HDAC Inhibitors as Anticancer Agents

Tumor initiation and progression are regulated by epigenetic processes that frequently involve histone deacetylases (HDACs), enzymes that control protein acetylation status and epigentically regulate histone tail, chromatin conformation, protein-DNA interaction, and transcription. HDACs are an integral part of the regulation of multiple processes of life, ranging from gene expressions to protein activities, and high expression of HDACs is commonly found in several types of cancer, indicating its potential usefulness in anticancer therapies.

Description

University of Pittsburgh researchers have developed a series of chromane-based hydroxamic acids that have been demonstrated to be potent and selective HDAC inhibitors with potential use as novel anticancer and anti-neurodegenerative agents.

Applications

· Treating cancer
· Treating neurodegenerative disease

Advantages

· Entirely novel set of histone deacetylase inhibitors

Invention Readiness

In vitro data

IP Status

https://patents.google.com/patent/US20240051931A1

Related Publication(s)

Terrab, L., Rosenker, C. J., Johnstone, L., Ngo, L. K., Zhang, L., Ware, N. F., Miller, B., Topacio, A. Z., Sannino, S., Brodsky, J. L., & Wipf, P. (2020). Synthesis and Selective Functionalization of Thiadiazine 1,1-Dioxides with Efficacy in a Model of Huntington’s Disease. ACS Medicinal Chemistry Letters, 11(5), 984–990. https://doi.org/10.1021/acsmedchemlett.0c00018