Transcription of the multidrug resistance gene MDR1: a therapeutic target.
Two decades ago, the overexpression of P-glycoprotein (Pgp) was first demonstrated to mediate the energy-dependent efflux of a variety of chemotherapeutic agents from tumor cells, resulting in the development of multidrug resistance (MDR). Not surprisingly, this discovery triggered an ongoing search for agents that would inhibit Pgp function, with the hope that by doing so the MDR phenotype could be reversed. As our understanding of Pgp function and pharmacokinetics has increased, this quest has become more urgent, as well as more complex.
Scotto
K W
KW
Memorial Sloan-Kettering Cancer Center and, Weill Graduate School of Cornell University, 1275 York Avenue, New York, NY 10021, USA. k-scotto@mskmail.mskcc.org
Johnson
R A
RA
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000235:genetics* / Q000378:metabolism / Q000493:pharmacokinetics; D000818:Animals; D018906:Antineoplastic Agents, Alkylating / Q000737:chemistry / Q000627:therapeutic use*; D004149:Dioxoles / Q000737:chemistry / Q000627:therapeutic use*; D018432:Drug Resistance, Multiple / Q000235:genetics*; D019008:Drug Resistance, Neoplasm / Q000187:drug effects* / Q000235:genetics; D005544:Forecasting; D006801:Humans; D007546:Isoquinolines / Q000737:chemistry / Q000627:therapeutic use*; D008954:Models, Biological; D015394:Molecular Structure; D044005:Tetrahydroisoquinolines; D000077606:Trabectedin; D014158:Transcription, Genetic
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D018906:Antineoplastic Agents, Alkylating; D004149:Dioxoles; D007546:Isoquinolines; D044005:Tetrahydroisoquinolines; D000077606:Trabectedin