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Biological and Medicinal Chemistry

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Hypoxia-Activated Pro-Drugs of the KDAC Inhibitor Vorinostat (SAHA)

Ewen D. D. Calder, Anna Skwarska, Ishna N. Mistry, Deborah Sneddon, Stuart Conway, Ester M. Hammond

Version 1 posted 16 October 2019

664

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Biological and Medicinal Chemistry

Working Paper

Design, Synthesis and Characterization of Covalent KDM5 Inhibitors

Saleta Vazquez-Rodriguez, Miranda Wright, Catherine Rogers, Adam Cribbs, Srikannathasan Velupillai, Martin Philpott, Henry Lee, James E. Dunford, Kilian Huber, Matthew B. Robers, Jim Vasta, Marie-Laetitia Thezenas, Sarah Bonham, Benedikt M. Kessler, James Bennett, Oleg Fedorov, Florence Raynaud, Adam Donovan, Julian Blagg, Vassilios Bavetsias, Udo Oppermann, Akane Kawamura, Paul Brennan

Version 1 posted 11 September 2018

883

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Biological and Medicinal Chemistry

Working Paper

First fluorescent acetylspermidine deacetylation assay for HDAC10 identifies selective inhibitors with cellular target engagement

Daniel Herp, Johannes Ridinger, Dina Robaa, Stephen A. Shinsky, Karin Schmidtkunz, Talha Z. Yesiloglu, Theresa Bayer, Raphael R. Steimbach, Corey J. Herbst-Gervasoni, Annika Merz, Christophe Romier, Peter Sehr, Nikolas Gunkel, Aubry K. Miller, David W. Christianson, Ina Oehme, Wolfgang Sippl, Manfred Jung

Version 4 posted 30 March 2022

1,327

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Biological and Medicinal Chemistry

Working Paper

Potent and Selective N-Terminal BRD4 Bromodomain Inhibitors by Targeting Non-Conserved Residues and Structured Water Displacement

Huarui Cui, Anand Divakaran, Anil K. Pandey, Jorden A. Johnson, huda zahid, zachary hoell, mikael ellingson, ke shi, Hideki Aihara, Daniel A. Harki, william pomerantz

Version 1 posted 23 April 2020

565

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Biological and Medicinal Chemistry

Working Paper

An Activity-based Probe Targeting Non-catalytic, Highly Conserved Amino Acid Residues Within Bromodomains

Melissa D’Ascenzio, Kathryn Pugh, Rebecca Konietzny, Georgina Berridge, Cynthia Tallant, Shaima Hashem, Octovia P. Monteiro, Jason R. Thomas, Markus Schirle, Stefan Knapp, Brian D. Marsden, Oleg Fedorov, Chas Bountra, Benedikt M. Kessler, Paul E. Brennan

Version 1 posted 17 October 2018

502

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Biological and Medicinal Chemistry

Working Paper

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

Michael Brand, James Clayton, Mustafa Moroglu, Matthias Schiedel, Sarah Picaud, Joseph Bluck, Anna Skwarska, Anthony Chan, Corentine Laurin, Amy Scorah, Larissa See, Timothy Rooney, Oleg Fedorov, Gabriella Perell, Prakriti Kalra, Wilian Cortopassi, Kirsten Christensen, Richard Cooper, Robert Paton, William Pomerantz, Philip Biggin, Ester M. Hammond, Panagis Filippakopoulos, Stuart Conway

Version 1 posted 06 April 2020

617

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3

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Biological and Medicinal Chemistry

Working Paper

Discovery of an MLLT1/3 YEATS Domain Chemical Probe

Moses Moustakim, Thomas Christott, Octovia P. Monteiro, James Bennett, Charline Giroud, Jennifer Ward, Catherine Rogers, Paul Smith, Ioanna Panagakou, Laura Diaz Saez, Suet Ling Felce, Vicki Gamble, Carina Gileadi, Nadia Halidi, David Heidenreich, Apirat Chaikuad, Stefan Knapp, Kilian Huber, Gillian Farnie, Jag Heer, Nenad Manevski, Gennady Poda, Rima Al-awar, Darren J. Dixon, Paul E. Brennan, Oleg Fedorov

Version 1 posted 18 September 2018

585

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Biological and Medicinal Chemistry

Working Paper

Nitroreductase-Mediated Release of Inhibitors of Lysine-Specific Demethylase 1 (LSD1) from Prodrugs in Transfected Acute Myeloid Leukaemia Cells

Manfred Jung, Eva-Maria Herrlinger, Mirjam Hau, Desiree M. Redhaber, Gabriele Greve, Dominica Willmann, Simon Steimle, Michael Müller, Michael Lübbert, Cornelius Miething, Roland Schüle

Version 1 posted 24 October 2019

952

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Biological and Medicinal Chemistry

Working Paper

Ru Catalyst Facilitates Total Chemical Protein Synthesis to Investigate the Effect of Epigenetic Modifications Decorated on Linker Histone H1.2 and Heterochromatin Protein 1α (HP1α)

Naoki Kamo, Tomoya Kujirai, Hitoshi Kurumizaka, Hitoshi Murakami, Gosuke Hayashi, Akimitsu Okamoto

Version 1 posted 08 December 2020

609

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Theoretical and Computational Chemistry

Working Paper

Computational Insights in DNA Methylation: Catalytic and Mechanistic Elucidations

Mansour H. Almatarneh, Ghada G. Kayed, Mohammednoor Altarawneh, Yuming Zhao, Amita Verma

Version 1 posted 12 November 2021

190

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40 results in epigenetics in Keywords: epigenetics

Hypoxia-Activated Pro-Drugs of the KDAC Inhibitor Vorinostat (SAHA)

Design, Synthesis and Characterization of Covalent KDM5 Inhibitors

First fluorescent acetylspermidine deacetylation assay for HDAC10 identifies selective inhibitors with cellular target engagement

Potent and Selective N-Terminal BRD4 Bromodomain Inhibitors by Targeting Non-Conserved Residues and Structured Water Displacement

An Activity-based Probe Targeting Non-catalytic, Highly Conserved Amino Acid Residues Within Bromodomains

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

Discovery of an MLLT1/3 YEATS Domain Chemical Probe

Nitroreductase-Mediated Release of Inhibitors of Lysine-Specific Demethylase 1 (LSD1) from Prodrugs in Transfected Acute Myeloid Leukaemia Cells

Ru Catalyst Facilitates Total Chemical Protein Synthesis to Investigate the Effect of Epigenetic Modifications Decorated on Linker Histone H1.2 and Heterochromatin Protein 1α (HP1α)

Computational Insights in DNA Methylation: Catalytic and Mechanistic Elucidations

40 results in Keywords: epigenetics