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I have engaged in a great deal of reading on human intestinal efflux
transporters. The ones that seem to be "significant" are: BRCP,
ISBT, LRP, MRP-1, MRP-2, MDR-1 (PGP) and PEPT1. My question is
simple. How does one take a new chemical entity (NCE) and test to
see if any of these is an active efflux transporter in humans. Of
course, PGP is easy to do with CACO-2 cells. But what about the
rest. The literature is replete with references and lots of genetic
information, but a "synthesis of thought" (e.g., a good review
article) on practical testing seems to be elusive. Any help would be
greatly appreciated. Thanks, Harold.
Harold Boxenbaum, Ph.D.
14621 Settlers Landing Way
North Potomac, MD 20878-4305
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