Current Medicinal Chemistry - Volume 16, Issue 26, 2009

Calcium-Channel Blockers (CCBs), or calcium antagonists, are a heterogeneous group of drugs that produce cardiovascular effects by preventing the influx of calcium ions through L-type voltage-dependent calcium channels in specialized electrical system and conduction tissue cells, like myocardial and vascular smooth muscle cells. In recent years, CCBs have found their way in obstetrics and gynecology, especially in the Read More

The L-type Ca2+ channel plays a critical role in cardiac function as the main route for entry of calcium into cardiac myocytes. It is essential to excitability as it shapes the long plateau phase of the cardiac action potential that is unique to cardiac ventricular myocytes. It is necessary for contraction as it triggers the release of calcium from sarcoplasmic reticulum stores for actin-myosin interaction. The L-type Ca2+ chann Read More

The Translocator protein (TSPO), formerly known as the peripheral-type benzodiazepine receptor, is an 18 kDa mitochondrial protein primarily involved in steroid biosynthesis in both peripheral and glial cells. It has been extensively reported that TSPO regulates the rate-limiting translocation of cholesterol from the outer to the inner mitochondrial membrane before its transformation by cytochrome P450scc into pregnenolone Read More

The pharmacological properties of small organic molecules depend on their three-dimensional (3D) structure. That includes physico-chemical properties (e.g. solubility, partition equilibria) and molecular recognition such as binding to a therapeutic macromolecular target. At physiological temperature, the 3D structure of a flexible small molecules is expected to cover an ensemble of energetically accessible conformations. Read More

In contrast with the parent class of flavonoids, the distribution of the isoflavonoid class in the plant kingdom is relatively limited, probably owing to the sporadic occurrence of isoflavone synthase. Isoflavonoids have been mostly found in the subfamily Fabaceae/Papilionoideae of the Leguminosae family. Isoprenoid-substituted (also called complex) isoflavonoids are expressed from a smaller number of plants, as a res Read More