Mini Reviews in Medicinal Chemistry - Volume 6, Issue 12, 2006

The development of safe and effective gene delivery methods is a major challenge to enable gene therapy or DNA vaccines to become a reality. Currently there are two major approaches for delivery of genetic material, viral and non-viral. The majority of on-going clinical trials in gene therapy or DNA vaccines use retroviruses and adenoviruses for delivering genetic materials. Viral delivery systems are far more effectiv Read More

Carbohydrates have been proven as valuable scaffolds to display pharmocophores and the resulting molecules have demonstrated useful biological activity towards various targets including the somatostatin receptors (SSTR), integrins, HIV-1 protease, matrix metalloproteinases (MMP), multidrug resistance-associated protein (MRP), and as RNA binders. Carbohydrate-based compounds have also shown antibacterial and herbicidal activity.

Most biological molecules exhibit more than one function. In particular, many molecules have the ability to directly/ indirectly scavenge free radicals and thus act in living organisms as antioxidant. During oxidative stress, the increase of these molecules levels seems to be a biological response that in synergism with the other antioxidant defence systems may protect cells from oxidation. Among these structures, chond Read More

Pro-inflammatory lipid mediators (i.e. eicosanoids), cytokines (i.e. TNF-α) and reactive oxygen species are targets of interest in the regulation of liver inflammation and oxidative stress. In the current review, we summarize recent advances in the pharmacological modulation of these pathways with especial emphasis on the participation of Kupffer cells, the liver resident macrophages and the cell type most directly rela Read More

There appear to be compelling evidences presenting adiponectin as a key regulator of energy homeostasis. Over the past 10 years, much work has been done to identify the molecular mechanisms by which adiponectin functions in the body. We and other groups have demonstrated that adiponectin activates multiple signaling pathways, which mediate its anti-diabetic, anti-atherogenic and anti-inflammatory functions. Co Read More

β-(1,3)-Glucans are widely distributed within microorganisms or seaweeds in which they act as membrane components or for energy storage, respectively. Since these glucans are not biosynthesized by mammals, they are likely to activate the immune system of their host. Since the discovery of their positive involvement as immunomodulator agents, numerous studies were published all around the glycosciences. The Read More

Non-steroidal anti-inflammatory drugs (NSAID) target the enzyme cyclooxygenase (COX) thus affording relieve from pain, inflammation or fever. As COX-dependently formed prostanoids not only mediate signals involved in inflammation and pain, but also regulate important physiological cardiovascular functions, some NSAID have recently been reported to be associated with arterial thrombosis or hypertension. This is in c Read More

Tumor Associated Carbohydrate Antigens (TACAs) constitute powerful tools as tumor markers and as targets for anticancer immunotherapy. In this review, methods of production of glycopeptide-based vaccines, as well as results of preclinical and clinical studies in cancer patients are discussed.

Cyclooxygenase plays a pivotal role in the transformation of the arachidonic acid to prostaglandins (PGs) and thromboxane. It is composed of two kinds of enzymes, namely cyclooxygenase 1 (COX-1) and cyclooxygenase 2 (COX- 2). Cyclooxygenase 1 is the constructive enzyme whereas the cyclooxygenase 2 is the inducible enzyme. Inhibiting cyclooxygenase 1 is always associated with some undesirable side-effects, while inh Read More

Calmodulin is a Ca2+ binding protein found in many eukaryotic cells. It is one of the most important intracellular mediators of Ca2+-dependant signaling in eukaryotic cells. It regulates diverse processes including mitosis, muscle contraction and nucleotide metabolism by modulating the activity of at least 30 different target enzymes in a calciumdependant manner. Calmodulin plays an important role in the regulation of pr Read More