Evaluation of substrate and inhibitor properties of a novel MDR modulator H17 towards transmembrane efflux pumps.

Basic Information

ID: ALA1152477

Journal: Eur J Med Chem

Title: Evaluation of substrate and inhibitor properties of a novel MDR modulator H17 towards transmembrane efflux pumps.

Authors: Richter M, Richter A, Langner A, Hilgeroth A.

Abstract: Substrate and inhibitor properties of H17 as novel modulator of transmembrane efflux pump activities have been characterized in an in situ absorption model. Poor substrate properties towards P-glycoprotein (P-gp) and multidrug resistance-associated protein (MRP) have been demonstrated. In competition with a MRP substrate H17 proved to have strong MRP-inhibiting properties. The profile of a strong inhibitor with poor substrate properties makes H17 a perspective hopeful candidate for effective therapies of transmembrane efflux pump activities.

CiteXplore: 18752872

DOI: 10.1016/j.ejmech.2008.07.014

Patent ID: