Rationally Engineered, Chemically Stable Tunicamycin Analogues Decouple DPAGT1 Inhibition from Non-Selective Toxicity

TL;DR

Tunicamycin cyclitol analogues are established as a structurally distinct class of selective DPAGT1-targeted anticancer agents and it is demonstrated that stabilization of the glycosidic linkage is an effective strategy for enhancing pharmacological selectivity, improving in vivo performance, and simplifying the synthetic route.