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P-glycoprotein-mediated resistance to chemotherapy in cancer cells: using recombinant cytosolic domains to establish structure-function relationships BJMBR
Di Pietro,A.; Dayan,G.; Conseil,G.; Steinfels,E.; Krell,T.; Trompier,D.; Baubichon-Cortay,H.; Jault,J.-M..
Resistance to chemotherapy in cancer cells is mainly mediated by overexpression of P-glycoprotein (Pgp), a plasma membrane ATP-binding cassette (ABC) transporter which extrudes cytotoxic drugs at the expense of ATP hydrolysis. Pgp consists of two homologous halves each containing a transmembrane domain and a cytosolic nucleotide-binding domain (NBD) which contains two consensus Walker motifs, A and B, involved in ATP binding and hydrolysis. The protein also contains an S signature characteristic of ABC transporters. The molecular mechanism of Pgp-mediated drug transport is not known. Since the transporter has an extraordinarily broad substrate specificity, its cellular function has been described as a "hydrophobic vacuum cleaner". The limited knowledge...
Tipo: Info:eu-repo/semantics/article Palavras-chave: P-glycoprotein (Pgp); Multidrug resistance; Anticancer chemotherapy; ATP; Steroids; Flavonoids.
Ano: 1999 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X1999000800001
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