Skip to main content

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

Buy Article:

$55.00 plus tax (Refund Policy)

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.

P>
No References
No Citations
No Supplementary Data
No Article Media
No Metrics

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: 2010-12-01

  • Access Key
  • Free content
  • Partial Free content
  • New content
  • Open access content
  • Partial Open access content
  • Subscribed content
  • Partial Subscribed content
  • Free trial content
Cookie Policy
X
Cookie Policy
Ingenta Connect website makes use of cookies so as to keep track of data that you have filled in. I am Happy with this Find out more