Membrane transporters can have clinically relevant effects on the pharmacokinetics and pharmacodynamics of a drug in various organs and tissues by controlling its absorption, distribution and elimination. Together with metabolizing enzymes, they can drive a drug’s pharmacological action, as well as a drug can modulate transporter expression or activity, hence the importance of evaluating transporter-mediated drug-drug interactions recommended by the FDA guidelines. Genomembrane have developed transiently expressing ready-to-use cells to study FDA approved transporters (TransiPort). I had described this product range and their unique features in a previous post. I would like to introduce in this one 2 newly released cells overexpressing OATP1A2 and OATP2B1 transporters.
NADPH is a critical cofactor supporting numerous biochemical reactions. In ADME-Tox studies, NAD(P)H regeneration is strongly recommended when using drug metabolizing enzymes (ex. Cytochrome P450 (CYP), Flavin-containing MonoOxygenases (FMO)), Recombinant CYPs (incl. bactosomes) or cellular fractions (Microsomes, S9). Currently, the most simple and cost-effective way to regenerate the NAD(P)H in situ and enzymatically is to use the commercially-available RapidStart™ NADPH Regenerating System (Xenotech-Sekisui).
RapidStart uses an enzymatic reaction that changes NADP to NADPH, which is then oxidized by CYPs back to NADP, and the cycle continues…
Following up on my series of posts based on Dr Chris Bohl’s work at Sekisui Xenotech, in this post I invite you to take a look at the work he has published, together with Dr Christopher Seib, Maciej Czerwinski, Zell Woodworth and David Buckley, Ph.D., illustrating the characterization of isolated human liver lysosomes, and validating them as test systems for in vitro assessment of catabolic stability of biologics drugs entering the cell by the endosomal–lysosomal pathway.
In a few forthcoming posts, I’d like to share several short articles published by Dr Chris Bohl of Sekisui Xenotech, a technical expert in the field of ADME-Tox tools and applications. I feel they may be of special interest to researchers working in the field of ADME-Tox studies.
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