2018
Molecular mechanism underlying the subtype-selectivity of competitive inhibitor NF110 and its distinct potencies in human and rat P2X3 receptors
Li B, Wang J, Cheng X, Liu Y, Yang Y, Yang X, Guo C, Niu Y, Cao P, Lu X, Zhu M, Tian Y, Yu Y. Molecular mechanism underlying the subtype-selectivity of competitive inhibitor NF110 and its distinct potencies in human and rat P2X3 receptors. Science Bulletin 2018, 63: 1616-1625. PMID: 36658853, DOI: 10.1016/j.scib.2018.11.016.Peer-Reviewed Original ResearchP2X3 receptorsP2X receptorsExperimental animalsDifferent P2X receptorsLower bodyRat P2X3 receptorsDistinct potenciesSubtype-selective mannerHuman P2X3 receptorsLF domainInhibitors/modulatorsPreclinical dataClinical trialsAmino acidsEquivalent amino acidsATP-binding pocketClinical researchExtracellular ATPSubstitution of residuesReceptorsCation channelsPharmacological activitiesDorsal fin domainInhibitory efficacyChannel activity
2017
Selective Calcium-Dependent Inhibition of ATP-Gated P2X3 Receptors by Bisphosphonate-Induced Endogenous ATP Analog ApppI
Ishchenko Y, Shakirzyanova A, Giniatullina R, Skorinkin A, Bart G, Turhanen P, Määttä J, Mönkkönen J, Giniatullin R. Selective Calcium-Dependent Inhibition of ATP-Gated P2X3 Receptors by Bisphosphonate-Induced Endogenous ATP Analog ApppI. Journal Of Pharmacology And Experimental Therapeutics 2017, 361: 472-481. PMID: 28404687, DOI: 10.1124/jpet.116.238840.Peer-Reviewed Original ResearchConceptsNitrogen-Containing BisphosphonatesP2X3 receptorsP2X7 receptorBone cancerInhibitory actionBone resorptive disordersNodose ganglion neuronsRat sensory neuronsPrimary bone cancerRat P2X3 receptorsPatch-clamp techniqueWeak agonist activityCalcium-dependent inhibitionBone metastasesTrigeminal neuronsPurinergic mechanismsUnbearable symptomsGanglion neuronsReceptor subtypesSensory neuronsP2X receptorsPathologic processesAgonist activityHuman P2X3Human embryonic kidney cells
This site is protected by hCaptcha and its Privacy Policy and Terms of Service apply