Current Medicinal Chemistry - Volume 14, Issue 26, 2007

The introduction of highly active antiretroviral therapy (HAART) in 1996 dramatically changed the course of HIV infection. This therapy involves the use of at least three agents from two distinct classes of antivirals: a protease inhibitor (PI) in combination with two nucleoside/nucleotide reverse transcriptase inhibitors (N(t)RTIs), or a non-nucleoside reverse transcriptase inhibitor (NNRTI) in combination with NRTIs. Nine drugs cont Read More

The renin-angiotensin system (RAS) is frequently activated in the patients with chronic liver diseases, and recent studies have shown that RAS plays a pivotal role in the progression of chronic liver diseases, i.e., liver fibrosis and hepatocellular carcinoma (HCC). Angiotensin-II (AT-II) reportedly stimulates contractility and proliferation of the activated hepatic stellate cells, and increases the transforming growth factor-β (TGF-β) e Read More

A successful unified pharmacophore/receptor model which has guided the synthesis of subtype selective compounds is reviewed in light of recent developments both in ligand synthesis and structural studies of the binding site itself. The evaluation of experimental data in combination with a comparative model of the α1β2γ2 GABAA receptor leads to an orientation of the pharmacophore model within the Bz BS. Results not onl Read More

Respiratory viral infections account for a substantial proportion of morbidity world wide and contribute notably to the socioeconomic burden of diseases. Amongst the most important viruses identified so far are Rhinoviruses, Influenza A and Respiratory Syncytial Virus. The knowledge base has broadened at the clinical and experimental level in recent years. However, therapeutic options are still limited. This may be partly d Read More

The diagnosis of pituitary disorders is difficult because several hormone systems are involved. The clinical presentation is often vague and slowly progressing, and clinicians therefore have to rely very much on correct biochemical measurements. This is also associated with difficulties since the pituitary hormones interact, the binding proteins are influenced by the other axes and a variety of other effects, and finally the hormone Read More

Naturally occurring and synthetic peptides may be a novel class of clinically useful antibiotics. A large body of experimental data on structure function relationships for such peptides is available, but the molecular mechanism of their action remains elusive in most cases. Computer simulations can give detailed insights into the interactions between peptides and lipid bilayers, at least one crucial step in the antimicrobi Read More

Valproic acid (2-n-propylpentanoic acid, VPA) is well-established as a mood-stabilizer for bipolar disorder, in addition to its application as a treatment in neurological disorders such as epilepsy, migraine headaches, and chronic neuropathic pain. Its mechanisms of actions in any of the disorders have not yet been fully elucidated but currently include GABA-ergic inhibitory effects, the suppression of NMDA-mediated excit Read More

The O-N intramolecular acyl migration, also named as an acyl shift or acyl transfer reaction, is well-known in organic and peptide chemistry as a simple rearrangement which proceeds under very mild aqueous conditions. Despite a long history with this reaction, its application in medicinal chemistry has only lately been proposed. In the last decade, this reaction has been intensively studied and several applications of this re Read More

Isoflavones are an important class of phytoestrogens that are found at extrememly high levels in soy. Up until recently, daidzein and genistein were considered to be the most important and hence most studied isoflavones, however more recently attention has shifted to isoflavone metabolies. Equol represents the main active product of daidzein metabolism, produced via specific microflora in the gut. It has a longer half life an Read More

Since the first description of self-reactive antibodies in systemic autoimmune rheumatic diseases, many autoantigens have been identified as useful diagnostic biomarkers in clinical immunology. Among the autoantigens, double-stranded desoxoribonucleic acid (dsDNA), the Smith antigen (Sm), topoisomerase-I (topo-I), proliferating cell nuclear antigen (PCNA), and others were described as hallmark targets of systemic autoimmu Read More