In vitro characterization and rational analog design of a novel inhibitor of telomerase assembly in MDA MB 231 breast cancer cell line.

ABSTRACT: Tumor cells have unlimited replicative potential, principally due to telomerase activity, which requires assembly of components such as dyskerin (hDKC1), human telomerase reverse transcriptase and human telomerase RNA (hTR). The present study aimed to develop novel inhibitors of telomerase to target the interaction between hTR and hDKC1. Based on docking‑based virtual screening, the candidates R1D2‑10 and R1D2‑15, which exert an in vitro inhibitory effect on telomerase activity, were selected. Human mammary adenocarcinoma MDA‑MB 231 cell line was selected to evaluate the treatment with the aforementioned compounds; the effect on telomere length was evaluated by qPCR, where both compounds caused telomere shortening. Furthermore, expression of genes related to apoptosis and senescence

SUBMITTER: Armando R 

PROVIDER: S-EPMC9500588 | biostudies-literature | 2022 Nov

REPOSITORIES: biostudies-literature