Drug intelligence / Profile preview

GNE049

Development stage
Preclinical
Lead developer
Genentech
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

GNE049 is a potent and selective small molecule inhibitor of the bromodomains of CREB-binding protein (CBP) and E1A-binding protein p300 (EP300). Developed by Genentech, it serves as a chemical probe to investigate the role of these paralogous transcriptional co-activators in gene regulation. GNE049 has demonstrated the ability to reverse HIV-1 latency in primary cell models by disrupting the enhancer-like chromatin structure of the latent provirus, thereby promoting viral transcription. Its high selectivity for CBP/p300 over other bromodomain-containing proteins makes it a valuable tool in epigenetic research and a potential lead for therapeutic strategies targeting viral reservoirs or certain cancers.

02

Targets

EP300 BD (E1A Binding Protein p300 Bromodomain)CREBBP BD (Creb-binding protein bromodomain)

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