Results 161 to 170 of about 5,118 (209)

Geranylgeranyl pyrophosphate-mediated protein geranylgeranylation regulates endothelial cell proliferation and apoptosis during vasculogenesis in mouse embryo

Journal of Genetics and Genomics, 2021
Vascular development is essential for the establishment of the circulatory system during embryonic development and requires the proliferation of endothelial cells. However, the underpinning regulatory mechanisms are not well understood. Here, we report that geranylgeranyl pyrophosphate (GGPP), a metabolite involved in protein geranylgeranylation, plays
Na Xu, Yue Zhao, Chao-Jun Li
exaly   +3 more sources

Geranylgeranyl Diphosphate-Based Inhibitors of Post-Translational Geranylgeranylation of Cellular Proteins

Journal of Medicinal Chemistry, 1996
A novel series of stable analogs of geranylgeranyl diphosphate (GGdP) are described in which the biologically labile diphosphate moiety of GGdP is replaced by portions that can act as stable isosters. The compounds inhibited the geranylgeranyltransferase activity in whole PC-3 prostate cancer cells, as determined by the inhibition of post-translational
MACCHIA, MARCO, JANNITTI N, GERVASI G, DANESI, ROMANO   +3 more
openaire   +3 more sources

Inhibitors of Protein: Geranylgeranyl Transferases

Current Medicinal Chemistry, 2006
The enzyme protein:geranylgeranyl transferase-1 (PGGT-1 or GGTase-I) catalyzes the geranylgeranylation of cysteine residues near the C-termini of a variety of proteins, including most monomeric GTP binding precursor proteins belonging to the Rho, Rac and Rap subfamilies.
Farid, El Oualid, Louis H, Cohen, Gijs A, van der Marel, Mark, Overhand   +3 more
openaire   +2 more sources

Stable analogues of geranylgeranyl diphosphate possessing improved geranylgeranyl versus farnesyl protein transferase inhibitory selectivity

Bioorganic & Medicinal Chemistry Letters, 2003
Phosphonoacetamido(oxy) groups have proven to be good mimics of the diphosphate portion in geranylgeranyl protein transferase I (GGTase I) inhibitors. The introduction of small alkyl groups (Me, Et) into the diphosphate mimic moiety caused a further decrease in collateral farnesyl protein transferase (FTase) inhibitory activity, thereby improving ...
Filippo, Minutolo, Simone, Bertini, Laura, Betti, Romano, Danesi, Gianbattista, Gervasi, Gino, Giannaccini, Chiara, Papi, Giorgio, Placanica, Silvia, Barontini, Simona, Rapposelli, Marco, Macchia   +10 more
openaire   +3 more sources

Digeranyl bisphosphonate inhibits geranylgeranyl pyrophosphate synthase

Biochemical and Biophysical Research Communications, 2007
A primary cellular target of the clinical nitrogenous bisphosphonates is the isoprenoid biosynthetic pathway. Specifically these drugs inhibit the enzyme farnesyl pyrophosphate synthase and deplete cells of larger isoprenoids. Inhibition of this enzyme results in impaired processing of both farnesylated and geranylgeranylated proteins.
Andrew J, Wiemer, Huaxiang, Tong, Kelly M, Swanson, Raymond J, Hohl   +3 more
openaire   +2 more sources

Phosphonomethylphosphorylmethyl(oxy)-analogues of geranylgeranyl diphosphate as stable and selective geranylgeranyl protein transferase inhibitors

Il Farmaco, 2004
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).
MINUTOLO, FILIPPO, M. ANTONELLO, S. BARONTINI, BERTINI, SIMONE, BETTI, LAURA, DANESI, ROMANO, G. GERVASI, GIANNACCINI, GINO, C. PAPI, PLACANICA, GIORGIO, RAPPOSELLI, SIMONA, MACCHIA, MARCO   +11 more
openaire   +2 more sources

Stable propylphosphonic acid analogues of geranylgeranyl diphosphate possessing inhibitory activity on geranylgeranyl protein transferase

Il Farmaco, 2004
Stable analogues of geranylgeranyl diphosphate, possessing 3-(phosphono)propionamido moieties in the place of the metabolically unstable diphosphate portion, were prepared and submitted to prenyltransferase (GGTase and FTase) inhibition assays. In one case, an excellent GGTase inhibitory activity was obtained (IC(50) = 39 nM), accompanied by a certain ...
MINUTOLO, FILIPPO, ASSO V, BERTINI, SIMONE, BETTI, LAURA, GERVASI G, GHILARDI E, GIANNACCINI, GINO, PLACANICA, GIORGIO, PROTA G, RAPPOSELLI, SIMONA, MACCHIA, MARCO   +10 more
openaire   +3 more sources

Phosphonomethylphosphorylmethyl(oxy)‐Analogues of Geranylgeranyl Diphosphate as Stable and Selective Geranylgeranyl Protein Transferase Inhibitors.

ChemInform, 2005
AbstractFor Abstract see ChemInform Abstract in Full Text.
Marco Macchia, et al. et al.
openaire   +1 more source