Current Pharmaceutical Design - Volume 8, Issue 7, 2002

The constant increase of life expectancy is associated with major ageing of developed populations. This indicates that the new century will have one of most epidemic progressions of cardiovascular, cancer and inflammatory diseases. The high challenge for medical research is to compress such morbidity. In these conditions, invertebrates have demonstrated to be truly useful models in drug discovery for such ageing diseas Read More

Serine proteases (SP), such as thrombin, factor Xa, elastase, trypsin are implicated in many clinical disorders such as emphysema, arthritis and cardiovascular diseases. These enzymes, in normal physiological conditions, are regulated by naturally occurring serine protease inhibitors, such as anti-thrombin III involved in thromb in inhibition. Primitive parasitic invertebrates have co-evolved highly specific mechanisms to commu Read More

This review discusses the role of protease inhibition with emphasis on the effects of inflammation and vascular immune phenomena in non-immunocompromised hosts. A vast body of knowledge elucidating the role of protease inhibition and hemostasis has accumulated in recent years. The two subjects are intimately linked, but the focus of this review is limited to the anti-inflammatory effects of protease inhibitors. In lig Read More

Since the initial description of a peptidase activity, namely pepsin, in the middle of the 19th century, our understanding of the molecular basis of peptidase function and activation has greatly improved. Further, by sequencing entire genomes, we have reached a stage whereby it is now possible to appreciate the tremendous diversity and unique specificities of peptidases. Because of their importance in most if not all vital Read More

During the last eight years a number of bioactive lipid mediators, the amides or esters of long chain fatty acids, have been discovered or re-discovered. These are: anandamide (N-arachidonoyl-ethanolamine, AEA) and 2-arachidonoylglycerol (2-AG), two endogenous agonists of cannabinoid receptors; oleamide (cis-9- octadecenoamide), a putative endogenous sleep-inducing factor; N-palmitoylethanol amine (PE Read More

Following protein biosynthesis, some of the most important cellular mechanisms that generate biological diversity are the enzymatically driven post-translational modifications that ultimately lead to the formation of bioactive molecules. Within the secretory pathway, a multitude of precursor proteins are thus modified resulting in hormones, neuropeptides, growth factors, receptors and even enzymes. These modifications incl Read More