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In vitro and in silico analysis of the effects of D2 receptor antagonist target binding kinetics on the cellular response to fluctuating dopamine concentrations.
de Witte WEA, Versfelt JW, Kuzikov M, Rolland S, Georgi V, Gribbon P, Gul S, Huntjens D, van der Graaf PH, Danhof M, Fernández-Montalván A, Witt G, de Lange ECM. de Witte WEA, et al. Br J Pharmacol. 2018 Nov;175(21):4121-4136. doi: 10.1111/bph.14456. Epub 2018 Sep 21. Br J Pharmacol. 2018. PMID: 30051456 Free PMC article.
Characterization of 12 GnRH peptide agonists - a kinetic perspective.
Nederpelt I, Georgi V, Schiele F, Nowak-Reppel K, Fernández-Montalván AE, IJzerman AP, Heitman LH. Nederpelt I, et al. Br J Pharmacol. 2016 Jan;173(1):128-41. doi: 10.1111/bph.13342. Epub 2015 Nov 4. Br J Pharmacol. 2016. PMID: 26398856 Free PMC article.
Binding kinetics in drug discovery - A current perspective.
Georgi V, Andres D, Fernandez-Montalvan AE, Stegmann CM, Becker A, Mueller-Fahrnow A. Georgi V, et al. Front Biosci (Landmark Ed). 2017 Jan 1;22(1):21-47. doi: 10.2741/4470. Front Biosci (Landmark Ed). 2017. PMID: 27814600 Free article. Review.
Halogen-Aromatic π Interactions Modulate Inhibitor Residence Times.
Heroven C, Georgi V, Ganotra GK, Brennan P, Wolfreys F, Wade RC, Fernández-Montalván AE, Chaikuad A, Knapp S. Heroven C, et al. Angew Chem Int Ed Engl. 2018 Jun 11;57(24):7220-7224. doi: 10.1002/anie.201801666. Epub 2018 May 9. Angew Chem Int Ed Engl. 2018. PMID: 29601130 Free PMC article.
Binding Kinetics Survey of the Drugged Kinome.
Georgi V, Schiele F, Berger BT, Steffen A, Marin Zapata PA, Briem H, Menz S, Preusse C, Vasta JD, Robers MB, Brands M, Knapp S, Fernández-Montalván A. Georgi V, et al. J Am Chem Soc. 2018 Nov 21;140(46):15774-15782. doi: 10.1021/jacs.8b08048. Epub 2018 Nov 6. J Am Chem Soc. 2018. PMID: 30362749
A miniaturized mode-of-action profiling platform enables high throughput characterization of the molecular and cellular dynamics of EZH2 inhibition.
Falkenstern L, Georgi V, Bunse S, Badock V, Husemann M, Roehn U, Stellfeld T, Fitzgerald M, Ferrara S, Stöckigt D, Stresemann C, Hartung IV, Fernández-Montalván A. Falkenstern L, et al. Among authors: fernandez montalvan a. Sci Rep. 2024 Jan 19;14(1):1739. doi: 10.1038/s41598-023-50964-x. Sci Rep. 2024. PMID: 38242973 Free PMC article.
Dual targeting of the androgen receptor and PI3K/AKT/mTOR pathways in prostate cancer models improves antitumor efficacy and promotes cell apoptosis.
Sugawara T, Nevedomskaya E, Heller S, Böhme A, Lesche R, von Ahsen O, Grünewald S, Nguyen HM, Corey E, Baumgart SJ, Georgi V, Pütter V, Fernández-Montalván A, Vasta JD, Robers MB, Politz O, Mumberg D, Haendler B. Sugawara T, et al. Among authors: fernandez montalvan a. Mol Oncol. 2024 Mar;18(3):726-742. doi: 10.1002/1878-0261.13577. Epub 2024 Jan 15. Mol Oncol. 2024. PMID: 38225213 Free PMC article.
39 results