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Items: 11

1.

Considerations for improved performance of competition association assays analysed with the Motulsky-Mahan's "kinetics of competitive binding" model.

Georgi V, Dubrovskiy A, Steigele S, Fernández-Montalván AE.

Br J Pharmacol. 2019 Aug 24. doi: 10.1111/bph.14841. [Epub ahead of print]

PMID:
31444916
2.

Inhibition of BUB1 Kinase by BAY 1816032 Sensitizes Tumor Cells toward Taxanes, ATR, and PARP Inhibitors In Vitro and In Vivo.

Siemeister G, Mengel A, Fernández-Montalván AE, Bone W, Schröder J, Zitzmann-Kolbe S, Briem H, Prechtl S, Holton SJ, Mönning U, von Ahsen O, Johanssen S, Cleve A, Pütter V, Hitchcock M, von Nussbaum F, Brands M, Ziegelbauer K, Mumberg D.

Clin Cancer Res. 2019 Feb 15;25(4):1404-1414. doi: 10.1158/1078-0432.CCR-18-0628. Epub 2018 Nov 14.

PMID:
30429199
3.

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.

Angew Chem Int Ed Engl. 2018 Jun 11;57(24):7220-7224. doi: 10.1002/anie.201801666. Epub 2018 May 9.

PMID:
29601130
4.

Isoform-Selective ATAD2 Chemical Probe with Novel Chemical Structure and Unusual Mode of Action.

Fernández-Montalván AE, Berger M, Kuropka B, Koo SJ, Badock V, Weiske J, Puetter V, Holton SJ, Stöckigt D, Ter Laak A, Centrella PA, Clark MA, Dumelin CE, Sigel EA, Soutter HH, Troast DM, Zhang Y, Cuozzo JW, Keefe AD, Roche D, Rodeschini V, Chaikuad A, Díaz-Sáez L, Bennett JM, Fedorov O, Huber KVM, Hübner J, Weinmann H, Hartung IV, Gorjánácz M.

ACS Chem Biol. 2017 Nov 17;12(11):2730-2736. doi: 10.1021/acschembio.7b00708. Epub 2017 Oct 24.

5.

Super-enhancers define a proliferative PGC-1α-expressing melanoma subgroup sensitive to BET inhibition.

Gelato KA, Schöckel L, Klingbeil O, Rückert T, Lesche R, Toedling J, Kalfon E, Héroult M, Lejeune P, Mönning U, Fernández-Montalván AE, Bäurle S, Siegel S, Haendler B.

Oncogene. 2018 Jan 25;37(4):512-521. doi: 10.1038/onc.2017.325. Epub 2017 Oct 9.

6.

Benzoisoquinolinediones as Potent and Selective Inhibitors of BRPF2 and TAF1/TAF1L Bromodomains.

Bouché L, Christ CD, Siegel S, Fernández-Montalván AE, Holton SJ, Fedorov O, Ter Laak A, Sugawara T, Stöckigt D, Tallant C, Bennett J, Monteiro O, Díaz-Sáez L, Siejka P, Meier J, Pütter V, Weiske J, Müller S, Huber KVM, Hartung IV, Haendler B.

J Med Chem. 2017 May 11;60(9):4002-4022. doi: 10.1021/acs.jmedchem.7b00306. Epub 2017 May 1.

7.

Binding kinetics in drug discovery - A current perspective.

Georgi V, Andres D, Fernandez-Montalvan AE, Stegmann CM, Becker A, Mueller-Fahrnow A.

Front Biosci (Landmark Ed). 2017 Jan 1;22:21-47. Review.

PMID:
27814600
8.

BAY 1125976, a selective allosteric AKT1/2 inhibitor, exhibits high efficacy on AKT signaling-dependent tumor growth in mouse models.

Politz O, Siegel F, Bärfacker L, Bömer U, Hägebarth A, Scott WJ, Michels M, Ince S, Neuhaus R, Meyer K, Fernández-Montalván AE, Liu N, von Nussbaum F, Mumberg D, Ziegelbauer K.

Int J Cancer. 2017 Jan 15;140(2):449-459. doi: 10.1002/ijc.30457. Epub 2016 Oct 20.

9.

ATAD2 is an epigenetic reader of newly synthesized histone marks during DNA replication.

Koo SJ, Fernández-Montalván AE, Badock V, Ott CJ, Holton SJ, von Ahsen O, Toedling J, Vittori S, Bradner JE, Gorjánácz M.

Oncotarget. 2016 Oct 25;7(43):70323-70335. doi: 10.18632/oncotarget.11855.

10.

Discovery and Characterization of a Highly Potent and Selective Aminopyrazoline-Based in Vivo Probe (BAY-598) for the Protein Lysine Methyltransferase SMYD2.

Eggert E, Hillig RC, Koehr S, Stöckigt D, Weiske J, Barak N, Mowat J, Brumby T, Christ CD, Ter Laak A, Lang T, Fernandez-Montalvan AE, Badock V, Weinmann H, Hartung IV, Barsyte-Lovejoy D, Szewczyk M, Kennedy S, Li F, Vedadi M, Brown PJ, Santhakumar V, Arrowsmith CH, Stellfeld T, Stresemann C.

J Med Chem. 2016 May 26;59(10):4578-600. doi: 10.1021/acs.jmedchem.5b01890. Epub 2016 May 3.

11.

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.

Br J Pharmacol. 2016 Jan;173(1):128-41. doi: 10.1111/bph.13342. Epub 2015 Nov 4.

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