M, et al. Among authors: kosak u. ChemMedChem. 2022 Mar 4;17(5):e202100694. doi: 10.1002/cmdc.202100694. Epub 2022 Feb 3. ChemMedChem. 2022. PMID: 34994078
12 results