Ontology highlight
ABSTRACT:
SUBMITTER: Marverti G
PROVIDER: S-EPMC8041318 | biostudies-literature | 2021 Mar
REPOSITORIES: biostudies-literature
Marverti Gaetano G Marraccini Chiara C Martello Andrea A D'Arca Domenico D Pacifico Salvatore S Guerrini Remo R Spyrakis Francesca F Gozzi Gaia G Lauriola Angela A Santucci Matteo M Cannazza Giuseppe G Tagliazucchi Lorenzo L Cazzato Addolorata Stefania AS Losi Lorena L Ferrari Stefania S Ponterini Glauco G Costi Maria P MP
Journal of medicinal chemistry 20210312 6
Drug-target interaction, cellular internalization, and target engagement should be addressed to design a lead with high chances of success in further optimization stages. Accordingly, we have designed conjugates of folic acid with anticancer peptides able to bind human thymidylate synthase (hTS) and enter cancer cells through folate receptor α (FRα) highly expressed by several cancer cells. Mechanistic analyses and molecular modeling simulations have shown that these conjugates bind the hTS mono ...[more]