Drug Design Reviews - Online (Discontinued) - Volume 2, Issue 1, 2005

Type 2 diabetes mellitus (T2DM) represents an increasing epidemic in most of the countries throughout the Western world. One of the main determinants of such a situation is the growing incidence of overweight and obesity. However, the pathophysiological link between obesity and T2DM still remains unclear. The discovery of the circulating hormone resistin, which is produced mainly by adipocytes and appears to be Read More

Many bacteria start production of pathogenicity factors when organised in aggregates, so-called biofilms, where they are much more protected against toxic agents. To form biofilms bacteria monitor their cell density by a process called quorum sensing using small, water soluble molecules which act as autoinducers. N-acyl homoserine lactones (AHL) where the acyl side chains vary in length and degree of oxidation and 4,5- Read More

During the past century human life expectancy has increased significantly due to improved health care, including the availability of vaccines and new pharmaceutical drugs. With the aging population on the rise, complex diseases such as Alzheimer's disease, Parkinson's disease and various types of cancers, combined with new diseases with debilitating consequences can reduce the general quality of life. This, together with t Read More

It is estimated that over 100,000 patients require a pleurodesis in USA each year. Pleurodesis, the iatrogenic induction of pleural fibrosis to obliterate the pleural cavity, is the most effective way to prevent re-accumulation of pleural fluid. Currently used pleurodesing agents - talc, tetracycline derivatives and bleomycin - effect pleurodesis by inducing an acute pleural injury and inflammation, which eventually heals Read More

Sphingolipids, including ceramide, sphingomyelin, and glycosphingolipids, are essential components of eukaryotic cell membranes. At the cell surface, they form species- and cell type-specific patterns that change with cell growth, differentiation, transformation and oncogenesis. Apart from their structural role, they serve as attachment sites for many pathogens and are critically involved in the regulation of inter- and in Read More

G protein-coupled receptors (GPCRs) are major targets for drug discovery. They offer innumerable therapeutic benefits through the promotion or inhibition of GPCR-mediated biochemical, physiological and disease processes. The detailed understanding of how GPCRs detect extracellular signals and transduce them to intracellular G proteins and second messenger pathways has led to the development and exploitation of c Read More

Nordihydroguaiaretic acid (NDGA) is a lignan present in the perspired resin of leaves of Larrea divaricata . This compound and its derivatives have “in vitro” inhibition against several viruses including HIV, herpes simplex I and II, and human papilloma. Junin virus is the etiologic agent of Argentine Hemorrhagic fever of great sanitary importance in Argentine. It is an endemo-epidemic illness transmitted to man by rodents Read More

(-)-Epigallocatechin-3-gallate (EGCG) is the most abundant of the green tea polyphenols. The properties ascribed to EGCG are anti-tumorigenic, anti-inflammatory, antioxidative, antiproliferative, antibacterial and antiviral effects. Recent studies also report pro-inflammatory and pro-apoptotic effects, with a mechanism of action through cell cycle progression inhibition. Its novel properties include inhibition of expression of the Read More