Fluorescent Inhibitors for IspF, an Enzyme in the Non‐Mevalonate Pathway for Isoprenoid Biosynthesis and a Potential Target for Antimalarial Therapy

Abstract

Designed inhibitors (like 1) of IspF, a key enzyme in the non-mevalonate pathway for terpene biosynthesis and a potential antimalarial target, were synthesized and evaluated. Since fluorescent probes were introduced in these ligands, their affinity towards IspF from E. coli could be determined by fluorescence titrations. The binding modes of two ligands in ternary complexes with IspF and a ZnII ion were clarified by X-ray analysis.