Current Medicinal Chemistry - Volume 13, Issue 25, 2006

In the last decades, the physiological and pharmacological properties of dopamine receptors were controversial principally because of the lack of selective ligand for some receptor subtypes. Since 1997, some specific D4 agonists have been described and have allowed a therapeutic approach. We report here, compounds described as D4 agonist and when available the SAR. The major studies for physiological implications and th Read More

Structure-based Drug Design (SBDD) is an essential part of the modern medicinal chemistry, and has led to the acceleration of many projects, and even to drugs on the market. Programs that perform docking and scoring of ligands to receptors are powerful tools in the drug designer's armoury that enhance the process of SBDD. They are even deployed on the desktop of many bench chemists. It is timely to review the state of th Read More

Coronary heart disease (CHD) is the leading cause of mortality in Western societies, affecting about one third of the population before their seventieth year. Over the past decades modifiable risk factors of CHD have been identified, including smoking and diet. These factors when altered can have a significant impact on an individuals' risk of developing CHD, their overall health and quality of life. There is strong evidence s Read More

The mucosal immune system comprises B cells that can mount potent antibody responses against a variety of mucosal pathogens. Mucosal B cell responses can play a decisive role in protection against mucosal pathogens. Induction of mucosal B cell responses can be achieved through mucosal vaccination. However, mucosal administration of antigens without the use of adjuvants or delivery systems can lead to toleranc Read More

The efficient removal of unwanted cells, such as senescent, damaged, mutated or infected cells is crucial for the maintenance of normal liver function. In fact, apoptosis has emerged as a potential contributor to the pathogenesis of a number of hepatic disorders, such as viral hepatitis, autoimmune diseases, ethanolinduced injury, cholestasis, and hepatocellular carcinoma. In contrast to the effect of cytotoxic bile acids i Read More

The assessment of S-100B in acute neurological disorders such as global hypoxia, ischaemic or haemorrhagic stroke and traumatic brain injury reflects severity of symptoms and outcome. However, the temporal profile of S-100B release depends on topography, intensity and pathophysiology of the damage e.g. immediate release after traumatic brain injury following the acute destruction of neuronal tissue or Read More

Autoimmune diseases are believed to develop mainly from three factors comprising genetic predisposition, environmental factors and immune (dys-) regulation. In this context, specific nucleic acids of exogenous or endogenous origin that signal through nucleic acid-specific Toll-like receptors (TLRs) have gained much research attention. During ongoing autoimmune disease microbial nucleic acids contribute to flares of disease Read More

The basal ganglia are a highly interconnected group of subcortical nuclei in the vertebrate brain that play a critical role not only in the control of movements but also in some cognitive and behavioral functions. Several recent studies have emphasized that serotonergic pathways in the central nervous system (CNS) are intimately involved in the modulation of the basal ganglia and in the pathophysiology of human involuntary m Read More

There is continued interest in development of antisense reagents (ASRs), including especially antisense oligonucleotides and small interfering RNAs, for experimental as well as therapeutic purposes. Optimization of ASRs begins with target site selection. Here we review protocols which have been developed to empirically determine effective target sites in RNAs. Such library selection technologies have demonstrated clear utility, an Read More

It is now widely accepted that airway inflammation is the key factor underlying the pathogenesis of asthma. Inhaled corticosteroids remain the most important anti-inflammatory treatment for asthma. However, they are rather non-specific in their actions and their use raises concerns over side effects and compliance issues, particularly in children and adolescents. Moreover, a significant sub-group of asthmatic patients resp Read More