Drug Design Reviews - Online (Discontinued) - Volume 2, Issue 5, 2005

At present, there are ten times more anticancer drugs being tested in clinical trials than there were 15 years ago. However, many of the new anticancer agents target unconventional aspects of cancer development, interact with other drugs in an unpredictable manner and are predicted to show clinical benefit in only small subpopulations of patients. How can clinical trials be re-designed to accommodate the new features Read More

Lectins represent a class of proteins that recognize and interact with the carbohydrate moieties on biological polymers. Analyzed here are the lectins that interact with the fucose, the terminal carbohydrate residue of secretory glycoconjugates and plasma membrane glycopolymers of eukaryotic cells. The ability to selectively bind the unique fucose containing determinants, referred to as fine carbohydrate specificity, m Read More

Most current therapeutic approaches focus on targeting a protein or its function after it has been translated. A therapeutic approach that is gaining interest is altering the mRNA that encodes for a disease associated protein and preventing the protein from being produced. There are two major therapeutic methods to alter mRNA levels, antisense and RNA interference (RNAi). Currently, antisense is the more developed technolog Read More

Nucleosides are currently used in the treatment of many infections caused by viruses and against various cancers. The principal historic limitations of the development of nucleoside drugs that either directly inhibit DNA or RNA polymerases or that inhibit RNA and DNA replication by virtue of their ability to act as alternative substrates for these polymerases, have been the requirements for cellular penetration of the uncharge Read More

Ionic channels are membrane proteins that can be blocked by many different types of drugs such as local anesthetics, antiarrhythmics, etc. Therefore, they are considered drug targets, whose topology, at the ion channel level, has been analyzed by studying the interactions of specific ion channel blockers and site-directed mutant ion channels. Stereoselective interactions are especially interesting because they can rev Read More

Transcription factors belonging to the NF-kappaB superfamily are involved in several human pathologies, as well as in biological processes facilitating the onset of diseases. Among well established functions of NF-kappa B factors is the promotion of osteoclast differentiation in osteopenic diseases, the enhancement of inflammatory processes in cystic fibrosis, the involvement in asthma and pulmonary diseases associated t Read More

Modulating agents in combination with major chemotherapeutics have been proposed for restoring drug effectiveness in cellular or parasite resistance. Verapamil was the first in vitro modulating agent reported for resistant malaria followed by psychoactive drugs, natural products and other diverse structural compounds. However, conflicting results for in vitro and in vivo assays and in clinical tests have been reported f Read More