in therapy Farnesyltransferase inhibitors in hematologic malignancies: new horizons

摘要: Abstract Farnesyltransferase inhibitors (FTIs) are small-molecule that selectively inhibit farnesylation of a number intracellular substrate proteins such as Ras. Preclinical work has revealed their ability to effectively tumor growth across wide range malignant phenotypes. Many hematologic malignancies appear be reasonable disease targets, in they express relevant biologic Ras, Mitogen-Activated Protein Kinase (MAPK), AKT, and others may depend upon farnesyl protein transferase (FTase) activity promote proliferation survival. A host phase I trials have been recently launched assess the applicability FTIs malignancies, many which demonstrate effective enzyme target inhibition, low toxicity, some clinical responses. As result, II initiated variety settings, order further validate identify downstream signal transduction targets modified by these agents. It is anticipated studies will serve define optimal roles patients with provide insight into methods combine other agents.From bloodjournal.hematologylibrary.org guest on June 11, 2013. For personal use only.