Authors:

Hafsa Ouaakki

Date Created:

Not specified

Course Title:

Professor:

Not specified

About Paper:

Aberrant epigenetic modifications underpin oncogenic gene expression and contribute to tumorigenesis, therapeutic resistance, and cancer progression. Histone deacetylation results in a condensed chromatin state that is associated with gene silencing through transcriptional repression. Targeting histone deacetylase (HDAC) enzymes using highly selective proteolysis targeting chimeras (PROTACs) has been a focus of cancer therapeutic development due to downstream effects in cell-cycle regulation, DNA repair, and apoptosis. Here we demonstrate the efficacy of the PROTAC-based HDAC 3/8 degrader, YX22968 and the negative control YX24912-NC, on colony formation of four carcinoma cell lines: two non-small cell lung cancer cell lines H1299 and A549, the colorectal cancer cell line HCT116, and the triple-negative breast cancer cell line BT549. Our findings indicate that YX22968 is more effective in preventing growth of A549 and BT549 while YX24912-NC was able to limit growth of H1299 and HCT116. These results suggest that PROTAC-based HDAC 3/8 degraders can be used to restrict growth of carcinomas and highlight their ability as a potential clinical treatment for cancer. 80

Source:

University of Florida / 2024

Topics:

No topics listed

Co-authors:

Hafsa Ouaakki