Current Medicinal Chemistry - Volume 16, Issue 14, 2009

Normal somatic stem cells (SC) are naturally resistant to chemotherapeutic agents due to their expression of various membrane transporter molecules (such as MDR-1), detoxifying enzymes and DNA repair proteins. In addition, they also have a slow rate of cell turnover and therefore escape from chemotherapeutic agents that target rapidly replicating cells. Cancer stem cells (CSC), being the mutated counterparts of Read More

The metastatic spread of cancer is still the major barrier to the treatment of this disease. Understanding the molecular mechanisms underlying the metastatic process is of crucial importance to tune novel therapeutic strategies aimed at contrasting the dissemination of cancer. Metastasis is a sequential multistep process that ultimately leads to the cancer's outgrowth in a different organ from which it had originated. This clinic Read More

Hyaluronan (hyaluronic acid, HA) is a linear naturally occurring polysaccharide formed from repeating disaccharide units of N-acetyl-D-glucosamine and D-glucuronate. Despite its relatively simple structure, HA is an extraordinarily versatile glycosaminoglycan currently receiving attention across a wide front of research areas. It has a very high molar mass, usually in the order of millions of Daltons, and possesses interesting visco- Read More

Quinolones are among the most common frameworks present in the bioactive molecules and hence represent an attractive starting point for the design of combinatorial libraries. Since 1962 4-quinolone-3-carboxylic acid derivatives are clinically used as antibacterial agents worldwide. Currently, fluoroquinolones are approved by the WHO as second-line drugs to treat tuberculosis (TB), and their use in multidrug-resistan Read More

Peroxisome Proliferator Activated Receptors (PPARs) are a family of three related nuclear receptors first cloned in 1990. Their involvement in glucidic and lipidic homeostasis quickly made them an attractive target for the treatment of metabolic syndrome, the most prevalent mortality factor in developed countries. They therefore attracted much synthetical efforts, more particularly PPARγ. Supported by a large number Read More

Biosensors are available and applicable for detection and characterization of specific inhibitors of many enzymes. In this review, biosensors based on fixed acetylcholinesterase (AChE) or butyrylcholinesterase (BChE) are presented. Inhibition of selected enzymes by various compounds, such as organophosphorus and carbamate pesticides, nerve agents (e.g. sarin or VX), and other natural toxins (e.g. aflatoxins), was employed t Read More

Carotid artery intima-media thickness measured by ultrasound has been shown to be correlated with the presence of cardiovascular disease and is now accepted and used as a surrogate marker for atherosclerotic disease, an important organ damage of hypercholesterolemia. In particular, statins reduce ischemic heart disease, improve endothelial function, reduce pro-inflammatory cytokines, reduce left ventricular hypertr Read More

It is believed that the production and accumulation of beta-amyloid (Aβ) peptide is a critical step to the pathogenesis of Alzheimer's disease (AD). BACE 1 (beta-site APP-cleaving enzyme 1 or β-secretase), the key enzyme required for generating Aα from the β-amyloid precursor protein (APP), is regarded as an ideal target for AD therapeutic drug design. Due to low oral bioavailability, metabolic instability and poor ability to pen Read More