The diphosphate moiety of geranylgeranyldiphosphate (GGdP) was replaced with metabolically and hydrolytically stable analogous polar portions, in an attempt to obtain new geranylgeranyltransferase (GGTase) inhibitors, which could also be selective over congener enzyme farnesyltransferase (FTase). In particular, the phosphonomethylphosphorylmethoxy derivative showed the highest inhibition potency, accompanied by a satisfactory GGTase/FTase selectivity. © 2004 Elsevier SAS. All rights reserved.
Phosphonomethylphosphorylmethyl(oxy)-analogues of geranylgeranyl diphosphate as stable and selective geranylgeranyl protein transferase inhibitors / F. Minutolo, A. M., B. S., S. Bertini, L. Betti, R. Danesi, G. G., G. Giannaccini, P. C., G. Placanica, S. Rapposelli, M. Macchia. - In: IL FARMACO. - ISSN 0014-827X. - 59:11(2004 Nov), pp. 887-892. [10.1016/j.farmac.2004.08.002]
Phosphonomethylphosphorylmethyl(oxy)-analogues of geranylgeranyl diphosphate as stable and selective geranylgeranyl protein transferase inhibitors
R. Danesi;
2004
Abstract
The diphosphate moiety of geranylgeranyldiphosphate (GGdP) was replaced with metabolically and hydrolytically stable analogous polar portions, in an attempt to obtain new geranylgeranyltransferase (GGTase) inhibitors, which could also be selective over congener enzyme farnesyltransferase (FTase). In particular, the phosphonomethylphosphorylmethoxy derivative showed the highest inhibition potency, accompanied by a satisfactory GGTase/FTase selectivity. © 2004 Elsevier SAS. All rights reserved.
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