Current Medicinal Chemistry - Volume 15, Issue 21, 2008

Alzheimer's disease (AD) is a complex disease, involving multiple factors such as the production of aggregation- prone amyloid β (Aβ) peptides, the formation of fibrillarly tangles of microtubule-associating proteins, Tau, and the polymorphism of cholesterol binding protein, APOE4. While understanding the mechanism of AD and the involvement of key players should lead to rational drug discovery against this disease, a tra Read More

Background: Endometriosis is an estrogen-dependent disease, associated with pelvic pain and infertility, with still limited knowledge of the pathogenesis, pathophysiology of related infertility and evolution. Objective: To investigate proteogenomic approaches and new trends of endometriosis treatment. Methods: A literature search was carried out for all articles on endometriosis related to immune system, and t Read More

Molecular substructures and fragment descriptors are important tools for many computational applications in medicinal chemistry and drug design. Here we briefly review the history of molecular fragmentation methods and describe the currently most widely used approaches. Then we focus on random fragmentation methods that have only recently been introduced and discuss selected applications. It is shown that the generati Read More

Lysophosphatidic acid (LPA, 1- or 2-acyl-sn-glycerol 3-phosphate) is a simple phospholipid but displays an intriguing cell biology that is mediated via interactions with both G-protein-coupled seven transmembrane receptors (GPCRs) and nuclear hormone receptors. So far, seven GPCRs (LPA1-5 and recently reported GPR87/LPA6 and P2Y5/LPA7) and a nuclear hormone receptor, PPARγ, have been identified. LPA is predominantly Read More

The expansion of fluorescent techniques for studying the ligand-receptor interaction resulted in a burst of the novel fluorescent ligands development. The discovery of the ligand, that is of high affinity to the receptor and whose localization could be easily visualized, even on the single cell level, gave the researchers a strong impulse to investigate that field of GPCR ligands. Moreover, paying attention to the “non pharm Read More

Quorum sensing (QS) systems are bacterial cell-to-cell communication systems that use small molecules as signals. Since QS is involved in the regulation of virulence and biofilm formation in several pathogenic bacteria, it has been suggested as a new target for the development of novel antibacterial therapies. As such, interference with the signal receptors by using chemical compounds has been proposed as an alternati Read More

Atherosclerosis being a leading death cause in many countries is a chronic inflammatory process in which inflammation, immune activation, and oxidative stress are interactively involved. Some epidemiological and many experimental studies suggest that development of atherosclerosis is associated with the amount of iron stored in the body. Transport of electrons between different forms of iron makes it essential for many Read More

Cetirizine, marketed as a racemic mixture containing both levocetirizine and dextrocetirizine, is a member of the second generation H1 antihistamines clinically used for the treatment of symptoms associated with seasonal allergic rhinitis. Recently, its single R-enantiomer levocetirizine has been approved by the FDA as the newest antihistamine. Cetirizine is a piperazine derivative related to the first generat Read More