Development of novel mitochondrial pyruvate carrier inhibitors for breast cancer treatment.

ABSTRACT: Reprogrammed metabolism of cancer cells offers a unique target for pharmacological intervention. The mitochondrial pyruvate (Pyr) carrier (MPC) plays important roles in cancer progression by transporting cytosolic Pyr into the mitochondria for use in the tricarboxylic acid cycle. In the current study, a series of novel fluoro-substituted aminocarboxycoumarin derivatives have been evaluated for their MPC inhibition properties. Our studies indicate that the aminocarboxycoumarin template elicits potent MPC inhibitory characteristics, and specifically, structure-activity relationship studies show that the N-methyl-N-benzyl structural template provides the optimal inhibitory capacity. Further respiratory experiments demonstrate that candidate compounds specifically inhibit Pyr-driven respiratio

SUBMITTER: Schumacher TJ 

PROVIDER: S-EPMC12355554 | biostudies-literature | 2025 Aug

REPOSITORIES: biostudies-literature