Mini Reviews in Medicinal Chemistry - Volume 8, Issue 1, 2008

Liver diseases afflict more than 10% of the world population. Although the main risk factors are known and the population at risk is monitored, new biomarkers are urgently needed to allow early diagnosis and hence more effective therapeutic interventions. Here, we revise the contribution of proteomics to the study of liver diseases and its potential impact in the clinical practice is evaluated.

Since 1990 eight new antiepileptic drugs (AEDs) have been developed. Among these new drugs, Topiramate (TPM) is one of the latest AEDs available for treating drug resistant partial epilepsy both in adults and in children. The mechanisms underlying TPM antiepileptic activity are still incompletely understood. However, TPM, a sulfamatesubstituted derivative of the naturally occurring monosaccharide D-fructose, has a Read More

The nucleocapsid protein (NC) plays seminal roles in HIV replication, thus representing a major drug target. NC functions rely on its two zinc-fingers and flanking basic residues. Zinc ejectors inhibit NC functions, but with limited specificity. New classes of molecules competing with NC or its viral nucleic acid and enzyme partners are reviewed here.

The emergence of drug resistant strains of important human pathogens has made urgent the necessity of finding new targets and novel antimicrobial agents. One of the most promising targets is FabH. In this review we summarize the progress made in the design of FabH inhibitors and the role played by the 3D-structure of the enzyme in the drug design process.

The combination of electrochemistry coupled on-line to mass spectrometry (EC-MS) forms a powerful analytical technique with unique applications in the fields of drug metabolism and proteomics. In this review the latest developments are surveyed from both instrumental and application perspectives. The limitations and solutions for coupling an electrochemical system to a mass spectrometer are discussed. The electroch Read More

Virtual high-throughput screening (vHTS) is a powerful technique for identifying hit molecules as starting points for medicinal chemistry. Numerous successful applications of vHTS have been published using a large variety of methodologies. This review attempts to identify the essential factors for successful virtual screening in the hit identification phase.

The two isoforms of enzyme cyclooxygenase viz. COX-1 and COX-2 play key roles in the metabolism of arachidonic acid. The enzyme COX-2, when over expressed, leads to more production of prostaglandins causing inflammation and it also participates in the propagation of cancer. Therefore, COX-2 becomes the cellular target of a number of chemical entities for the treatment of inflammatory diseases as well as for the chemo Read More

Thyroid stimulating hormone (TSH; also known as thyrotropin), binds cognate receptors on the surface of thyrocytes to regulate proliferation and thyroid hormone synthesis. This unidimensional view of TSH is being transformed as new evidence indicates that TSH acts on adipose tissue. Adipocyte inflammatory responses that predispose to cardiovascular disease may occur in thyroid disorders associated with elevated TSH levels.