Medicinal Chemistry Reviews - Online (Discontinued) - Volume 2, Issue 5, 2005

Lipases are the most used enzymes as biocatalyst in the resolution of chiral compounds. To improve the results, many different techniques have been proposed (protein engineering, random mutagenesis with selection pressure, screening in the nature, etc). However, bearing in mind that enzymes are commonly utilised in the industry in an immobilised form, a simple strategy has recently been reported to permitting greatl Read More

Phospholipases A2 belong to a large family of enzymes involved in the generation of several second messengers that play an important role in signal transduction processes associated with normal brain function. The phospholipase A2 family includes secretory phospholipase A2, cytosolic phospholipase A2, calcium-independent phospholipase A2, and plasmalogen-selective phospholipase A2. The systemic administration of Read More

Tuberculosis (TB) remains the leading cause of mortality due to a bacterial pathogen, Mycobacterium tuberculosis, and infects approximately 32 % of the world's human population. It is estimated that 8.2 million new TB cases occurred worldwide in the year 2000, with approximately 1.8 million deaths in the same year, and more than 95 % of those were in developing countries. The interruption of centuries of decline in case rat Read More

Wide range of dose-limiting toxicities and tumor resistance to drug are significant limitations of the successful use of cis-diamminedichloroplatinum (cisplatin). For a long time it was believed that generally trans-isomers of platinum containing complexes are devoid of biological activity. Data accumulated by the structure-activity relationship studies up to date, confirm that trans-platinum(II) and trans-platinum(IV) complexes o Read More

Pentacyclic triterpenes have been found in many plants and can be isolated from any parts of the plant. Triterpene derivatives were shown to have biological activities including anti-HIV-1 and anti-cancer. The modes of action of the anti-HIV-1 triterpenes have been reported to be associated with virus entry, reverse transcription, virus assembly, and maturation. This review will focus on the mechanisms of action of anti-HIV triterp Read More

Immunosuppressive therapy can be used to prevent graft rejection and to treat autoimmune diseases. Recent advances in the understanding of this immune response have focused on the development of new immunosuppressive medications and new approaches to induction of immunological tolerance and reduction of late graft losses. In this overview, preclinical and clinical studies of the new immunosuppressiv Read More