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Bioorg Med Chem Lett
; 16(3): 507-11, 2006 Feb.
Article
in English
| MEDLINE
| ID: mdl-16289818
ABSTRACT
Farnesyltransferase inhibitors identified from an ECLiPS library were optimized using solution-phase synthesis. X-ray crystallography of inhibited complexes was used to identify substructures that coordinate to the active site zinc. The X-ray structures were ultimately used to guide the design of second-generation analogs with FTase IC(50)s of less than 1.0 nM.