Design Principles for Fragment Libraries: Maximizing the Value of Learnings from Pharma Fragment-Based Drug Discovery (FBDD) Programs for Use in Academia
Keserű, György M, Erlanson, Daniel A, Ferenczy, György G, Hann, Michael M, Murray, Christopher W, Pickett, Stephen D
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Published in Journal of medicinal chemistry (22.09.2016)
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Vinylation of α‑Aminoazoles with Triethylamine: A General Strategy to Construct Azolo[1,5‑a]pyrimidines with a Nonsubstituted Ethylidene Fragment
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Published in Organic letters (02.04.2021)
Published in Organic letters (02.04.2021)
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Direct Targeting Options for STAT3 and STAT5 in Cancer
Orlova, Anna, Wagner, Christina, de Araujo, Elvin D, Bajusz, Dávid, Neubauer, Heidi A, Herling, Marco, Gunning, Patrick T, Keserű, György M, Moriggl, Richard
Published in Cancers (03.12.2019)
Published in Cancers (03.12.2019)
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Benchmark Sets for Binding Hot Spot Identification in Fragment-Based Ligand Discovery
Wakefield, Amanda E, Yueh, Christine, Beglov, Dmitri, Castilho, Marcelo S, Kozakov, Dima, Keserű, György M, Whitty, Adrian, Vajda, Sandor
Published in Journal of chemical information and modeling (28.12.2020)
Published in Journal of chemical information and modeling (28.12.2020)
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Site-Selective Antibody Conjugation with Dibromopyrazines
Szepesi Kovács, Dénes, Pásztor, Bettina, Ábrányi-Balogh, Péter, Petri, László, Imre, Tímea, Simon, József, Tátrai, Enikő, Várady, György, Tóvári, József, Szijj, Peter A., Keserű, György M.
Published in Bioconjugate chemistry (18.09.2024)
Published in Bioconjugate chemistry (18.09.2024)
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Contribution of Noncovalent Recognition and Reactivity to the Optimization of Covalent Inhibitors: A Case Study on KRasG12C
Péczka, Nikolett, Ranđelović, Ivan, Orgován, Zoltán, Csorba, Noémi, Egyed, Attila, Petri, László, Ábrányi-Balogh, Péter, Gadanecz, Márton, Perczel, András, Tóvári, József, Schlosser, Gitta, Takács, Tamás, Mihalovits, Levente M., Ferenczy, György G., Buday, László, Keserű, György M.
Published in ACS chemical biology (16.08.2024)
Published in ACS chemical biology (16.08.2024)
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Molecular Mechanism of Labelling Functional Cysteines by Heterocyclic Thiones
Mihalovits, Levente M., Kollár, Levente, Bajusz, Dávid, Knez, Damijan, Bozovičar, Krištof, Imre, Tímea, Ferenczy, György G., Gobec, Stanislav, Keserű, György M.
Published in Chemphyschem (02.01.2024)
Published in Chemphyschem (02.01.2024)
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Exploring protein hotspots by optimized fragment pharmacophores
Bajusz, Dávid, Wade, Warren S., Satała, Grzegorz, Bojarski, Andrzej J., Ilaš, Janez, Ebner, Jessica, Grebien, Florian, Papp, Henrietta, Jakab, Ferenc, Douangamath, Alice, Fearon, Daren, von Delft, Frank, Schuller, Marion, Ahel, Ivan, Wakefield, Amanda, Vajda, Sándor, Gerencsér, János, Pallai, Péter, Keserű, György M.
