FTase Inhibitor II

FTase Inhibitor II is a potent farnesyl transferase inhibitor.

Protein prenylation is reported as a key mechanism by which functional association of proteins to membranes is mediated. Ras proteins that are regulators of cell proliferation and differentiation are among the proteins undergoing farnesylation.

In vitro: Previous study found that cells were treated with FTase Inhibitor II and two GGTase inhibitors (GGTI-286 and GGTI-2147) and the results showed that there was no change in cell growth in the presence of these inhibitors, even when 100 μM of the drugs were added to the culture. In addition, when cells were treated with a combination of GGTI-2147 and FTase Inhibitor II, ranging from 0.1 nM to 100 μM, cell growth was not affected. Additionally, in the presence of both 50 μM FTase Inhibitor II and 50 μM GGTI-2147, the FTase and GGTase I enzyme activities were abolished [1].

In vivo: Currently, there is no animal in vivo data reported.

Clinical trial: Up to now, FTase Inhibitor II is still in the preclinical development stage.

Reference:
[1] V.  Manne, C. S. Ricca, J. G. Brown, et al. Ras farnesylation as a target for novel antitumor agents: Potent and selective farnesyl diphosphate analog inhibitors of farnesyltransferase. Drug Development Research 34, 121-137 (1995).