The mergers of large pharmaceutical companies, the globalization of R&D processes and the integration of biologics into big pharma have resulted in massive job losses for medicinal chemists in the traditional US pharmace...
The cloning of the three tachykinin receptors in the late 1980s formed the basis of intense preclinical research efforts into the systems relating to the tachykinin receptors, as well as compound screening campaigns. Rem...
Thermal shift assays are one of the label-free technologies gaining popularity in drug discovery and academic research. This review summarizes the various detection formats used in these assays, and provides an in-depth ...
The liver X receptors LXR alpha and LXR beta regulate the expression of genes promoting cellular cholesterol efflux and the formation of HDL particles, and are atheroprotective. However, LXR alpha and LXR beta also regul...
Chemokines and chemokine receptors form a complex and diverse system known to be relevant for leukocyte activation and trafficking. There has been significant interest in the development of anti-inflammatory drugs that a...
mTOR is a serine-threonine kinase that plays a key role in the regulation of cellular growth. The mTOR pathway consists of two distinct complexes: mTOR/Raptor (mTORC1) and mTOR/Rictor (mTORC2). In response to changes in ...
In the past decade, intensive efforts have focused on the discovery of both nucleos(t)ide and non-nucleoside inhibitors of the HCV NS5B polymerase. These efforts have resulted in several promising agents advancing in cli...
Antagonism of the adenosine A(2A) receptor has emerged as a promising non-dopaminergic approach for the potential treatment of Parkinson's disease (PD). Several pharmaceutical and academic institutions have ongoing resea...
Interest in sphingosine-1-phosphate (S1P)(1) receptor agonists has increased steadily since the discovery that the mechanism of action of fingolimod (FTY-720)-induced lymphopenia is linked to the S1P GPCR family. Fingoli...
Since 2008, significant advances have been made in understanding the role of diacylglycerol acyl transferase-1 (DGAT1) in disease states such as diabetes and obesity. Gene deletion and overexpression studies have provide...
Antiplatelet therapy is a crucial component of disease management for patients with acute coronary syndromes or chronic stable coronary disease, as well as individuals undergoing percutaneous coronary intervention with s...