Current Pharmaceutical Design - Volume 8, Issue 27, 2002

The enediynes remain among the most potent antitumoral agents to have been discovered in the past decade. Following prodrug activation, the enediynes undergo cycloaromatization reactions resulting in formation of highly reactive diradical intermediates. The diradical species engage in atom-transfer chemistry to produce neutral arene products, in the process inducing damage to key macromolecules. Several of the nat Read More

Gene therapy will change medicine by treating the diseases at their core levels revolutionizing the way to deliver functional proteins. The development of this technology relies in designing optimal systems for DNA transfer and expression (transfection), cationic lipids being a promising alternative. Being safer than viral vectors, they also allow the delivery of larger plasmids and can be easily GMP-manufactured and store Read More

Binding of ligands such as polycyclic aromatic hydrocarbons to the Aryl hydrocarbon Receptor (AhR) and the sequence of events leading to induction of xenobiotic-metabolising enzymes such as the cytochrome P450 isoform 1A1 and subsequent generation of DNA adducts is historically associated with the process of chemical carcinogenesis. Cancer chemopreventative agents, on the other hand, often exert their biologic Read More

Telomerase is a cellular ribonucleoprotein reverse transcriptase responsible for the maintenance of telomeres, the tandemly repeating guanine-rich nucleic acid sequences at the 3'-ends of eukaryotic chromosomes that serve to protect chromosomal stability and maintain integrity. Telomerase enzyme activity is essential for the sustained proliferation of most immortal cells, including cancer cells, and is currently an important re Read More

Camptothecins are cytotoxic agents with a wide spectrum of antitumor activity. The unique mechanism of action, the impressive preclinical efficacy and the clinical success of irinotecan and topotecan have stimulated intensive efforts to identify novel analogues. The development of novel camptothecins was recently rationalized on the basis of the detailed knowledge of mechanism of drug-target interaction and was aimed Read More