Dennis C. Dean

TL;DR: A heterotrimeric GTP-binding protein (G protein)-coupled receptor (GPC-R) of the pituitary and arcuate ventro-medial and infundibular hypothalamus of swine and humans was cloned and was shown to be the target of the GHSs.

TL;DR: A binding assay is developed and shown that labeled ezetimibe glucuronide binds specifically to a single site in brush border membranes and to human embryonic kidney 293 cells expressing NPC1L1, which unequivocally establish NPC1 L1 as the direct target of ezETimibe and should facilitate efforts to identify the molecular mechanism of cholesterol transport.

TL;DR: The finding that metabolism of the TZD ring of troglitazone was catalyzed selectively by P450 3A enzymes is significant in light of the recent report that trog litazone is an inducer of this isoform in human hepatocytes.

TL;DR: A specific high affinity binding site in porcine and rat anterior pituitary membranes that mediates the activity of these secretagogues has now been identified and is tightly correlated with GH-secretory activity.

TL;DR: The data suggest that diclofenac undergoes biotransformation to reactive metabolites in rats and that CYP isoforms of the 2B, 2C, and 3A subfamilies are involved in this bioactivation process.