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Fluorescent Inhibitors for IspF, an Enzyme in the Non‐Mevalonate Pathway for Isoprenoid Biosynthesis and a Potential Target for Antimalarial Therapy
Author(s) -
Crane Christine M.,
Kaiser Johannes,
Ramsden Nicola L.,
Lauw Susan,
Rohdich Felix,
Eisenreich Wolfgang,
Hunter William N.,
Bacher Adelbert,
Diederich François
Publication year - 2006
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.200503003
Subject(s) - enzyme , chemistry , fluorescence , biosynthesis , biochemistry , mevalonate pathway , terpenoid , mevalonic acid , ternary complex , stereochemistry , combinatorial chemistry , physics , quantum mechanics
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 Zn II ion were clarified by X‐ray analysis.