P-glycoprotein (P-gp/MDR1)/ABCB1

摘要: The ABCB1 gene was cloned from non-polarized tumor cells where it confers multidrug resistance. P-gp is also expressed on organ barriers plays a protective role and affects the ADME of drugs. causes clinically significant DDIs, particularly for those drugs with narrow therapeutic index. Regulatory agencies require potential DDI risk to be evaluated in drug development. limits entry substrate into brain; therefore, selection during discovery process must involve rational design engineer out interactions centrally acting or, instead, integrate as beneficial factors reduced CNS side effects. Considerable species differences expression function exist. While Mdr duplicated by Mdr1a Mdr1b preclinical species, single MDR1-encoded humans fulfills functions two isoforms. are associated physiological pathophysiological conditions such pathogenesis Alzheimer’s disease. It could become new target treatment Developing modulator chemotherapy through restoring sensitivity anticancer reagents has emerged focus pharmaceutical industry. However, clinical studies modulators not encouraging because toxicity profiles have been improved.