WebSep 15, 2007 · We conducted an in vitro screen for resistance to lonafarnib, a farnesyl protein transferase inhibitor that blocks prenylation of a number of proteins important in cell proliferation, and identified 9 mutations clustering around the lonafarnib binding site. In patients treated with a combination of imatinib and lonafarnib, we identified ... WebOct 1, 2000 · Specific inhibitors of farnesyl transferase have been developed in recent years, many of them showing in vitro and in vivo growth inhibitory or cytostatic activity. Recently, results of the first clinical studies with various farnesyl transferase inhibitors have been presented. In the design of phase I and II studies, either single-agent or ...
Transformation by HrasG12V is consistently associated with
WebOct 1, 2024 · AbstractPurpose:. Mutant KRAS is a major driver of pancreatic oncogenesis and therapy resistance, yet KRAS inhibitors are lacking in the clinic. KRAS requires farnesylation for membrane localization and cancer-causing activity prompting the development of farnesyltransferase inhibitors (FTIs) as anticancer agents. However, … WebApr 22, 2024 · A potential strategy to inhibit oncogenic RAS activity is the disruption of RAS prenylation, an obligate step for RAS membrane localization and effector pathway signaling, through inhibition of... lightning music
Dual Farnesyl and Geranylgeranyl Transferase Inhibitor Thwarts …
WebJan 24, 2024 · KO-2806 is a potent next-generation inhibitor of farnesyl transferase designed to improve upon potency, pharmacokinetic and physicochemical properties of earlier FTI drug candidates. WebFarnesyl transferase inhibitors are a new class of biologically active anticancer drugs. … WebFurthermore, these compounds differ from the mono- or dipeptidyl analogs previously described as inhibitors of farnesyl-protein transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as ... lightning multi-function adapter 5in1