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Publications

Controlling Intramolecular Interactions in the Design of Selective, High-Affinity Ligands for the CREBBP Bromodomain.

Brand M. et al, (2021), J Med Chem

Fragment Binding to the Nsp3 Macrodomain of SARS-CoV-2 Identified Through Crystallographic Screening and Computational Docking.

Schuller M. et al, (2020), bioRxiv

Open Science Discovery of Potent Non-Covalent SARS-CoV-2 Main Protease Inhibitors

Boby ML. et al, (2020)

DFG-1 Residue Controls Inhibitor Binding Mode and Affinity, Providing a Basis for Rational Design of Kinase Inhibitor Selectivity.

Schröder M. et al, (2020), J Med Chem, 63, 10224 - 10234

Synthesis and Biological Investigation of (+)-JD1, an Organometallic BET Bromodomain Inhibitor

Hassell-Hart S. et al, (2020), Organometallics, 39, 408 - 416

Controlling Intramolecular Interactions in the Design of Selective, High-Affinity, Ligands for the CREBBP Bromodomain

Brand M. et al, (2020)

Structural Insights into Interaction Mechanisms of Alternative Piperazine-urea YEATS Domain Binders in MLLT1.

Ni X. et al, (2019), ACS Med Chem Lett, 10, 1661 - 1666

A Chemical Probe for Tudor Domain Protein Spindlin1 to Investigate Chromatin Function.

Fagan V. et al, (2019), J Med Chem, 62, 9008 - 9025

Discovery of a Potent and Selective Fragment-like Inhibitor of Methyllysine Reader Protein Spindlin 1 (SPIN1).

Xiong Y. et al, (2019), J Med Chem, 62, 8996 - 9007

C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays.

Le Bihan Y-V. et al, (2019), Eur J Med Chem, 177, 316 - 337

Discovery of a potent and selective fragment-like inhibitor of SPIN1

Yan X. et al, (2019), ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 258

Fragment-based discovery of a chemical probe for the PWWP1 domain of NSD3.

Böttcher J. et al, (2019), Nat Chem Biol, 15, 822 - 829

Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening.

Resnick E. et al, (2019), J Am Chem Soc, 141, 8951 - 8968

A chemical toolbox for the study of bromodomains and epigenetic signaling.

Wu Q. et al, (2019), Nat Commun, 10

SGC-GAK-1: A Chemical Probe for Cyclin G Associated Kinase (GAK).

Asquith CRM. et al, (2019), J Med Chem, 62, 2830 - 2836

Discovery of a Selective Inhibitor for the YEATS Domains of ENL/AF9.

Christott T. et al, (2019), SLAS Discov, 24, 133 - 141

An Activity-Based Probe Targeting Non-Catalytic, Highly Conserved Amino Acid Residues within Bromodomains.

D'Ascenzio M. et al, (2019), Angew Chem Int Ed Engl, 58, 1007 - 1012

Design, Synthesis and Characterization of Covalent KDM5 Inhibitors.

Vazquez-Rodriguez S. et al, (2019), Angew Chem Int Ed Engl, 58, 515 - 519

WNT Activates the AAK1 Kinase to Promote Clathrin-Mediated Endocytosis of LRP6 and Establish a Negative Feedback Loop.

Agajanian MJ. et al, (2019), Cell Rep, 26, 79 - 93.e8

Structure-Based Approach toward Identification of Inhibitory Fragments for Eleven-Nineteen-Leukemia Protein (ENL).

Heidenreich D. et al, (2018), J Med Chem, 61, 10929 - 10934

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