Publications by authors named "Tom Heightman"

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Discovery of 6-Fluoro-5-{4-[(5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl]piperazin-1-yl}--methylpyridine-2-carboxamide (AZD9574): A CNS-Penetrant, PARP1-Selective Inhibitor.
Jeffrey W Johannes, Amber Y S Balazs, Derek Barratt, Michal Bista, Matthew D Chuba, Tom D Heightman

J Med Chem· December 2024

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Fragment-Based Discovery of a Novel, Brain Penetrant, Orally Active HDAC2 Inhibitor.
Emiliano Tamanini, Shin Miyamura, Ildiko M Buck, Benjamin D Cons, Lee Dawson, Tom D Heightman

ACS Med Chem Lett· October 2022

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Fragment-Guided Discovery of Pyrazole Carboxylic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2 Related Factor 2 (KEAP1:NRF2) Protein-Protein Interaction.
David Norton, William G Bonnette, James F Callahan, Maria G Carr, Charlotte M Griffiths-Jones, Tom D Heightman

J Med Chem· November 2021

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ASTX029, a Novel Dual-mechanism ERK Inhibitor, Modulates Both the Phosphorylation and Catalytic Activity of ERK.
Joanne M Munck, Valerio Berdini, Luke Bevan, Jessica L Brothwood, Juan Castro, Tom D Heightman

Mol Cancer Ther· October 2021

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Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}--methylpyridine-2-carboxamide (AZD5305): A PARP1-DNA Trapper with High Selectivity for PARP1 over PARP2 and Other PARPs.
Jeffrey W Johannes, Amber Balazs, Derek Barratt, Michal Bista, Matthew D Chuba, Tom D Heightman

J Med Chem· October 2021

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Discovery of ASTX029, A Clinical Candidate Which Modulates the Phosphorylation and Catalytic Activity of ERK1/2.
Tom D Heightman, Valerio Berdini, Luke Bevan, Ildiko M Buck, Maria G Carr

J Med Chem· August 2021

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Fragment-based drug discovery: opportunities for organic synthesis.
Jeffrey D St Denis, Richard J Hall, Christopher W Murray, Tom D Heightman, David C Rees

RSC Med Chem· December 2020

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Structure-Activity and Structure-Conformation Relationships of Aryl Propionic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1/Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1/NRF2) Protein-Protein Interaction.
Tom D Heightman, James F Callahan, Elisabetta Chiarparin, Joseph E Coyle, Charlotte Griffiths-Jones

J Med Chem· May 2019

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Enabling synthesis in fragment-based drug discovery by reactivity mapping: photoredox-mediated cross-dehydrogenative heteroarylation of cyclic amines.
Rachel Grainger, Tom D Heightman, Steven V Ley, Fabio Lima, Christopher N Johnson

Chem Sci· February 2019

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Quantitation of ERK1/2 inhibitor cellular target occupancies with a reversible slow off-rate probe.
Honorine Lebraud, Olga Surova, Aurélie Courtin, Marc O'Reilly, Chiara R Valenzano, Tom D Heightman

Chem Sci· December 2018

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Fragment-Based Discovery of a Potent, Orally Bioavailable Inhibitor That Modulates the Phosphorylation and Catalytic Activity of ERK1/2.
Tom D Heightman, Valerio Berdini, Hannah Braithwaite, Ildiko M Buck, Megan Cassidy

J Med Chem· June 2018

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Highly Potent Clickable Probe for Cellular Imaging of MDM2 and Assessing Dynamic Responses to MDM2-p53 Inhibition.
Honorine Lebraud, Richard A Noble, Nicole Phillips, Keisha Heam, Juan Castro, Tom D Heightman

Bioconjug Chem· June 2018

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Protein degradation: a validated therapeutic strategy with exciting prospects.
Honorine Lebraud, Tom D Heightman

Essays Biochem· November 2017

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Visualization of Endogenous ERK1/2 in Cells with a Bioorthogonal Covalent Probe.
James Sipthorp, Honorine Lebraud, Rebecca Gilley, Andrew M Kidger, Hanneke Okkenhaug, Tom D Heightman

Bioconjug Chem· June 2017

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Discovery of a Potent Nonpeptidomimetic, Small-Molecule Antagonist of Cellular Inhibitor of Apoptosis Protein 1 (cIAP1) and X-Linked Inhibitor of Apoptosis Protein (XIAP).
Emiliano Tamanini, Ildiko M Buck, Gianni Chessari, Elisabetta Chiarparin, James E H Day, Tom D Heightman

J Med Chem· June 2017

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Protein Degradation by In-Cell Self-Assembly of Proteolysis Targeting Chimeras.
Honorine Lebraud, David J Wright, Christopher N Johnson, Tom D Heightman

ACS Cent Sci· December 2016

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Structure of the Epigenetic Oncogene MMSET and Inhibition by N-Alkyl Sinefungin Derivatives.
Dominic Tisi, Elisabetta Chiarparin, Emiliano Tamanini, Puja Pathuri, Joseph E Coyle, Tom D Heightman

ACS Chem Biol· November 2016

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In-gel activity-based protein profiling of a clickable covalent ERK1/2 inhibitor.
Honorine Lebraud, David J Wright, Charlotte E East, Finn P Holding, Marc O'Reilly, Tom D Heightman

Mol Biosyst· August 2016

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Isoxazole-Derived Amino Acids are Bromodomain-Binding Acetyl-Lysine Mimics: Incorporation into Histone H4 Peptides and Histone H3.
Angelina R Sekirnik Née Measures, David S Hewings, Natalie H Theodoulou, Lukass Jursins, Katie R Lewendon, Tom D Heightman

Angew Chem Int Ed Engl· July 2016

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Monoacidic Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1:NRF2) Protein-Protein Interaction with High Cell Potency Identified by Fragment-Based Discovery.
Thomas G Davies, William E Wixted, Joseph E Coyle, Charlotte Griffiths-Jones, Keisha Hearn, Tom D Heightman

J Med Chem· April 2016

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BRD4 assists elongation of both coding and enhancer RNAs by interacting with acetylated histones.
Tomohiko Kanno, Yuka Kanno, Gary LeRoy, Eric Campos, Hong-Wei Sun, Tom D Heightman

Nat Struct Mol Biol· December 2014

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Optimization of sphingosine-1-phosphate-1 receptor agonists: effects of acidic, basic, and zwitterionic chemotypes on pharmacokinetic and pharmacodynamic profiles.
John Skidmore, Jag Heer, Christopher N Johnson, David Norton, Sally Redshaw, Tom D Heightman

J Med Chem· December 2014

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A series of potent CREBBP bromodomain ligands reveals an induced-fit pocket stabilized by a cation-π interaction.
Timothy P C Rooney, Panagis Filippakopoulos, Oleg Fedorov, Sarah Picaud, Wilian A Cortopassi, Tom D Heightman

Angew Chem Int Ed Engl· June 2014

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Targeting low-druggability bromodomains: fragment based screening and inhibitor design against the BAZ2B bromodomain.
Fleur M Ferguson, Oleg Fedorov, Apirat Chaikuad, Martin Philpott, Joao R C Muniz, Tom Heightman

J Med Chem· December 2013

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Fragment-based discovery of 6-azaindazoles as inhibitors of bacterial DNA ligase.
Steven Howard, Nader Amin, Andrew B Benowitz, Elisabetta Chiarparin, Haifeng Cui, Tom D Heightman

ACS Med Chem Lett· December 2013

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