Synthesis and evaluation of GGPP geometric isomers: divergent substrate specificities of FTase and GGTase I.

Abstract:

:A stereocontrolled synthetic route has been used to prepare two of the geometric isomers of all-trans-GGPP. Neither of these isomers is effective substrates for mammalian GGTase I, but 3 is a potent inhibitor of this enzyme (IC(50)=100 nM). Surprisingly, both compounds are effective substrates for mammalian FTase.

journal_name

Bioorg Med Chem Lett

authors

Zahn TJ,Whitney J,Weinbaum C,Gibbs RA

doi

10.1016/s0960-894x(01)00292-x

subject

Has Abstract

pub_date

2001-06-18 00:00:00

pages

1605-8

issue

12

eissn

0960-894X

issn

1464-3405

pii

S0960894X0100292X

journal_volume

11

pub_type

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