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Literature summary for 2.5.1.60 extracted from

  • Coxon, F.P.; Taylor, A.; Stewart, C.A.; Baron, R.; Seabra, M.C.; Ebetino, F.H.; Rogers, M.J.
    The gunmetal mouse reveals Rab geranylgeranyl transferase to be the major molecular target of phosphonocarboxylate analogues of bisphosphonates (2011), Bone, 49, 111-121.
    View publication on PubMed
Search for more literature for 2.5.1.60

Inhibitors

Inhibitors Comment Organism Structure
2-PEPC i.e.3-PEPC, protein geranylgeranyltransferase-II is the major pharmacological target of the inhibitor Mus musculus
3-(1-methylpyridin-1-ium-3-yl)-2-phosphonopropanoate i.e.NE1048 , protein geranylgeranyltransferase-II is the major pharmacological target of the inhibitor Mus musculus
3-PEHPC i.e.3-PEHPC, protein geranylgeranyltransferase-II is the major pharmacological target of the inhibitor Mus musculus
3-PEPC i.e.2-PEPC, protein geranylgeranyltransferase-II is the major pharmacological target of the inhibitor Mus musculus
additional information protein geranylgeranyltransferase-II is the major pharmacological target of phosphonocarboxylate inhibitors. Analysis of several different phosphonocarboxylate drugs demonstrates a very good correlation between the ability of these drugs to inhibit the enzyme with their ability to reduce macrophage cell viability and induce apoptosis Mus musculus
risedronate
-
 Mus musculus

Organism

Organism UniProt Comment Textmining
Mus musculus
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-
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General Information

General Information Comment Organism
physiological function cells from the gunmetal gm/gm mouse, which bear a homozygous mutation in protein geranylgeranyltransferase-II that results in about 80% reduced activity of this enzyme compared to wild-type or heterozygous mice, are more sensitive to the effects of active phosphonocarboxylates, including reducing macrophage cell viability, inhibiting osteoclast formation and inhibiting fluid-phase endocytosis Mus musculus