ArticleThe Journal of biological chemistry2011
Recognition of sulfonylurea receptor (ABCC8/9) ligands by the multidrug resistance transporter P-glycoprotein (ABCB1): functional similarities based on common structural features between two multispecific ABC proteins.
Article in The Journal of biological chemistry, 2011. 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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Who cites it
20 citing papers in PubMed, 30 citations in OpenAlex.
- Personalized Therapeutics for KAnnual review of pharmacology and toxicology · 2023Review
- The Rat Continuous Intestine Model Predicts the Impact of Particle Size and Transporters on the Oral Absorption of Glyburide.Molecular pharmaceutics · 2023Article
- KThe Journal of pharmacology and experimental therapeutics · 2021Article
- An Ancient CFTR Ortholog Informs Molecular Evolution in ABC Transporters.Developmental cell · 2019Article
- Article
- Structural model, functional modulation by ivermectin and tissue localization of Haemonchus contortus P-glycoprotein-13.International journal for parasitology. Drugs and drug resistance · 2018Article
- Diagnostic Value of Semiquantitative Analysis of 99mTechnetium-Methoxyisobutylisonitrile (99mTc-MIBI) Imaging in Predicting Early-Stage Cervical Lymph Node Metastasis of Thyroid Carcinoma.Medical science monitor : international medical journal of experimental and clinical research · 2017Article
- In silico analysis of the binding of anthelmintics to Caenorhabditis elegansP-glycoprotein 1.International journal for parasitology. Drugs and drug resistance · 2016Article
- The shifting landscape of KATP channelopathies and the need for 'sharper' therapeutics.Future medicinal chemistry · 2016Review
- Jump into a New Fold-A Homology Based Model for the ABCG2/BCRP Multidrug Transporter.PloS one · 2016Article
- Kir6.2 activation by sulfonylurea receptors: a different mechanism of action for SUR1 and SUR2A subunits via the same residues.Physiological reports · 2015Article
- Structurally distinct ligands rescue biogenesis defects of the KATP channel complex via a converging mechanism.The Journal of biological chemistry · 2015Article
- Systemic Administration of Glibenclamide Fails to Achieve Therapeutic Levels in the Brain and Cerebrospinal Fluid of Rodents.PloS one · 2015Article
- The unusual stoichiometry of ADP activation of the KATP channel.Frontiers in physiology · 2014Article
- The Sur1-Trpm4 Channel in Spinal Cord Injury.Journal of spine · 2013Article
- On the origin of large flexibility of P-glycoprotein in the inward-facing state.The Journal of biological chemistry · 2013Article
- The human transporter associated with antigen processing: molecular models to describe peptide binding competent states.The Journal of biological chemistry · 2012Article
- Divergent CFTR orthologs respond differently to the channel inhibitors CFTRinh-172, glibenclamide, and GlyH-101.American journal of physiology. Cell physiology · 2012Article
- Comparative effects of glibenclamide and riluzole in a rat model of severe cervical spinal cord injury.Experimental neurology · 2012Article
- Plant Lessons: Exploring ABCB Functionality Through Structural Modeling.Frontiers in plant science · 2011Article
Corrections and comments
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Authors and funding
9 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
ATP-sensitive K(+) (K(ATP)) channels are the target of a number of pharmacological agents, blockers like hypoglycemic sulfonylureas and openers like the hypotensive cromakalim and diazoxide. These agents act on the channel regulatory subunit, the sulfonylurea receptor (SUR), which is an ABC protein with homologies to P-glycoprotein (P-gp). P-gp is a multidrug transporter expressed in tumor cells and in some healthy tissues. Because these two ABC proteins both exhibit multispecific recognition properties, we have tested whether SUR ligands could be substrates of P-gp. Interaction with P-gp was assayed by monitoring ATPase activity of P-gp-enriched vesicles. The blockers glibenclamide, tolbutamide, and meglitinide increased ATPase activity, with a rank order of potencies that correlated with their capacity to block K(ATP) channels. P-gp ATPase activity was also increased by the openers SR47063 (a cromakalim analog), P1075 (a pinacidil analog), and diazoxide. Thus, these molecules bind to P-gp (although with lower affinities than for SUR) and are possibly transported by P-gp. Competition experiments among these molecules as well as with typical P-gp substrates revealed a structural similarity between drug binding domains in the two proteins. To rationalize the observed data, we addressed the molecular features of these proteins and compared structural models, computerized by homology from the recently solved structures of murine P-gp and bacterial ABC transporters MsbA and Sav1866. Considering the various residues experimentally assigned to be involved in drug binding, we uncovered several hot spots, which organized spatially in two main binding domains, selective for SR47063 and for glibenclamide, in matching regions of both P-gp and SUR.
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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.