Current Medicinal Chemistry - Volume 15, Issue 7, 2008

Malignant Mesothelioma is an aggressive and fatal type of tumor. The incidence of mesothelioma has increased in the past 30 years and is now common as male cancers of the liver, bone and bladder, especially in Europe and Australia. The main risk factor is asbestos exposure even if other co-factor, such as simian virus 40 (SV40) could be implied in its etiology. Unfortunately, its incidence is expected to continue to increase Read More

Glucocorticoids play an essential role in the regulation of multiple physiological processes, including energy metabolism, maintenance of blood pressure and stress responses, as well as cognitive functions. On a tissue-specific level, glucocorticoid action is controlled by 11beta-hydroxysteroid dehydrogenase enzymes. The type 1 enzyme (11beta-HSD1) is a NADP(H)-dependent bidirectional enzyme in vitro and reduces cortison Read More

Nicotinamide adenine dinucleotide (NAD), generally considered a key component involved in redox reactions, has been found to participate in an increasingly diverse range of cellular processes, including signal transduction, DNA repair, and post-translational protein modifications. In recent years, medicinal chemists have become interested in the therapeutic potential of molecules affecting interactions of NAD with NAD-dep Read More

Metabotropic glutamate (mGlu) receptors have received much attention, driven by a strong belief in the potential of these modulatory glutamate receptors as drug targets. So far, major drug discovery programs have largely focused on group I (mGlu1 and 5) and II (mGlu2 and 3) mGlu receptors, which have been implicated in neuropathological and various psychiatric disorders. The four group III representatives (mGlu4 Read More

Polyelectrolyte multilayer films have been well characterized for almost two decades and there is now a growing interest for the development of biomimetic films that could be used in vitro or in vivo to control cellular behaviors. In this review, the important properties of multilayer films designed for cell/surface interactions will be highlighted. The first part will deal with the physico-chemical properties of polypeptide and Read More

Oxytocin (OT) is a neurohypophysial hormone synthesized in the paraventricular and supraoptic nuclei of the hypothalamus. Although OT-like substances have been identified in all vertebrates, OT has been found only in mammals where it plays a major role in the onset and maintaining of behaviors which are typical of these animals, such as labour and lactation. Recently, several data have suggested the involvement of OT Read More

Platensimycin was recently discovered by Merck Research Laboratories and has created considerable interest given its potent antibacterial activity and mode of action. The use of RNA gene-silencing techniques and screening libraries of natural products allowed Merck to find this antibiotic which may have otherwise been missed using conventional methods. Interestingly, platensimycin has shown good activity against a panel of G Read More

Despite its clinical importance, the mechanism of preeclampsia is unclear; however, many believe placental pathology might be related to maternal systemic disease. If this is true, a factor which mediates information from the placenta to the maternal circulation can be hypothesized. Among a variety of such reported factors, soluble fms-like tyrosine kinase-1 (sFlt1) will be the focus of this review. The hypoxic placenta, which is Read More

Bronchiolitis obliterans syndrome (BOS) is the leading cause of death in lung transplant recipients (LTR). BOS is thought to result from chronic immunologic/inflammatory insults leading to peri-bronchiolar leukocyte infiltration, with a subsequent exuberant tissue re-modelling and fibro-obliteration of the luminal space of the allograft airways. Diagnosis is based on functional criteria and severity is graded on the degree o Read More

Asporin is an extracellular matrix protein that belongs to the small leucine-rich repeat proteoglycan (SLRP) family of proteins. It is unique among SLRPs in that it lacks a glycosaminoglycan attachment site and contains an asparatic acid (D) repeat at its amino terminus. Its biological role has been unclear, but recent genetic studies have demonstrated association between asporin and various bone and joint diseases, including Read More