Ontology highlight
ABSTRACT:
SUBMITTER: Rastelli EJ
PROVIDER: S-EPMC8876255 | biostudies-literature | 2021 Aug
REPOSITORIES: biostudies-literature
Rastelli Ettore J EJ Sannino Sara S Hart Duncan J DJ Sharlow Elizabeth R ER Lazo John S JS Brodsky Jeffrey L JL Wipf Peter P
Bioorganic & medicinal chemistry letters 20210602
We developed JMS-053, a potent inhibitor of the dual specificity phosphatase PTP4A3 that is potentially suitable for cancer therapy. Due to the emerging role of the unfolded protein response (UPR) in cancer pathology, we sought to identify derivatives that combine PTP4A3 inhibition with induction of endoplasmatic reticulum (ER) stress, with the goal to generate more potent anticancer agents. We have now generated bifunctional analogs that link the JMS-053 pharmacophore to an adamantyl moiety and ...[more]