Cytochrome P450 enzymes function to metabolize both endogenous and exogenous compounds. Both the 3A and 2C isoforms are present in human liver of which CYP2C9 seems most highly expressed. Tienilic acid is a specific suicide substrate for CYP2C9 and CYP2C10 whereby its oxidation inactivates the enzyme. The time...

Arachidonyl ethanolamide (AEA) is an endogenous lipid neurotransmitter with cannabinergic activity, binding to both the central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptors. Fatty acid amide hydrolase (FAAH) is the enzyme responsible for the hydrolysis and inactivation of AEA. Metabolism of AEA by...

The PtdIns phosphates play an important role in the generation and transduction of intracellular signals. PtdIns-(4,5)-P2-biotin is an affinity probe which allows the PIP2 to be detected through an interaction with the biotin ligand. This design allows PtdIns-(4,5)-P2 to serve as a general probe for any protein with...

Central cannabinoid (CB1) receptor antagonists and inverse agonists exhibit therapeutic potential for obesity and drug dependence, while being devoid of psychotropic effects. CAY10508 is a potent and selective central cannabinoid (CB1) receptor inverse agonist with a Ki value of 243 nM and an EC50 of 195 nM. A 10 µM...

PX-478 suppresses both constitutive and hypoxia-induced levels of HIF-1alpha in cancer cells, resulting in reduced expression of HIF-1alpha target genes. It induces apoptosis in human tumor xenografts in mice to an extent that is proportional to initial HIF-1alpha level. PX-478 can also increase chemo- or...