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Using Structural and Mechanistic Information to Design Novel Inhibitors/Substrates of P-Glycoprotein

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Design of inhibitors of P-glycoprotein still represents a challenging task for medicinal chemists. The polyspecificity of the transporter combined with the limited structural information renders rational drug design approaches rather ineffective. Within this article we will exemplify how recent insights into structure and mechanism of Pglycoprotein may aid in design of potent inhibitors.


Keywords: ATP-binding cassette; ATPases; ATPbinding site; Blood brain barrier; Bosutinib; Breast cancer related protein; Central nervous system; Cyclic peptide P-glycoprotein inhibitor; Cytochrome P450-3A4; Dasatinib; Dopamine transporter; GABAA receptor; Ligand docking; MDR; Multidrug resistance; NCI-60 screening; Nilotinib; Norepinephrine transporter; Nucleotide binding domain; Pharmacophore modeling; Positron emission tomography; Protein-ligand interaction fingerprints; Quinazolinones; Radiolabeled P-gp substrates; SAV1866; Serotonine reuptake transporter; Single-photon emission computed tomography; Structure activity relationship; Transmembrane domain; Tyrosine kinases (TKs)

Document Type: Research Article


Affiliations: Medical University of Vienna, Institute of Medical Chemistry, Waehringer Strasse 10, 1090 Wien, Austria.

Publication date: December 1, 2010


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