Identification of a New Interesting BAG3 Modulator Able to Disrupt Cancer-Related Pathways.

ABSTRACT: Continuing the research aimed at discovering new BAG3 modulators as attractive anticancer drug candidates, a screening campaign on an in-house library is performed, including compounds featuring a large variety of scaffolds. The obtained results prompted a focus on the triazole moiety and, following a stepwise structural refinement of this scaffold guided by biophysical assays and computational studies, a very attractive compound (2) is identified showing a tight interaction with BAG3 and displaying a significant cytotoxic activity. The discovery of compound 2, whose effects on apoptosis and proteostasis confirm the disruption of BAG3-related pathways, is particularly relevant given the limited number of BAG3 modulators reported so far. Moreover, the computational data highlight the potent

SUBMITTER: Ruggiero D 

PROVIDER: S-EPMC12530843 | biostudies-literature | 2025 Oct

REPOSITORIES: biostudies-literature