Back to Search Start Over

Identification and Development of BRD9 Chemical Probes

Authors :
Ester Colarusso
Maria Giovanna Chini
Giuseppe Bifulco
Gianluigi Lauro
Assunta Giordano
Source :
Pharmaceuticals, Vol 17, Iss 3, p 392 (2024)
Publication Year :
2024
Publisher :
MDPI AG, 2024.

Abstract

The development of BRD9 inhibitors involves the design and synthesis of molecules that can specifically bind the BRD9 protein, interfering with the function of the chromatin-remodeling complex ncBAF, with the main advantage of modulating gene expression and controlling cellular processes. Here, we summarize the work conducted over the past 10 years to find new BRD9 binders, with an emphasis on their structure–activity relationships, efficacies, and selectivities in preliminary studies. BRD9 is expressed in a variety of cancer forms, hence, its inhibition holds particular significance in cancer research. However, it is crucial to note that the expanding research in the field, particularly in the development of new degraders, may uncover new therapeutic potentials.

Details

Language :
English
ISSN :
14248247
Volume :
17
Issue :
3
Database :
Directory of Open Access Journals
Journal :
Pharmaceuticals
Publication Type :
Academic Journal
Accession number :
edsdoj.8d4de4c0eea4455b9814d0b37742734
Document Type :
article
Full Text :
https://doi.org/10.3390/ph17030392