Advanced search
Start date
(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

From Hit Seeking to Magic Bullets: The Successful Union of Epigenetic and Fragment Based Drug Discovery (EPIDD plus FBDD)

Full text
Vaidergorn, Miguel M. [1] ; Emery, Flavio da Silva [1] ; Ganesan, A. [2]
Total Authors: 3
[1] Univ Sao Paulo, Sch Pharmaceut Sci Ribeirao Preto, BR-14040903 Ribeirao Preto, SP - Brazil
[2] Univ East Anglia, Sch Pharm, Norwich NR4 7TJ, Norfolk - England
Total Affiliations: 2
Document type: Journal article
Source: Journal of Medicinal Chemistry; v. 64, n. 19, p. 13980-14010, OCT 14 2021.
Web of Science Citations: 0

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. (AU)

FAPESP's process: 17/21146-4 - Heterocyclic chemistry and epigenetic for the development of library of compounds for medicinal chemistry purposes.
Grantee:Flavio da Silva Emery
Support Opportunities: Regular Research Grants
FAPESP's process: 13/50677-7 - Exploring epigenetic targets to fight neglected diseases: Selective sirtuin-2 inhibitors as leishmanicidal compounds
Grantee:Flavio da Silva Emery
Support Opportunities: Research Grants - Research Partnership for Technological Innovation - PITE