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Authors whose works are in public domain in at least one jurisdiction

List of works by Tom D Heightman

3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands

scientific article

A series of potent CREBBP bromodomain ligands reveals an induced-fit pocket stabilized by a cation-π interaction

scientific article published on 12 May 2014

Bromodomain-peptide displacement assays for interactome mapping and inhibitor discovery

scientific article published in 2011

Click JAHAs: conformationally restricted ferrocene-based histone deacetylase inhibitors

Discovery of a Potent Nonpeptidomimetic, Small-Molecule Antagonist of Cellular Inhibitor of Apoptosis Protein 1 (cIAP1) and X-Linked Inhibitor of Apoptosis Protein (XIAP).

scientific article

Enabling synthesis in fragment-based drug discovery by reactivity mapping: photoredox-mediated cross-dehydrogenative heteroarylation of cyclic amines

scientific article published on 21 December 2018

Fragment-Based Discovery of a Potent, Orally Bioavailable Inhibitor That Modulates the Phosphorylation and Catalytic Activity of ERK1/2

scientific article published on 31 May 2018

Highly Potent Clickable Probe for Cellular Imaging of MDM2 and Assessing Dynamic Responses to MDM2-p53 Inhibition

scientific article published on 12 June 2018

Quantitation of ERK1/2 inhibitor cellular target occupancies with a reversible slow off-rate probe

scientific article published on 17 September 2018

Selective inhibition of BET bromodomains

scientific article

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

scientific article published on 25 April 2019

Synthesis and Biological Evaluation of JAHAs: Ferrocene-Based Histone Deacetylase Inhibitors

scientific article

The design and synthesis of 5- and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains

scientific article published on January 2013

Visualization of Endogenous ERK1/2 in Cells with a Bioorthogonal Covalent Probe.

scientific article

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