Farnesyltransferase Inhibitors in Cancer Therapy

  • Saïd M. Sebti
  • Andrew D. Hamilton

Part of the Cancer Drug Discovery and Development book series (CDD&D)

Table of contents

  1. Front Matter
    Pages i-xii
  2. Paul Workman
    Pages 1-20
  3. Chih-Chin Huang, Carol A. Fierke, Patrick J. Casey
    Pages 21-36
  4. Stephen B. Long, Lorena S. Beese
    Pages 37-48
  5. David Knowles, Jiazhi Sun, Saul Rosenberg, Saïd M. Sebti, Andrew D. Hamilton
    Pages 49-64
  6. Jackson B. Gibbs, Samuel L. Graham, George D. Hartman, Kenneth S. Koblan, Nancy E. Kohl, Charles Omer et al.
    Pages 65-70
  7. Veeraswamy Manne, Frank Lee, Ning Yan, Craig Fairchild, William C. Rose
    Pages 71-86
  8. W. Robert Bishop, James J.-K. Pai, Lydia Armstrong, Marguerite B. Dalton, Ronald J. Doll, Arthur Taveras et al.
    Pages 87-101
  9. Judith S. Sebolt-Leopold, Daniele M. Leonard, W. R. Leopold
    Pages 103-114
  10. Patrick Mailliet, Abdel Laoui, Jean-Dominique Bourzat, Marc Capet, Michel Chevé, Alain Commerçon et al.
    Pages 115-144
  11. Fuyuhiko Tamanoi, Keith Del Villar, Nicole Robinson, MeeRhan Kim, Jun Urano, Wenli Yang
    Pages 145-157
  12. Eric J. Bernhard, Ruth J. Muschel, Elizabeth Cohen-Jonathan, Gilles Favre, Andrew D. Hamilton, Saïd M. Sebti et al.
    Pages 171-195
  13. Michael H. Gelb, Frederick S. Buckner, Kohei Yokoyama, Junko Ohkanda, Andrew D. Hamilton, Lisa Nguyen et al.
    Pages 221-232
  14. Amita Patnaik, Eric K. Rowinsky
    Pages 233-249
  15. Adrienne D. Cox, L. Gerard Toussaint III, James J. Fiordalisi, Kelley Rogers-Graham, Channing J. Der
    Pages 255-273
  16. Back Matter
    Pages 275-280

About this book


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.


biochemistry cancer cancer therapy cardiovascular disease cell chemistry development drugs medicinal chemistry radiation research screening tumorigenesis

Editors and affiliations

  • Saïd M. Sebti
    • 1
  • Andrew D. Hamilton
    • 2
  1. 1.H. Lee Moffitt Cancer Center and Research InstituteUniversity of South FloridaTampaUSA
  2. 2.Department of ChemistryYale UniversityNew HavenUSA

Bibliographic information