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Electrophilic MiniFrags Revealed Unprecedented Binding Sites for Covalent HDAC8 Inhibitors.
Keeley AB, Kopranovic A, Di Lorenzo V, Ábrányi-Balogh P, Jänsch N, Lai LN, Petri L, Orgován Z, Pölöske D, Orlova A, Németh AG, Desczyk C, Imre T, Bajusz D, Moriggl R, Meyer-Almes FJ, Keserü GM. Keeley AB, et al. Among authors: keseru gm. J Med Chem. 2024 Jan 11;67(1):572-585. doi: 10.1021/acs.jmedchem.3c01779. Epub 2023 Dec 19. J Med Chem. 2024. PMID: 38113354 Free PMC article.
4-Aryl-3-arylsulfonyl-quinolines as negative allosteric modulators of metabotropic GluR5 receptors: From HTS hit to development candidate.
Galambos J, Domány G, Nógrádi K, Wágner G, Keserű GM, Bobok A, Kolok S, Mikó-Bakk ML, Vastag M, Sághy K, Kóti J, Szakács Z, Béni Z, Gál K, Szombathelyi Z, Greiner I. Galambos J, et al. Among authors: keseru gm. Bioorg Med Chem Lett. 2016 Feb 15;26(4):1249-52. doi: 10.1016/j.bmcl.2016.01.024. Epub 2016 Jan 11. Bioorg Med Chem Lett. 2016. PMID: 26774652
Discovery and Preclinical Characterization of 3-((4-(4-Chlorophenyl)-7-fluoroquinoline-3-yl)sulfonyl)benzonitrile, a Novel Non-acetylenic Metabotropic Glutamate Receptor 5 (mGluR5) Negative Allosteric Modulator for Psychiatric Indications.
Galambos J, Bielik A, Krasavin M, Orgován Z, Domány G, Nógrádi K, Wágner G, Balogh GT, Béni Z, Kóti J, Szakács Z, Bobok A, Kolok S, Mikó-Bakk ML, Vastag M, Sághy K, Laszy J, Halász AS, Balázs O, Gál K, Greiner I, Szombathelyi Z, Keserű GM. Galambos J, et al. Among authors: keseru gm. J Med Chem. 2017 Mar 23;60(6):2470-2484. doi: 10.1021/acs.jmedchem.6b01858. Epub 2017 Mar 1. J Med Chem. 2017. PMID: 28212015
Discovery of 4-amino-3-arylsulfoquinolines, a novel non-acetylenic chemotype of metabotropic glutamate 5 (mGlu5) receptor negative allosteric modulators.
Galambos J, Bielik A, Wágner G, Domány G, Kóti J, Béni Z, Szigetvári Á, Sánta Z, Orgován Z, Bobok A, Kiss B, Mikó-Bakk ML, Vastag M, Sághy K, Krasavin M, Gál K, Greiner I, Szombathelyi Z, Keserű GM. Galambos J, et al. Among authors: keseru gm. Eur J Med Chem. 2017 Jun 16;133:240-254. doi: 10.1016/j.ejmech.2017.03.071. Epub 2017 Mar 29. Eur J Med Chem. 2017. PMID: 28390229
220 results