A LARGE superfamily of receptors containing seven transmembrane (TM) helices transmits
hormonal and sensory signals across the plasma membrane to heterotrimeric G proteins at …

A method was developed to measure Fourier-transform infrared (FTIR) difference spectra of
detergent-solubilized rhodopsin expressed in COS cells. Experiments were performed on …

Six proton pump inhibitors (PPIs), omeprazole, lansoprazole, esomeprazole, dexlansoprazole,
pantoprazole, and rabeprazole, were shown to be weak inhibitors of cytochromes P450 (…

The discovery of asunaprevir (BMS-650032, 24) is described. This tripeptidic acylsulfonamide
inhibitor of the NS3/4A enzyme is currently in phase III clinical trials for the treatment of …

An automated process is described for the detailed assessment of the in vitro metabolic
stability properties of drug candidates in support of pharmaceutical property profiling. …

The bile salt export pump (BSEP) is located on the canalicular plasma membrane of hepatocytes
and plays an important role in the biliary clearance of bile acids (BAs). Therefore, any …

Rhodopsin is a seven-transmembrane helix receptor that binds and catalytically activates the
heterotrimeric G protein transducin (G t ). This interaction involves the cytoplasmic surface …

The discovery of BMS-605339 (35), a tripeptidic inhibitor of the NS3/4A enzyme, is described.
This compound incorporates a cyclopropylacylsulfonamide moiety that was designed to …

Liquid chromatography/tandem mass spectrometry (LC/MS/MS) is the bioanalytical method
of choice to support plate‐based, in vitro early ADME (Absorption, Distribution, Metabolism …

Iterative structure–activity analyses in a class of highly functionalized furo[2,3-b]pyridines
led to the identification of the second generation pan-genotypic hepatitis C virus NS5B …