Resistance to standard anti-cancer treatments is a persistent concern in the field of oncology. In general, there is an initial overall response to first line chemotherapeutics in patients; however, overtime they acquire resistance and experience relapse, leading to an increase in dose or a change in drug regimen. The translesion synthesis (TLS) pathway is a DNA damage tolerance mechanism, which allows proliferating cells to bypass DNA lesions. Previous studies examining the suppression of TLS signaling have increased sensitivity to first-line chemotherapeutics, marking the pathway as an emerging therapeutic target. We have identified small molecules as inhibitors of key protein-protein interactions in the TLS pathway and have evaluated their ability to increase the efficacy of cisplatin in preliminary cellular assays. Herein, we report the identification of these compounds as well as describe their anti-TLS activity.

Identification and characterization of small molecule scaffolds as inhibitors of the translesion synthesis pathway

254th National Meeting (2017)

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.