Poly (ADP-ribose) Polymerase Inhibitors Alan Ashworth INTRODUCTION Cancer cells may harbor defects in DNA repair pathways leading to genomic instability. This can foster tumorigenesis but also provides a weakness that…
Proteasome Inhibitors Christopher J. Kirk Brian B. Tuch Shirin Arastu-Kapur Lawrence H. Boise BIOCHEMISTRY OF THE UBIQUITIN-PROTEASOME PATHWAY The ubiquitin proteasome system is involved in the degradation of more than…
Histone Deacetylase Inhibitors and Demethylating Agents Steven D. Gore Stephen B. Baylin James G. Herman INTRODUCTION The past decade has seen an explosive growth, especially at a genome-wide level, in…
Kinase Inhibitors as Anticancer Drugs Charles L. Sawyers INTRODUCTION In 2001, the first tyrosine-kinase inhibitor imatinib was approved for clinical use in chronic myeloid leukemia. The spectacular success of this…
Antimicrotubule Agents Christopher J. Hoimes Lyndsay N. Harris MICROTUBULES Microtubules are vital and dynamic cytoskeletal polymers that play a critical role in cell division, signaling, vesicle transport, shape, and polarity,…
Topoisomerase Interactive Agents Khanh T. Do Shivaani Kummar James H. Doroshow Yves Pommier CLASSIFICATION, BIOCHEMICAL, AND BIOLOGIC FUNCTIONS OF TOPOISOMERASES Nucleic acids (DNA and RNA) being long polymers, topoisomerases fulfill…
Antimetabolites M. Wasif Saif Edward Chu ANTIFOLATES Reduced folates play a key role in one-carbon metabolism, and they are essential for the biosynthesis of purines, thymidylate, and protein biosynthesis. Aminopterin…
Platinum Analogs Peter J. O’Dwyer A. Hilary Calvert INTRODUCTION The platinum drugs represent a unique and important class of antitumor compounds. Alone or in combination with other chemotherapeutic agents, cis-diamminedichloroplatinum…
Alkylating Agents Kenneth D. Tew PERSPECTIVES Alkylating agents were the first anticancer molecules developed, and they are still used today. After more than 50 years of use, the basic chemistry…
Pharmacogenomics Christine M. Walko Howard L. McLeod INTRODUCTION The evolution of understanding cancer biology has yielded many advances that have been translated into cancer treatment. Application of this knowledge has…
