Author : Saïd M. Sebti
Publisher : Springer Science & Business Media
ISBN 13 : 1592590136
Total Pages : 285 pages
Book Rating : 4.5/5 (925 download)
Book Synopsis Farnesyltransferase Inhibitors in Cancer Therapy by : Saïd M. Sebti
Download or read book Farnesyltransferase Inhibitors in Cancer Therapy written by Saïd M. Sebti and published by Springer Science & Business Media. This book was released on 2000-10-22 with total page 285 pages. Available in PDF, EPUB and Kindle. Book excerpt: With the explosion of research on genes capable of causing cancer, it has become clear that mutations in the GTPase, Ras, a major regulator of cell division, are found in about 30% of all human cancers, and that farnesylation, a lipid posttranslational modification of Ras, is required for its cancer-causing activity. In Farnesyltransferase Inhibitors in Cancer Therapy, cutting-edge researchers describe their efforts to design, synthesize, and evaluate the biological activities of farnesyltransferase inhibitors (FTIs) and geranylgeranyltransferase inhibitors (GGTIs) that can be used as anticancer drugs and in cardiovascular and parasitic therapy. The authors survey in detail such inhibitors as CAAX box peptidomimetics, FPP mimics, and bisubstrate transition state analogs, and critically review their uses in combination with radiation and other cytotoxic agents, such as gemcitabine, cisplatin, and taxanes. The book also discusses the results from several phase I and II human clinical trials using a variety of FTIs, and demonstrates the design of hypothesis-driven clinical trials with proof-of-concept using biochemical endpoints. Illuminating and richly detailed, Farnesyltransferase Inhibitors in Cancer Therapy constitutes today's standard reference for the pathbreaking use of FTIs and GGTIs in anticancer therapy and offers basic and clinical investigators a comprehensive treatment of the scientific and medical aspects of farnesyltransferase inhibitors.