Farnesyltransferase inhibitors in cancer therapy / edited by Said M. Sebti and Andrew Hamilton.

Format:

Book

Contributor:

Sebti, Saïd M.

Hamilton, Andrew D.

Series:

Cancer drug discovery and development

Language:

English

Subjects (All):

Dimethylallyltranstransferase--Inhibitors--Therapeutic use--Testing.

Dimethylallyltranstransferase.

Cancer--Chemotherapy.

Cancer.

Dimethylallyltranstransferase--antagonists & inhibitors.

Antineoplastic Agents--chemical synthesis.

Drug Design.

Enzyme Inhibitors--therapeutic use.

Genes, ras.

Testing.

Medical Subjects:

Dimethylallyltranstransferase--antagonists & inhibitors.

Antineoplastic Agents--chemical synthesis.

Drug Design.

Enzyme Inhibitors--therapeutic use.

Genes, ras.

Physical Description:

xii, 280 pages : illustrations ; 26 cm.

Place of Publication:

Totowa, N.J. : Humana Press, [2001]

Summary:

Cutting-edge researchers describe their efforts to design, synthesize, and evaluate the biological activities of farensyltransferase inhibitors (FTIs); geranylgeranyltransferase inhibitors (GGTIs) are also discussed as potential anticancer drugs. 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. 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.

Contents:

1 Signal Transduction Pathways: A Goldmine for Therapeutic Targets / Paul Workman 1

2 The Biochemistry of Farnesyltransferase and Geranylgeranyltransferase I / Chih-Chin Huang, Carol A. Fierke, Patrick J. Casey 21

3 Structures of Protein Farnesyltransferase / Stephen B. Long, Lorena S. Beese 37

4 Peptidomimetic-Based Inhibitors of Farnesyltransferase / David Knowles, Jiazhi Sun, Saul Rosenberg, Said M. Sebti, Andrew D. Hamilton 49

5 Antitumor Efficacy of a Farnesyltransferase Inhibitor in Transgenic Mice / Jackson B. Gibbs, Samuel L. Graham, George D. Hartman, Kenneth S. Koblan, Nancy E. Kohl, Charles Omer, Angel Pellicier, Jolene Windle, Allen Oliff 65

6 Development of Farnesyltransferase Inhibitors as Potential Antitumor Agents / Veeraswamy Manne, Frank Lee, Ning Yan, Craig Fairchild, William C. Rose 71

7 Tricyclic Farnesyl Protein Transferase Inhibitors: Antitumor Activity and Effects on Protein Prenylation / W. Robert Bishop, James J.-K. Pai, Lydia Armstrong, Marguerite B. Dalton, Ronald J. Doll, Arthur Taveras, George Njoroge, Michael Sinensky, Fang Zhang, Ming Liu, Paul Kirschmeier 87

8 Histidylbenzylglycinamides: A Novel Class of Farnesyl Diphosphate-Competitive Peptidic Farnesyltransferase Inhibitors / Judith S. Sebolt-Leopold, Daniele M. Leonard, W. R. Leopold 103

9 From Random Screening of Chemical Libraries to the Optimization of FPP-Competitive Inhibitors of Farnesyltransferase / Patrick Mailliet, Abdel Laoui, Jean-Dominique Bourzat, Marc Capet, Michel Cheve, Alain Commercon, Norbert Dereu, Alain LeBrun, Jean-Paul Martin, Jean-Francois Peyronel, Christophe Salagnad, Fabienne Thompson, Martine Zucco, Jean-Dominique Guitton, Guy Pantel, Marie-Christine Bissery, Clive Brealey, Jacques Lavayre, Yves Lelievre, Jean-Francois Riou, Patricia Vrignaud, Marc Duchesne, Francois Lavelle 115

10 Genetic Analysis of FTase and GGTase I and Natural Product Farnesyltransferase Inhibitors / Fuyuhiko Tamanoi, Keith Del Villar, Nicole Robinson, MeeRhan Kim, Jun Urano, Wenli Yang 145

11 Effects of Farnesyltransferase Inhibitors on Cytoskeleton, Cell Transformation, and Tumorigenesis: The FTI-Rho Hypothesis / George C. Prendergast 159

12 Prenyltransferase Inhibitors as Radiosensitizers / Eric J. Bernhard, Ruth J. Muschel, Elizabeth Cohen-Jonathan, Gilles Favre, Andrew D. Hamilton, Said M. Sebti, W. Gillies McKenna 171

13 Farnesyltransferase and Geranylgeranyltransferase I Inhibitors as Novel Agents for Cancer and Cardiovascular Diseases / Said M. Sebti, Andrew D. Hamilton 197

14 Protein Prenylation in Trypanosomatids: A New Piggy-Back Medicinal Chemistry Target for the Development of Agents Against Tropical Diseases / Michael H. Gelb, Frederick S. Buckner, Kohei Yokoyama, Junko Ohkanda, Andrew D. Hamilton, Lisa Nguyen, Bartira Rossi-Bergmann, Kenneth D. Stuart, Said M. Sebti, Wesley C. Van Voorhis 221

15 Early Clinical Experience with Farnesyl Protein Transferase Inhibitors: From the Bench to the Bedside / Amita Patnaik, Eric K. Rowinsky 233

16 Phase I Trial of Oral R115777 in Patients with Refractory Solid Tumors: Preliminary Results / Gary R. Hudes, Jessie Schol 251

17 Farnesyltransferase and Geranylgeranyltransferase Inhibitors: The Saga Continues / Adrienne D. Cox, L. Gerard Toussaint III, James J. Fiordalisi, Kelley Rogers-Graham, Channing J. Der 255.

Notes:

Includes bibliographical references and index.

ISBN:

0896036294

OCLC:

43701932