[Effect of genetic polymorphism on the activity of drug transporters and its clinical significance].
Drug transport is an important source of inter-individual variations in drug responses and is also a common site where drug-drug interactions happen. In recent years, more and more novel identified transporters have been added into the transporter super family, and this trend will continue in the future. Among the transporter members of this family, ATP-dependent efflux transporter P-glycoprotein (MDR1) and organic anion transporters (OATP) are the most important proteins involved in drug transport. MDR1 is the most well known transporter. Widely distributed in tissues such as the gastrointestinal tract, liver, kidney and so on, MDR1 plays an important role in drug absorption, distribution and excretion. Its functional genetic polymorphisms have significantly changed the pharmacokinetics of its substrate drugs, which has important clinical implications. OATP expressed in multiple tissues, and it mediated the drug excretion through the bile acid and kidney. Some genetic polymorphism of OATP genes is the cause of some abnormal drug responses.
Zhang
Hai-xia
HX
Institute of Clinical Pharmacology, Central South University, Changsha 410078, China.
Wang
Lian-sheng
LS
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000235:genetics*; D004347:Drug Interactions / Q000235:genetics; D006801:Humans; D026901:Membrane Transport Proteins / Q000235:genetics / Q000378:metabolism*; D027361:Organic Anion Transporters / Q000235:genetics*; D004364:Pharmaceutical Preparations / Q000378:metabolism; D011110:Polymorphism, Genetic
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D026901:Membrane Transport Proteins; D027361:Organic Anion Transporters; D004364:Pharmaceutical Preparations