A macrocyclic peptide inhibitor traps MRP1 in a catalytically incompetent conformation
Pietz H, Abbas A, Johnson Z, Oldham M, Suga H, Chen J. A macrocyclic peptide inhibitor traps MRP1 in a catalytically incompetent conformation. Proceedings Of The National Academy Of Sciences Of The United States Of America 2023, 120: e2220012120. PMID: 36893260, PMCID: PMC10089224, DOI: 10.1073/pnas.2220012120.Peer-Reviewed Original ResearchConceptsMultidrug resistance protein 1MRP1 overexpressionSubstrate transportAdenosine triphosphate-binding cassetteCatalytically incompetent conformationStructurally unrelated moleculesCpI1Small molecule inhibitorsAdenosine triphosphatePlasma membraneA-resolutionCryoelectron microscopyCryo-EMUnrelated moleculesConformational changesMultidrug resistanceMRP1 functionProtein 1Macrocyclic peptidesMultidrug transporter P-glycoproteinFlexible sidechainsXenobiotic compoundsNanomolar potencyCellular toxicityTherapeutic candidate
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