[Structure and function of P-glycoprotein].
P-glycoprotein is a membrane ATPase transporter responsible for multidrug resistance. Its primary structure is known from cDNA sequencing, but its tri-dimension structure remains hypothetical. Its physiological role in detoxification, as well as its involvement in anticancer drug transport, are no longer questioned, but its molecular mechanism of action remains unknown. It appears likely that it extrudes the drugs laterally, in the plane of the membrane, that several distinct drug or modulator binding sites exist, that its activity is regulated by phosphorylation. Purification and reconstitution of P-glycoprotein will probably allow to better understand its mechanism of action.
Robert
J
J
Fondation Bergonié et université de Bordeaux II, France.
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000235:genetics / Q000378:metabolism / Q000502:physiology; D000970:Antineoplastic Agents / Q000627:therapeutic use; D001665:Binding Sites; D002352:Carrier Proteins / Q000378:metabolism; D018118:Chloride Channels / Q000378:metabolism; D018432:Drug Resistance, Multiple; D006801:Humans; D008954:Models, Biological; D008969:Molecular Sequence Data; D017434:Protein Structure, Tertiary; D013329:Structure-Activity Relationship
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D000970:Antineoplastic Agents; D002352:Carrier Proteins; D018118:Chloride Channels
Structure et fonction de la glycoprotéine P.