Publications by authors named "Simon Holton"

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Surface-mutagenesis strategies to enable structural biology crystallization platforms.
Martina Schaefer, Vera Pütter, André Hilpmann, Ursula Egner, Simon James Holton

Acta Crystallogr D Struct Biol· September 2024

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Discovery and characterization of orally bioavailable 4-chloro-6-fluoroisophthalamides as covalent PPARG inverse-agonists.
Douglas L Orsi, Steven J Ferrara, Stephan Siegel, Anders Friberg, Léa Bouché, Simon J Holton

Bioorg Med Chem· January 2023

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Discovery and Characterization of the Potent and Highly Selective 1,7-Naphthyridine-Based Inhibitors BAY-091 and BAY-297 of the Kinase PIP4K2A.
Lars Wortmann, Nico Bräuer, Simon J Holton, Horst Irlbacher, Jörg Weiske

J Med Chem· November 2021

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Coordination of Di-Acetylated Histone Ligands by the ATAD2 Bromodomain.
Chiara M Evans, Margaret Phillips, Kiera L Malone, Marco Tonelli, Gabriel Cornilescu, Simon J Holton

Int J Mol Sci· August 2021

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Degradation of CCNK/CDK12 is a druggable vulnerability of colorectal cancer.
Sebastian M Dieter, Christine Siegl, Paula L Codó, Mario Huerta, Anna L Ostermann-Parucha, Simon J Holton

Cell Rep· July 2021

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The potent AMPK inhibitor BAY-3827 shows strong efficacy in androgen-dependent prostate cancer models.
Clara Lemos, Volker K Schulze, Simon J Baumgart, Ekaterina Nevedomskaya, Tobias Heinrich, Simon J Holton

Cell Oncol (Dordr)· June 2021

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Treating Cancer by Spindle Assembly Checkpoint Abrogation: Discovery of Two Clinical Candidates, BAY 1161909 and BAY 1217389, Targeting MPS1 Kinase.
Volker K Schulze, Ulrich Klar, Dirk Kosemund, Antje M Wengner, Gerhard Siemeister, Simon J Holton

J Med Chem· August 2020

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Damage Incorporated: Discovery of the Potent, Highly Selective, Orally Available ATR Inhibitor BAY 1895344 with Favorable Pharmacokinetic Properties and Promising Efficacy in Monotherapy and in Combination Treatments in Preclinical Tumor Models.
Ulrich Lücking, Lars Wortmann, Antje M Wengner, Julien Lefranc, Philip Lienau, Simon J Holton

J Med Chem· July 2020

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Inhibition of BUB1 Kinase by BAY 1816032 Sensitizes Tumor Cells toward Taxanes, ATR, and PARP Inhibitors and .
Gerhard Siemeister, Anne Mengel, Amaury E Fernández-Montalván, Wilhelm Bone, Jens Schröder, Simon J Holton

Clin Cancer Res· February 2019

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Discovery and Characterization of the Potent and Highly Selective (Piperidin-4-yl)pyrido[3,2- d]pyrimidine Based in Vitro Probe BAY-885 for the Kinase ERK5.
Duy Nguyen, Clara Lemos, Lars Wortmann, Knut Eis, Simon J Holton

J Med Chem· January 2019

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Isoform-Selective ATAD2 Chemical Probe with Novel Chemical Structure and Unusual Mode of Action.
Amaury E Fernández-Montalván, Markus Berger, Benno Kuropka, Seong Joo Koo, Volker Badock, Simon J Holton

ACS Chem Biol· November 2017

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Benzoisoquinolinediones as Potent and Selective Inhibitors of BRPF2 and TAF1/TAF1L Bromodomains.
Léa Bouché, Clara D Christ, Stephan Siegel, Amaury E Fernández-Montalván, Simon J Holton

J Med Chem· May 2017

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ATAD2 is an epigenetic reader of newly synthesized histone marks during DNA replication.
Seong Joo Koo, Amaury E Fernández-Montalván, Volker Badock, Christopher J Ott, Simon J Holton

Oncotarget· October 2016

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Functional and Structural Characterization of Bub3·BubR1 Interactions Required for Spindle Assembly Checkpoint Signaling in Human Cells.
Florian Prinz, Vera Puetter, Simon J Holton, Dorothee Andres, Christian M Stegmann

J Biol Chem· May 2016

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WXG100 protein superfamily consists of three subfamilies and exhibits an α-helical C-terminal conserved residue pattern.
Christian Poulsen, Santosh Panjikar, Simon J Holton, Matthias Wilmanns, Young-Hwa Song

PLoS One· January 2015

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Design of a bZip transcription factor with homo/heterodimer-induced DNA-binding preference.
Vivian Pogenberg, Larissa Consani Textor, Laurent Vanhille, Simon J Holton, Michael H Sieweke

Structure· March 2014

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Structural and biochemical characterization of Rv2140c, a phosphatidylethanolamine-binding protein from Mycobacterium tuberculosis.
Georg Eulenburg, Victoria A Higman, Anne Diehl, Matthias Wilmanns, Simon J Holton

FEBS Lett· September 2013

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Structural characterization of a D-isomer specific 2-hydroxyacid dehydrogenase from Lactobacillus delbrueckii ssp. bulgaricus.
Simon J Holton, Madhankumar Anandhakrishnan, Arie Geerlof, Matthias Wilmanns

J Struct Biol· February 2013

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The peroxisomal receptor Pex19p forms a helical mPTS recognition domain.
Nicole Schueller, Simon J Holton, Krisztian Fodor, Morlin Milewski, Petr Konarev

EMBO J· August 2010

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Stoichiometric protein complex formation and over-expression using the prokaryotic native operon structure.
Christian Poulsen, Simon Holton, Arie Geerlof, Matthias Wilmanns, Young-Hwa Song

FEBS Lett· February 2010

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Expression, purification, crystallization and preliminary crystallographic analysis of the mouse transcription factor MafB in complex with its DNA-recognition motif Cmare.
Larissa C Textor, Matthias Wilmanns, Simon J Holton

Acta Crystallogr Sect F Struct Biol Cryst Commun· August 2007

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Structure-based approaches to drug discovery against tuberculosis.
Simon J Holton, Manfred S Weiss, Paul A Tucker, Matthias Wilmanns

Curr Protein Pept Sci· August 2007

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Structural diversity in the six-fold redundant set of acyl-CoA carboxyltransferases in Mycobacterium tuberculosis.
Simon J Holton, Stephanie King-Scott, Ali Nasser Eddine, Stefan H E Kaufmann, Matthias Wilmanns

FEBS Lett· December 2006

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Investigation of the catalytic triad of arylamine N-acetyltransferases: essential residues required for acetyl transfer to arylamines.
James Sandy, Adeel Mushtaq, Simon J Holton, Pamela Schartau, Martin E M Noble

Biochem J· August 2005

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Structure of Mesorhizobium loti arylamine N-acetyltransferase 1.
Simon J Holton, Julien Dairou, James Sandy, Fernando Rodrigues-Lima, Jean Marie Dupret

Acta Crystallogr Sect F Struct Biol Cryst Commun· January 2005

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