Current Pharmaceutical Design - Volume 14, Issue 1, 2008

In this issue of Current Pharmaceutical Design the superfamily of TRP (Transient Receptor Potential) cation channels is the subject of four detailed reviews. A variety of more than 30 cation channels, members of the TRP family, permeable to Ca2+ and other cations are involved in several pathological and physiological conditions. Based on sequence homology, this superfamily of cation channels has been divided in six main Read More

The ligand deorphanization of TRP channels has a tremendous potential for biomedical and nutritional research, and this review highlights the role that natural products have played in the identification of ligands for these targets and their establishment as viable candidates for drug discovery. Specific ligands have so far been discovered only for some thermoTRPs, like TRPV1, TRPV3, TRPV4, TRPM8 and TRPA1, and the lack of s Read More

The mammalian branch of the Transient Receptor Potential (TRP) superfamily of cation channels consists of 28 members. They can be subdivided in six main subfamilies: the TRPC (‘Canonical’), TRPV (‘Vanilloid’), TRPM (‘Melastatin’), TRPP (‘Polycystin’), TRPML (‘Mucolipin’) and the TRPA (‘Ankyrin’) group. The TRPV subfamily comprises channels that are critically involved in nociception and thermo-sensing (TRPV1, TRPV2, TRPV3, TR Read More

Based on the painful effects of exposure to capsaicin, TRPV1 (transient receptor potential vanilloid subfamily member 1) lo-calization is most readily associated with peripheral sensory neurons, however, TRPV1 is now known to be expressed, albeit at lower levels, in the spinal cord, brain and a wide-range of non-neuronal cells. The latter includes epithelial cells (e.g. keratinocytes, urothe-lium, gastric epithelial cells, enterocytes, Read More

Increasing evidence exists to support the presence of functional transient receptor potential vanilloid type 1 (TRPV1) channels in the brain, where these receptors are unlikely to be activated by high temperature and low pH. Here we review this evidence as well as the literature data pointing to the potential role of endovanilloid-activated brain TRPV1 channels not only in the supraspinal control of pain, body temperature, cardiov Read More

Many examples of specific binding between small molecules are known that are associated with modified physiological and pharmacological activities. Conversely, the antagonism or synergism of small molecules is often correlated with specific binding between the molecules. It follows that small molecule binding can be used as a relatively quick, easy, and specific screen for functionally useful drug actions and interacti Read More

Novel drug delivery systems are one of the widely used delivery systems. In the present scenario, amongst them, “Drug Loaded Erythrocytes” is one of the growing and potential systems for delivery of drugs and enzymes. Erythrocytes are biocompatible, biodegradable, posses long circulation half-life and can be loaded with variety of biologically active substances. Carrier erythrocytes are prepared by collecting bloo Read More

About 50 peptides, and a similar number of peptide receptors, are known to be present in the gut and this amount is likely to rise significantly over the next few years. While there has been a massive research effort to define their functions and their anatomical distribution in the central nervous system (CNS), the understanding of their roles in the gut is far more limited. Classically, the physiological functions include the control of Read More