PCPA-5-fluorouracil conjugate

PCPA-5-fluorouracil is a research-stage small molecule prodrug conjugate designed to target cancers that overexpress lysine-specific demethylase 1 (LSD1). The compound consists of trans-2-phenylcyclopropylamine (PCPA), a known LSD1 inhibitor, covalently linked to the antimetabolite chemotherapy agent 5-fluorouracil (5-FU). This prodrug strategy utilizes the enzymatic activity of LSD1 to trigger the localized release of 5-FU within the tumor microenvironment. Upon binding and inhibiting LSD1, the PCPA moiety undergoes a chemical transformation that releases the active 5-FU payload, which then inhibits thymidylate synthase to exert cytotoxic effects. Preclinical studies in HCT116 colon cancer cells have demonstrated that this conjugate effectively inhibits cell proliferation, suggesting a potential for enhanced efficacy and reduced systemic toxicity compared to conventional 5-FU therapy.

Other names

PCPA + 5-fluorouraciltrans-2-phenylcyclopropylamine-5-fluorouracil conjugatetrans2-phenylcyclopropylamine-5-fluorouracil conjugatetrans 2-phenylcyclopropylamine-5-fluorouracil conjugatetranylcypromine-5-fluorouracil conjugatetranylcypromine5-fluorouracil conjugatetranylcypromine 5-fluorouracil conjugate