Heightman, Tom D.

Selective inhibition of BET bromodomains

Filippakopoulos, P., Qi, J., Picaud, S., Shen, Y., Smith, W. B., Fedorov, O., Morse, E. M., Keates, T., Hickman, T. T., Felletar, I., et al. (2010) · Nature

Protein Degradation and InhibitorsChromatin Remodeling and Cancer

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Protein Degradation by In-Cell Self-Assembly of Proteolysis Targeting Chimeras

Lebraud, H., Wright, D. J., Johnson, C. N., & Heightman, T. D. (2016) · ACS Central Science

Protein Degradation and InhibitorsClick Chemistry and Applications

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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

Davies, T. G., Wixted, W. E., Coyle, J. E., Griffiths-Jones, C., Hearn, K., McMenamin, R., Norton, D., Rich, S. J., Richardson, C., Saxty, G., et al. (2016) · Journal of Medicinal Chemistry

Genomics, phytochemicals, and oxidative stressComputational Drug Discovery Methods

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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)

Tamanini, E., Buck, I. M., Chessari, G., Chiarparin, E., Day, J. E. H., Frederickson, M., Griffiths-Jones, C. M., Hearn, K., Heightman, T. D., Iqbal, A., et al. (2017) · Journal of Medicinal Chemistry

Cell death mechanisms and regulationChemical Synthesis and Analysis

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Fragment-Based Discovery of a Novel, Brain Penetrant, Orally Active HDAC2 Inhibitor

Tamanini, E., Miyamura, S., Buck, I. M., Cons, B. D., Dawson, L., East, C., Futamura, T., Goto, S., Griffiths-Jones, C., Hashimoto, T., et al. (2022) · ACS Medicinal Chemistry Letters

Histone Deacetylase Inhibitors ResearchCholinesterase and Neurodegenerative Diseases

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