cycloSal-HEX

cycloSal-HEX is a salicylic alcohol (cycloSal) prodrug of HEX (1-hydroxy-2-oxopiperidin-3-yl phosphonate), a competitive small molecule phosphonate inhibitor of enolase 2 (ENO2). Developed by researchers at the University of Texas MD Anderson Cancer Center, it is designed to treat cancers harboring homozygous deletion of the glycolytic enzyme enolase 1 (ENO1), such as certain glioblastomas. These ENO1-deleted cancers are selectively vulnerable to the inhibition of the paralogous isoform ENO2. cycloSal-HEX was developed to improve upon the poor pharmacokinetics and stability of earlier prodrugs like POMHEX. It demonstrates efficient intracellular delivery and bioactivation in the glioblastoma microenvironment, making it a promising candidate for further in vivo evaluation.

Other names

cycloSal prodrug of HEX