Current Medicinal Chemistry - Volume 14, Issue 1, 2007

This review discusses antibacterial peptides from the perspective of development into clinically useful chemotherapeutic drugs using short lactoferricin based peptides as examples. The review shows how important features for antibacterial activity can be identified and explored using the molecular properties of a range of natural and non-natural amino acids. The results have been further refined quantitatively using a Read More

Two of the main pathological hallmarks of Alzheimer's disease (AD) are neuritic plaques and neurofibrillary tangles. Significant evidence supports a critical and probable causative role of βamyloid (Aβ) plaque formation. Since neuroprotective treatments are typically most effective at early stages of injury, the detection and measurement of Aβ load in living brain should be performed at early and perhaps even presymptoma Read More

Beta-blockers are a very important group of drugs widely used for the treatment of cardiovascular diseases. All aryloxyaminopropanols are chiral and show different stereoselectivity in their pharmacodynamic and pharmacokinetic properties for each enantiomer. The more potent beta-adrenoceptor blocking activity is generally associated with (S)-enantiomers. Most beta-blocking agents are sold as racemates although ( Read More

Airway inflammation is an outcome of complex interactions of multiple cell types in an inflammatory network. In recent years, it has become clear that a single target approach is unlikely to be effective for the treatment of inflammatory airway diseases such as asthma. This recognition suggests an alternative approach of targeting multiple cell types and/or mediators. Airway smooth muscle (ASM) cells are unique in serv Read More

Angiogenesis plays a key role in the development of cancer and is precondition for tumor growth, invasion and spread. Therefore, numerous angiogenesis inhibitors have been developed, of which some show potential to defeat cancer in preclinical and clinical trials. However, response to antiangiogenic treatments is often delayed and marked by high interindividual variability making a closely mashed and efficient observat Read More

The chemokine receptor, CXCR4, is a GPCR that transduces signals of its endogenous ligand, CXCL12 (stromal cell-derived factor-1, SDF-1). The CXCL12-CXCR4 system plays an important role in the migration of progenitors during embryologic development of the cardiovascular, hemopoietic, central nervous systems, etc. This system has recently been proven to be involved in several problematic diseases, including HIV infecti Read More

Statins are currently among the most commonly prescribed agents for the prevention of cardiovascular disease. Statins reduce serum cholesterol levels by reversibly inhibiting 3-hydroxy-3- methylglutaryl coenzyme A reductase, the rate-limiting enzyme in cholesterol biosynthesis, in the nanomolar range. Mounting evidence suggests that in addition to their vascular effects such as stabilization of atherosclerotic plaques a Read More

Influenza is a disease that deeply affects millions of people every year. There has not been any drug effective against all strains. Neuraminidase (NA) is the major surface glycoprotein of the influenza virus, which possesses critical enzymatic activity and has been considered as a suitable target for designing agents against influenza viruses. Here we review the structure and functions of this enzyme and touch upon the str Read More