ArticleMolecular pharmacology2014
Pore-exposed tyrosine residues of P-glycoprotein are important hydrogen-bonding partners for drugs.
Article in Molecular pharmacology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
20 citing papers in PubMed, 31 citations in OpenAlex.
- From vibrations to function: Spectroscopic detection and quantification of π-π stacking in drug-responsive protein complexes.Science advances · 2026Article
- From nicotine to SARS-CoV-2 antivirals with potent in vivo efficacy and a broad anti-coronavirus spectrum.Nature communications · 2026Article
- Mass Spectrometry Investigation of Some ATP-Binding Cassette (ABC) Proteins.Medicina (Kaunas, Lithuania) · 2024Review
- A Unique In Vitro Assay to Investigate ABCB4 Transport Function.International journal of molecular sciences · 2023Article
- Extended-ensemble docking to probe dynamic variation of ligand binding sites during large-scale structural changes of proteins.Chemical science · 2022Article
- Identification and characterisation of putative drug binding sites in human ATP-binding cassette B5 (ABCB5) transporter.Computational and structural biotechnology journal · 2021Article
- Computational Insights into Allosteric Conformational Modulation of P-Glycoprotein by Substrate and Inhibitor Binding.Molecules (Basel, Switzerland) · 2020Article
- The role of the degenerate nucleotide binding site in type I ABC exporters.FEBS letters · 2020Review
- Review
- Novel Nonsymmetrical 1,4-Dihydropyridines as Inhibitors of Nonsymmetrical MRP-Efflux Pumps for Anticancer Therapy.Pharmaceuticals (Basel, Switzerland) · 2020Article
- Active transport of rhodamine 123 by the human multidrug transporter P-glycoprotein involves two independent outer gates.Pharmacology research & perspectives · 2020Article
- The ABCG2 multidrug transporter is a pump gated by a valve and an extracellular lid.Nature communications · 2019Article
- Evidence for the Interaction of AMolecular pharmacology · 2019Article
- Comparison of mechanistic transport cycle models of ABC exporters.Biochimica et biophysica acta. Biomembranes · 2018Review
- Molecular Mechanism of Taurocholate Transport by the Bile Salt Export Pump, an ABC Transporter Associated with Intrahepatic Cholestasis.Molecular pharmacology · 2017Article
- Folding correction of ABC-transporter ABCB1 by pharmacological chaperones: a mechanistic concept.Pharmacology research & perspectives · 2017Article
- Interactions of retinoids with the ABC transporters P-glycoprotein and Breast Cancer Resistance Protein.Scientific reports · 2017Article
- Drug-protein hydrogen bonds govern the inhibition of the ATP hydrolysis of the multidrug transporter P-glycoprotein.Biochemical pharmacology · 2016Article
- In vitro and in vivo downregulation of the ATP binding cassette transporter B1 by the HMG-CoA reductase inhibitor simvastatin.Naunyn-Schmiedeberg's archives of pharmacology · 2016Article
- Molecular basis of the polyspecificity of P-glycoprotein (ABCB1): recent biochemical and structural studies.Advances in cancer research · 2015Review
Corrections and comments
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Authors and funding
10 authors at 4 institutions in 2 countries.
Funding
Abstract
The multispecific efflux transporter, P-glycoprotein, plays an important role in drug disposition. Substrate translocation occurs along the interface of its transmembrane domains. The rotational C2 symmetry of ATP-binding cassette transporters implies the existence of two symmetry-related sets of substrate-interacting amino acids. These sets are identical in homodimeric transporters, and remain evolutionary related in full transporters, such as P-glycoprotein, in which substrates bind preferentially, but nonexclusively, to one of two binding sites. We explored the role of pore-exposed tyrosines for hydrogen-bonding interactions with propafenone type ligands in their preferred binding site 2. Tyrosine 953 is shown to form hydrogen bonds not only with propafenone analogs, but also with the preferred site 1 substrate rhodamine123. Furthermore, an accessory role of tyrosine 950 for binding of selected propafenone analogs is demonstrated. The present study demonstrates the importance of domain interface tyrosine residues for interaction of small molecules with P-glycoprotein.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.