Six analogues of geranyl pyrophosphate (the monophosphates of geraniol and tetrahydrogeraniol, and the pyrophosphates of nerol, octan-1-ol, tetrahydrogeraniol and citronellol) were synthesized, and were found to be inhibitors of pig liver prenyl- (geranyl-)transferase. The effects of each analogue were analysed in kinetic experiments, which showed the pyrophosphates of citronellol, tetrahydrogeraniol and octan-1-ol to be the most potent inhibitors. The results are interpreted to support a previous hypothesis that the main forces in the binding of substrates to prenyltransferase are non-specific lipophilic forces and a pyrophosphate-binding force.
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Research Article| February 01 1969
Analogues of geranyl pyrophosphate as inhibitors of prenyltransferase
P. W. Holloway;
R. P. M. Bond;
Biochem J (1969) 111 (3): 333–343.
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G. Popják, P. W. Holloway, R. P. M. Bond, M. Roberts; Analogues of geranyl pyrophosphate as inhibitors of prenyltransferase. Biochem J 1 February 1969; 111 (3): 333–343. doi: https://doi.org/10.1042/bj1110333
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