Current Medicinal Chemistry - Volume 16, Issue 24, 2009

Tamoxifen is a widely known anti-estrogen which has been employed in adjuvant treatment of early-stage, estrogen- sensitive breast cancer for over 20 years. Less well known are the effects of tamoxifen on immune function, which we discuss here. We review the growing body of evidence which demonstrates immunomodulatory effects of tamoxifen, including in vitro and in vivo studies as well as observations made in breas Read More

With the rapid rise of tumor resistance, combinatorial anticancer therapies have gained favor over singlemolecule inhibition to maximize the suppression of oncogenic pathways. In this regard, HSP90 inhibitors have rapidly emerged as a class of promising drugs that can target multiple oncogenic pathways simultaneously. HSP90 is a highly conserved protein chaperone involved in essential cellular functions such as prote Read More

Among the various human cytochrome P450s (CYP450s) that catalyze the biotransformation of xenobiotics, CYP450 2D6 (CYP2D6) is one of the most important based on the number and wide variety of its drug substrates. CYP2D6 shows a high degree of interindividual variability, which is primarily due to the extensive genetic polymorphism that influences its expression and function. A number of drugs have been clinically Read More

The natural product hymenialdisine was first isolated in 1980 from the marine sponges of the genera Hymeniacidon, Acanthella, Axinella and Pseudaxinyssa. The structure was elucidated on the basis of X-ray crystallography demonstrating a structurally interesting pyrrole-azepin-8-one ring system bonded to a glycocyamidine ring. Great interest has been taken in synthesizing this type of scaffold due to its potent activity Read More

A decrease in the number of functioning pancreatic β-cells and insufficient insulin biosynthesis and/or secretion are the hallmarks of diabetes. Therefore, the identification of alternative sources to induce insulin-producing surrogate β-cells is of great importance. For the induction of insulin-producing cells from various cells and/or tissues, it is useful to mimic and reproduce expression alterations of various pancreatic transcri Read More

Tumor necrosis factor-alpha (TNF-α) is a central regulator of inflammation, and TNF-α antagonists may be effective in treating inflammatory disorders in which TNF-α plays an important pathogenetic role. Recombinant or modified proteins are an emerging class of therapeutic agents. To date, several recombinant or modified proteins which acts as TNF antagonists have been disclosed. In particular, antibodies that bind to Read More

The present paper summarizes the possible roles of frequent and unfavourable genetic variants in cerebrovascular disorders, such as stroke and leukoaraiosis. It also approaches the topic theoretically from functional and mathematical points of view, which can help make the accumulating data on genetic variants more understandable. The interplay of an unfavourable genetic polymorphism and environmental clinical facto Read More

This review aims to present different aspects related to cruzipain, one of the most important proteins of the etiological agent of Chagas disease that has been extensively studied in the last two decades, including all the particularities of the molecule as well as to highlight its participation in multiple relevant functions of the parasite to favour the cell invasion phenomena, to facilitate host tissues proteolytic degradation and to Read More