Current Medicinal Chemistry - Volume 17, Issue 30, 2010

Chronic infection and inflammation contribute to around 25% of cancer cases worldwide. While a direct link between several types of human malignancies and inflammation has now been established, in particular at the gastrointestinal level, the relationship between inflammation and thyroid cancer and the pathophysiology of chronic inflammation that induces papillary thyroid carcinoma (PTC) are still subjects of debat Read More

There is a growing body of evidence that links cancer with genes and pathways that are required for normal embryonic development, increasing the possibility that cancer cells with stem cell properties, particularly self-renewal and multipotentiality, are primarily involved in tumor formation and progression. One novel pathway that is important in regulating the morphogenesis, proliferation, survival and growth in a variety of Read More

Estrogen-dependent breast cancer (EDBC) is a kind of common malignant tumor in postmenopausal women with growing tendency in recent years. Aromatase (AR) is the key enzyme responsible for estrogen biosynthesis and has been considered as an important target for designing inhibitors as potent therapeutic agents for EDBC. AR inhibitors (AIs) are divided into steroidal and nonsteroidal compounds, and the latter shows high Read More

Adenosine is an important autocoid, exerting its physiological effects on the human body by activation of four different G-protein- coupled-receptors (GPCRs) classified as A1, A2A, A2B, and A3. These receptors are coupled to secondary messenger systems including adenylate cyclase, inositol phosphate metabolism, and K+, KATP and Ca2+ channels. Pharmacological agents that increase the activation of A1 adenosine Read More

This article highlights recent advances in the discovery of new positive allosteric modulators of the AMPA receptor, excluding compounds of thiadiazine chemotype, most of which were developed by Servier and the University of Liege. The field of AMPA receptor modulators continues to be a fertile area for the discovery of new potential therapeutic agents, and recent years have seen a marked diversification in the range Read More

Blockade of the human ether-a-go-go related gene 1 (hERG1) channel has been associated with an increased duration of ventricular repolarization, causing prolongation of the time interval between Q and T waves (long QT syndrome, or LQTS). LQTS may result in serious cardiovascular disorders such as tachyarrhythmia and sudden cardiac death. Diverse types of organic compounds bind to the wide intracellular cavity in the pore Read More

Metabolic syndrome is characterized primarily by abdominal obesity, high triglyceride- and low HDL cholesterol levels, elevated blood pressure, and increased fasting glucose levels, which are often associated with coronary heart diseases. Several factors, such as physical inactivity, age, and several endocrine and genetic factors can increase the risk of the development of the disease. Gathered evidence shows, that metaboli Read More

Herbivorous and omnivorous vertebrates have evolved in the presence of a variety of phytoestrogens, i.e., plant-derived compounds that can mimic, modulate or disrupt the actions of endogenous estrogens. Since the discovery of the estrus-inducing effects of some plant products in 1926, considerable effort has been devoted to the isolation and structural and pharmacological characterization of phytoestrogens. Recently, Read More

Amongst ionotropic glutamatergic receptors, the AMPA receptor subtype has been recognized as a major contributor to the fast excitatory neurotransmission in the central nervous system and the expression and maintenance of longterm potentiation. This receptor subtype also represents an interesting target to develop innovative therapeutic drugs such as positive allosteric modulators (AMPA receptor potentiat Read More

As the central energy source, the mitochondria are of great importance in the maintenance of the glia cells of the brain. It is presumed that mitochondrial energy production is affected not only by wellndash characterized genetic mutations of the mitochondria, which are associated with severe malfunctions and resultant acute glia and neuronal cell death, but also by a number of other unfavorable genetic variants. The g Read More

This paper will focus on understanding the role and action of reactive oxygen species (ROS) and reactive nitrogen species (RNS) in the molecular and biochemical pathways responsible for the regulation of the survival of hair cells and spiral ganglion neurons in the auditory portion of the inner ear. The pivotal role of ROS/RNS in ototoxicity makes them potentially valuable candidates for effective otoprotective strategies. In this r Read More