From hit seeking to magic bullets: The successful union of epigenetic and fragment based drug discovery (EPIDD + FBDD)

Vaidergorn, Miguel M., da Silva Emery, Flavio and Ganesan, A. (2021) From hit seeking to magic bullets: The successful union of epigenetic and fragment based drug discovery (EPIDD + FBDD). Journal of Medicinal Chemistry, 64 (19). pp. 13980-14010. ISSN 0022-2623

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Abstract

We review progress in the application of fragment-based drug discovery (FBDD) to epigenetic drug discovery (EPIDD) targeted at epigenetic writer and eraser enzymes as well as reader domains over the last 15 years. The greatest successes to date are in prospecting for bromodomain binding ligands. From a diverse array of fragment hits, multiple potent and selective compounds ensued, including the oncology clinical candidates mivebresib, ABBV-744, pelabresib, and PLX51107.

Item Type: Article
Additional Information: Funding Information: This study was financed in part by the Coordenação de Aperfeiçoamento de Pessoal de Nível Superior–Brasil (CAPES), Finance Code 001, by São Paulo Research Foundation (FAPESP) Grant No. 2013/50677-7 and 2017/21146-4, and by the National Council for Scientific and Technological Development (CNPq) Grant No. 313834/2018-0.
Uncontrolled Keywords: molecular medicine,drug discovery ,/dk/atira/pure/subjectarea/asjc/1300/1313
Faculty \ School: Faculty of Science > School of Pharmacy
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Depositing User: LivePure Connector
Date Deposited: 24 Nov 2021 03:13
Last Modified: 24 Nov 2021 03:13
URI: https://ueaeprints.uea.ac.uk/id/eprint/82297
DOI: 10.1021/acs.jmedchem.1c00787

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