Current Medicinal Chemistry - Volume 16, Issue 22, 2009

There is rapid development in the field of protein microarray technology with the promise of important advancements in the near future. Protein microarrays have been reportedly successful in serum tumor marker profiling as well as in drug discovery and medicinal chemistry when the effect of small molecules in protein-protein interaction is studied. Some of the bottlenecks of the technology are protein instability, problems w Read More

Drug-induced phospholipidosis is characterised by an excessive accumulation of polar phospholipids in cells or tissues. However, from a toxicological perspective the functional consequences of phospholipidosis remain uncertain and a regulatory position unclear. As a consequence, to minimize compound development risk pharmaceutical companies are beginning to proactively address phospholipidosis within drug disc Read More

Recently, there has been widespread interest in the use of non-invasive methods for the assessment of airway inflammation in a variety of lung diseases including chronic obstructive pulmonary disease (COPD). Sputum induction is a semi-invasive technique the value of which is not restricted to sputum cell counts, as inflammatory mediators can also be measured in the supernatants. However, none of the measurable biomar Read More

Phosphatidylinositol 3-kinases (PI3Ks) are a class of lipid kinases that phosphorylate phosphatidylinositol 4,5- bisphosphate (PIP2) at the 3-OH of the inositol ring to generate phosphatidylinositol 3,4,5-trisphosphate (PIP3), which in turn activates Akt and the downstream effectors like mTOR, and therefore play important roles in cell growth, survival, etc. The phosphatase and tensin homolog deleted in chromosome ten (PTEN), act Read More

Many litres of fluids are found outside cells in the human body. These fluids are rich in dissolved proteins that each have a characteristic three dimensional shape, necessary for normal function, which has been attained by the correct folding of their polypeptide chain(s). The structure of these extracellular proteins can be damaged by a variety of environmental stresses (e.g. heat and oxidation) leading to their partial unf Read More

Mucus production is a cardinal feature of bronchial asthma, contributing to morbidity and mortality in the disease. Goblet cells are major mucus-producing cells, and goblet cell hyperplasia (GCH) is one feature of airway remodeling, defined as structural changes occurring in the airway. A number of studies have demonstrated that Th2-type cells play critical roles in this process and that particularly interleukin-13 (IL-13), a Read More

Currently, the long-term usage of non-nucleoside reverse transcriptase inhibitors (NNRTIs) in HIV/AIDS patients eventually leads to the development of drug resistance and severe side effect. Therefore, it is imperative to look for the novel NNRTIs with potent and broad spectrum anti-mutant activity that are also safe and have excellent pharmacokinetic profiles. In this article, newly emerging NNRTIs scaffolds in recent three y Read More

The vascular endothelial growth factor (VEGF)/VEGF receptor pathways are essential for the regulation of angiogenesis during embryonic development and tumor progression. VEGF receptor 1 (VEGFR-1) has been shown to promote tumor growth and metastasis through the regulation of multiple biological functions in cancer cells, vasculature, stroma and other tumor-associated cells. VEGFR-1 signaling is required for th Read More

The translocator protein (18 kDa) (TSPO), formerly known as the peripheral benzodiazepine receptor (PBR), was originally identified as an alternate binding site for the central benzodiazepine receptor (CBR) ligand, diazepam, in the periphery, but has now been distinguished as a novel site. The TSPO is ubiquitously expressed in peripheral tissues but only minimally in the healthy brain and increased levels of TSPO expression hav Read More

This review, a sequel to part 1 in the series, collects about 107 chemical entities separated from the roots, leaves and flower buds of Panax ginseng, quinquefolius and notoginseng, and categorizes these entities into about 18 groups based on their structural similarity. The bioactivities of these chemical entities are described. The ‘Yin and Yang’ theory and the fundamentals of the ‘five elements’ applied to the traditional C Read More