Current Medicinal Chemistry - Volume 16, Issue 36, 2009

Transglutaminases are a large family of related and ubiquitous enzymes which catalyze the cross linking of a glutaminyl residue of a protein/peptide substrate to a lysyl residue of a protein/peptide co-substrate. In addition to lysyl residues, other second nucleophilic co-substrates may include monoamines or polyamines (to form mono- or bisubstituted /crosslinked adducts) or -OH groups (to form ester linkages). In absence of Read More

Eosinophils are major pro-inflammatory cells that make a major contribution to diseases that affect the upper and lower airways, skin and gastrointestinal tract. Interleukin (IL)-5 is central to their maturation and release from the bone marrow together with their subsequent accumulation and activation in the tissues. Mepolizumab is a humanized monoclonal antibody (mAb) with potent IL-5 neutralizing effects Read More

Anticancer active immunotherapy embodies the ideal antitumor therapy, as it theoretically combines target specificity with long-term disease control. Peptide-based cancer vaccines represent the most specific approach to polarize the immune system against malignant cells, since they are preparations made of single epitopes, the minimal immunogenic region of an antigen. Despite the strong rational, the promising preclini Read More

Cancer, which accounted for 7.9 million deaths (around 13% of all deaths) in 2007, is a leading cause of death in the world. Deaths from cancer worldwide are projected to continue rising, with an estimated 12 million deaths in 2030. Therefore, the rapid increase in the cancer burden represents a real crisis for public health and health systems worldwide. Although cancer chemotherapy will cause side effects and drug r Read More

The derivation of pluripotent embryonic stem (ES) cell lines has opened up new areas of research in basic and applied science, most significantly in developmental biology and regenerative medicine. While application-oriented research has for the most part focussed on obtaining differentiated, organotypic cells from ES cells for future cell grafting therapies, ES cells have more immediate potential for use in toxicological in vitro a Read More

The syntheses and transformations of 4-hydroxyquinoline-2-carboxylic acid, kynurenic acid, are reviewed, and special attention is paid to the pharmacological activities and pharmaceutical applications of its derivatives.

Recent clinical studies have shown that patients with chronic liver disease are insulin resistant. Of all etiologies of chronic liver disease including non-alcoholic fatty liver disease, the one that causes the most sever insulin resistance is hepatitis C virus (HCV) infection. Since insulin resistance promotes inflammatory and fibrogenic reactions in the liver, thus leading to the development of liver cirrhosis and hepatocellular carcin Read More

Multiple sclerosis (MS), a chronic demyelinating disorder, is characterized by recurrent neurological deficits or progressive impairment with a high risk of permanent disability. Since the exact pathophysiology and etiology remain still unclear, no curing therapy is currently available. However, several treatments with beneficial effect on relapse rate such as the first line therapies interferon-beta and glatiramer acetate were app Read More

It is well known that cyclins and cyclin-dependent kinases (CDKs) play essential roles in regulation of the cell cycle. In past two decades, the scientific researches suggest that the cyclin D1/ CDK4 complex is a key regulator of the transition through the G1 phase of the cell cycle. Moreover, deregulation of the cyclin D /CDK4 pathway has been identified in multiple tumor types. Thus, CDK4 is a genetically validated therapeuti Read More