Published in Nature communications (27.05.2021)
Published in Nature communications (27.05.2021)
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Fragment-Based Optimization of Dihydropyrazino-Benzimidazolones as Metabotropic Glutamate Receptor‑2 Positive Allosteric Modulators against Migraine
Szabó, György, Erdélyi, Péter, Kolok, Sándor, Vastag, Mónika, Halász, Attila S, Kis-Varga, Istvánné, Lévay, György I, Béni, Zoltán, Kóti, János, Greiner, István, Keserű, György M
Published in Journal of medicinal chemistry (24.06.2021)
Published in Journal of medicinal chemistry (24.06.2021)
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Novel-Type GABAB PAMs: Structure–Activity Relationship in Light of the Protein Structure
Krámos, Balázs, Hadady, Zsuzsa, Makó, Attila, Szántó, Gábor, Felföldi, Nóra, Magdó, Ildikó, Bobok, Amrita Ágnes, Bata, Imre, Román, Viktor, Visegrády, András, Keserű, György M., Greiner, István, Éles, János
Published in ACS medicinal chemistry letters (14.03.2024)
Published in ACS medicinal chemistry letters (14.03.2024)
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Activation-Free Sulfonyl Fluoride Probes for Fragment Screening
Petri, László, Ábrányi-Balogh, Péter, Csorba, Noémi, Keeley, Aaron, Simon, József, Ranđelović, Ivan, Tóvári, József, Schlosser, Gitta, Szabó, Dániel, Drahos, László, Keserű, György M
Published in Molecules (Basel, Switzerland) (29.03.2023)
Published in Molecules (Basel, Switzerland) (29.03.2023)
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Next-Generation Heterocyclic Electrophiles as Small-Molecule Covalent MurA Inhibitors
Ábrányi-Balogh, Péter, Keeley, Aaron, Ferenczy, György G, Petri, László, Imre, Tímea, Grabrijan, Katarina, Hrast, Martina, Knez, Damijan, Ilaš, Janez, Gobec, Stanislav, Keserű, György M
Published in Pharmaceuticals (Basel, Switzerland) (29.11.2022)
Published in Pharmaceuticals (Basel, Switzerland) (29.11.2022)
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Discovery of Immunoproteasome Inhibitors Using Large-Scale Covalent Virtual Screening
Scarpino, Andrea, Bajusz, Dávid, Proj, Matic, Gobec, Martina, Sosič, Izidor, Gobec, Stanislav, Ferenczy, György G, Keserű, György M
Published in Molecules (Basel, Switzerland) (16.07.2019)
Published in Molecules (Basel, Switzerland) (16.07.2019)
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Novel potent (dihydro)benzofuranyl piperazines as human histamine receptor ligands – Functional characterization and modeling studies on H3 and H4 receptors
Corrêa, Michelle F., Balico-Silva, André L., Kiss, Dóra J., Fernandes, Gustavo A.B., Maraschin, Jhonatan C., Parreiras-e-Silva, Lucas T., Varela, Marina T., Simões, Sarah C., Bouvier, Michel, Keserű, György M., Costa-Neto, Claudio M., Fernandes, João Paulo S.
Published in Bioorganic & medicinal chemistry (15.01.2021)
Published in Bioorganic & medicinal chemistry (15.01.2021)
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Discovery of isatin and 1H-indazol-3-ol derivatives as d-amino acid oxidase (DAAO) inhibitors
Szilágyi, Bence, Kovács, Péter, Ferenczy, György G., Rácz, Anita, Németh, Krisztina, Visy, Júlia, Szabó, Pál, Ilas, Janez, Balogh, György T., Monostory, Katalin, Vincze, István, Tábi, Tamás, Szökő, Éva, Keserű, György M.
Published in Bioorganic & medicinal chemistry (01.05.2018)
Published in Bioorganic & medicinal chemistry (01.05.2018)
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Comparative Evaluation of Covalent Docking Tools
Scarpino, Andrea, Ferenczy, György G, Keserű, György M
Published in Journal of chemical information and modeling (23.07.2018)
Published in Journal of chemical information and modeling (23.07.2018)
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Expanding the medicinal chemistry synthetic toolbox
Boström, Jonas, Brown, Dean G., Young, Robert J., Keserü, György M.
Published in Nature reviews. Drug discovery (01.10.2018)
Published in Nature reviews. Drug discovery (01.10.2018)
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