Current Medicinal Chemistry - Cardiovascular & Hematological Agents - Volume 2, Issue 3, 2004

The activation of platelets and the resultant aggregation have been shown to play important role in the pathogenesis of cardiovascular, cerebrovascular and peripheral vascular diseases and in acute coronary syndromes. Hence platelet adhesion and aggregation have been identified as promising targets for the development of anti-thrombotic drugs. Glycoprotein (GP) IIb / IIIa antagonism exerts a strong anti-platelet e Read More

Obesity is associated with increased incidence of cardiovascular mortality. However, the mechanisms that link increased fat mass with hypercholesterolemia, hypertension, endothelial dysfunction and coronary heart disease have not been fully elucidated. Unravelling the diverse neuroendocrine systems, which regulate energy balance and body fat has been a long-standing challenge in biology, with obesity as an i Read More

Phospholipase A2 (PLA2) catalyzes the hydrolysis of sn-2 fatty acids from membrane phospholipids resulting in the production of several biologically active phospholipid metabolites such as lysophospholipids, arachidonic acid, eicosanoids and platelet-activating factor. The majority of myocardial PLA2 activity is membrane-associated and does not require Ca2+ for activity (iPLA2). Myocardial iPLA2 demonstrates unique characteris Read More

In this paper, we review our current understanding of the medicinal chemistry of the major peptide systems, which influence body fluid homeostasis. Electrolytes play pivotal roles in intra- and intercellular communication, acidbase equilibrium and, when bound to several macromolecules, they regulate a myriad of enzymatic proteins, receptors and transcription factors. Cell turgor influences the plasma m Read More

A novel human plasma protein was found in the eluate from the dextran sulfate column, which was used for the treatment of the patients with hypercholesteremia to reduce plasma low density lipoprotein. The results of sequence analysis revealed that this protein was a homologue of heavy chains of inter-alpha-trypsin inhibitor (ITI) family, and it was termed IHRP (ITI family heavy chain related protein). IHRP was identif Read More

Cardiovascular disease continues to be a major health problem. Tremendous efforts have been invested in clinical and laboratory research in the hopes of decreasing the risk of patients with cardiovascular disease undergoing cardiac and non-cardiac surgeries. A powerful endogenous mechanism of cardioprotection, termed ischemic preconditioning, was reported in a laboratory setting whereby the myocardium can be Read More

Prostaglandin I2 (PGI2, prostacyclin), an eicosanoid of the cyclooxygenase pathway, causes relaxation of vascular smooth muscle in most blood vessels and inhibits platelet aggregation. PGI2 and its stable analogues activate a specific cell-surface receptor (IP receptor, IPR), which is coupled to adenylyl cyclase through Gs-protein. Elevation of 3': 5'-cyclic monophosphate (cyclic AMP, cAMP) levels has been considered to be a k Read More

Thrombin converts fibrinogen to fibrin and is the most powerful activator of platelets thus playing a crucial role in arterial and venous thrombosis. The limitations of heparin, largely used in the therapy of arterial and venous thromboembolism, has prompted the development of new antithrombotic drugs, able to directly inhibit thrombin. They comprise hirudin, bivalirudin and argatroban, which are antithrombins for p Read More