Mini Reviews in Medicinal Chemistry - Volume 10, Issue 7, 2010

After fifty years of DNA targeting through intercalators and groove binders and related studies now the current focus is in RNA targeting. Polyadenylic acid [poly(A)] tail of mRNA has been recently established as a potential drug target due to its significant role in the initiation of translation, maturation and stability of mRNA as well as in the production of alternate proteins in eukaryotic cells. Isoquinoline group of Read More

RNA interference technology has become a powerful laboratory tool to study gene function. Small interfering RNAs (siRNAs) have provided unprecedented opportunities for the development of new therapeutics in human diseases. Unfortunately, siRNA duplexes are not optimal drug-like molecules. The problems for their effective application are fundamentally delivery, stability and off-target effects. Chemical modification Read More

Host defence peptides (HDPs) are multi-functional inducers and effectors of host immunity. Through their direct antimicrobial activity HDPs have for been successfully utilized for many years as topical antibiotics and food preservatives. The more recent appreciation of HDP immunomodulatory activities offers additional opportunities for application as systemic antimicrobials, anti-inflammatory agents and vaccine adjuvants. HDP Read More

Sesquiterpene lactones of the guaianolide and eudermanolide types are considered of interest because they have an effect in the regulation and prevention of oxidative damage and inflammation-mediated biological damage. Dehydroleucodine, a natural sesquiterpene isolated from Artemisia douglasiana Besser, and ilicic aldehyde, a semi-synthetic sesquiterpene lactones, showed in vivo protection in ethanol-induced gastric m Read More

Although a relatively rare malignancy with a national incidence of 3500-4000 annually, Gastrointestinal Stromal Tumor (GIST) is of significance in the realm of clinical and pharmacological research. GIST exhibits remarkable uniformity in its pathogenesis and ultrastructure as 95% of cases are linked to constitutive activation and overexpression of a membrane tyrosine kinase, c-KIT (CD117). Although previously refractory to any Read More

Kv1.5 channels are homotetramers of α-pore subunits mainly present in human atrium and pulmonary vasculature. Thus, Kv1.5 is a pharmacological target for cardiovascular diseases. Kvβ1.3 assemblies with Kvα1.5 and modifies its gating and pharmacology. A further knowledge of α-β interactions and pharmacology will lead a better design of new drugs.

Species of the genus Iris (Iridaceae) have a long history of traditional medicinal use in many places of the world, and they have been previously recognized as rich sources of secondary metabolites, in which flavonoids are found predominantly. During the last decade (1999-2008) over 90 flavonoid constituents have been discovered and characterized, including 38 new compounds, from 15 species of Iris. This review elucid Read More