The Front Cover represents the screening process for identifying novel inhibitors of protein histidine phosphatase PHPT1. Illudalic acid, a fungal natural product derived from Omphalotus illudens (the Eastern American Jack-O’-Lantern mushroom, background) and its synthetic analogs are most potent PHPT1 activity reported to date, appear be reversible, non-competitive inhibitors. enzyme active si...

The RNA-dependent RNA polymerase from the Hepatitis C Virus (gene product NS5B) is a validated drug target because of its critical role in genome replication. There are at least four distinct allosteric sites on the polymerase to which several small molecule inhibitors bind. In addition, numerous crystal structures have been solved with different allosteric inhibitors bound to the polymerase. H...

Since the introduction of the first angiotensin-converting enzyme inhibitor (ACEI), captopril, in 1981, ACEIs have become a mainstay of antihypertensive therapy. In addition to lowering blood pressure, there is overwhelming evidence that ACEIs (and angiotensin receptor blockers) provide end-organ protection independent of their blood pressure–lowering properties in diseases such as congestive h...

Cytochrome P450 (CYP) is a heme containing enzyme superfamily that catalyzes the oxidative biotransformation of lipophilic substrates to hydrophilic metabolites facilitating their removal from cells. The CYPs were first recognized by Martin Klingenberg (Klingenberg, 1958) while studying the spectrophotometric properties of pigments in a microsomal fraction prepared from rat livers. When a dilut...