Abstract
The syntheses of two analogs (1a and 1b) of farnesyl pyrophosphate incorporating photoactive benzoylbenzoate esters are described. Both 1a and 1b are competitive inhibitors of yeast protein farnesyltransferase with respect to farnesyl pyrophosphate and have Ki values of 3300 nM and 880 nM, respectively. Upon photolysis for two hours, 1a and 1b inactivate the enzyme by 46% and 11%, respectively. These compounds should be useful for a variety of studies of protein prenyltransferases.
Original language | English (US) |
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Pages (from-to) | 4845-4848 |
Number of pages | 4 |
Journal | Tetrahedron Letters |
Volume | 37 |
Issue number | 28 |
DOIs | |
State | Published - Jul 8 1996 |
Bibliographical note
Funding Information:Acknowledgments: This research was supported by funds from the American Cancer Society (BE-222, IN-13-33-47, and JFRA-584). We thank C. D. Poulter for providing E. coli DH5oJpGP114.