Cardiovascular & Hematological Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Cardiovascular & Hematological Agents) - Volume 5, Issue 1, 2007

Apelin is a peptide recently isolated from bovine stomach extracts which appears to act as an endogenous ligand for the previously orphaned G-protein-coupled APJ receptor. The apelin gene encodes for a pre-propeptide consisting of 77 amino acids with mature apelin likely to be derived from the C-terminal region as either a 36, 17 or 13 amino acid peptide. Apelin mRNA expression and peptide immunoreactivity has been Read More

Computational methods have been explored for predicting agents that produce therapeutic or adverse effects in cardiovascular and hematological systems. The quantitative structure-activity relationship (QSAR) method is the first statistical learning methods successfully used for predicting various classes of cardiovascular and hematological agents. In recent years, more sophisticated statistical learning methods have been Read More

The five current members of the thrombospondin (TSP) family can be divided in two subgroups according to their molecular architecture. TSP-1 and -2 (subgroup A) are trimeric matricellular proteins that do not contribute directly to tissue integrity, but influence cell function by modulating cell-matrix interactions, whereas TSP-3, -4 and -5 (subgroup B) are pentameric proteins. TSP-1 and TSP-2 are markedly induced in heali Read More

The ADAM (a disintegrin and metalloprotease) family of proteins possess multi-domain structures composed of a signal peptide, a prodomain, a metalloprotease domain, a disintegrin-like domain, a cysteine rich domain, an epidermal growth factor-like domain, a transmembrane domain and cytoplasmic tail. The disintegrin-like domain shares sequence similarity with the soluble venom disintegrins, a family of proteins which ar Read More

Myocardial sarcolemmal ATP-dependent potassium (KATP) channels, which are normally closed by high ATP concentration, open during ischemia when ATP generation decreases favoring K+ efflux. This reduces action potential duration (APD) decreasing the time of Ca2+ influx and Ca2+ overload. This behavior suggested that they might be involved in the protection against stunning and arrhythmias and in the mechanism Read More

High plasma levels of LDL cholesterol, triglycerides and low levels of HDL cholesterol are strong and independent risk factors of coronary heart disease (CHD). The first two abnormalities are addressed by a variety of drugs including statins, cholesterol absorption inhibitors, fibrates and niacin. Some of these drugs also elevate HDL albeit weakly. Thus treatments optimized for HDL elevation are still an unmet medical nee Read More

Fucoidans -- sulphated polysaccharides extracted from brown algae - could be beneficial in patients with ischemic diseases. Their antithrombotic and proangiogenic properties promote in animals, neovascularization and angiogenesis which prevent necrosis of ischemic tissue. In 1997, endothelial progenitor cells were first identified in human peripheral blood. They are recruited from bone marrow and contribute to neo Read More

Brief periods of ischaemia induce in the myocardium an increased resistance to the injury due to a subsequent, more prolonged ischaemic episode. This phenomenon, known as ischaemic pre-conditioning (IPC), articulated in two distinct phases (an early and a delayed one), is ensured by different biological mechanisms. Although an exhaustive comprehension of these mechanisms has not yet been reached, it is widely acc Read More

Leukocyte recruitment and the expression of pro-inflammatory cytokines are prevalent characteristics of early atherogenesis [1]. Recently, several inflammatory mediators have been linked to atheroma formation and inflammatory pathways have been shown to promote thrombosis [1]. The discovery of mast cells, activated T lymphocytes and macrophages in atherosclerotic lesions, the detection of human leukocyte antigen Read More