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Statements

Subject Item
n2:RIV%2F68407700%3A21340%2F08%3A04155281%21RIV09-MSM-21340___
rdf:type
skos:Concept n18:Vysledek
dcterms:description
It has recently been found, that alcuronium and strychnine, respectively, enhance the binding of adiphenine, 4-DAMP, diphenylhydramine, diphenylpyraline, hyosciamine, N-piperidinyl benzilate, tropacine, scopolamine and some tricyclic antidepressants into orthosteric binding site at rat atrial (M2) receptors. Also, comparison of the kinetic data from studies with alcuronium, strychnine, gallamine, anatruxonium, truxillonium and diadonium, respectively, reveals different mechanisms of interaction with M2 receptors, though all ligands interact within a simple TCM. Multimodal binding and steric effects have been rather undervalued thus far in comparison with peculiarly intuitive concepts of multiple 'allosteric' binding sites and ligand induced conformation changes. In this work, a physical and terminological inconsistency of rather marketing term 'neutral cooperativity' is documented. It has recently been found, that alcuronium and strychnine, respectively, enhance the binding of adiphenine, 4-DAMP, diphenylhydramine, diphenylpyraline, hyosciamine, N-piperidinyl benzilate, tropacine, scopolamine and some tricyclic antidepressants into orthosteric binding site at rat atrial (M2) receptors. Also, comparison of the kinetic data from studies with alcuronium, strychnine, gallamine, anatruxonium, truxillonium and diadonium, respectively, reveals different mechanisms of interaction with M2 receptors, though all ligands interact within a simple TCM. Multimodal binding and steric effects have been rather undervalued thus far in comparison with peculiarly intuitive concepts of multiple 'allosteric' binding sites and ligand induced conformation changes. In this work, a physical and terminological inconsistency of rather marketing term 'neutral cooperativity' is documented. Použití fluorescenčních sond je jedním ze způsobů, jak překonat obtíže s použitím obvyklé metody vazby radioaktivně značených ligandů při studiu alosterické modulace muskarinových receptorů. Práce srovnává mechanismy interakcí klasických alosterických modulátorů s fluorescenčními akridinovými deriváty. Ukazuje se, přes rozdílnost individuálních mechanismů, že pro všechny testované ligandy je fyzikálním rámcem model ternárního komplexu.
dcterms:title
Nekompetitivní interakce na muskarinových receptorech v rámci modelu ternárního komplexu Noncompetitive interactions at muscarinic receptors within a simple ternary complex model Noncompetitive interactions at muscarinic receptors within a simple ternary complex model
skos:prefLabel
Noncompetitive interactions at muscarinic receptors within a simple ternary complex model Nekompetitivní interakce na muskarinových receptorech v rámci modelu ternárního komplexu Noncompetitive interactions at muscarinic receptors within a simple ternary complex model
skos:notation
RIV/68407700:21340/08:04155281!RIV09-MSM-21340___
n3:aktivita
n16:Z
n3:aktivity
Z(MSM6840770022)
n3:dodaniDat
n4:2009
n3:domaciTvurceVysledku
n12:1802364
n3:druhVysledku
n6:D
n3:duvernostUdaju
n14:S
n3:entitaPredkladatele
n10:predkladatel
n3:idSjednocenehoVysledku
382851
n3:idVysledku
RIV/68407700:21340/08:04155281
n3:jazykVysledku
n20:eng
n3:klicovaSlova
allosteric; proteins; ligand binding; muscarinic receptors
n3:klicoveSlovo
n8:allosteric n8:ligand%20binding n8:proteins n8:muscarinic%20receptors
n3:kontrolniKodProRIV
[347255F8540F]
n3:mistoKonaniAkce
Manchester
n3:mistoVydani
Oxford
n3:nazevZdroje
Fundamental and clinical pharmacology, volume 22, supplement 2, August 2008
n3:obor
n15:FR
n3:pocetDomacichTvurcuVysledku
1
n3:pocetTvurcuVysledku
1
n3:rokUplatneniVysledku
n4:2008
n3:tvurceVysledku
Proška, Jan
n3:typAkce
n19:WRD
n3:wos
000257551100384
n3:zahajeniAkce
2008-07-13+02:00
n3:zamer
n13:MSM6840770022
s:issn
0767-3981
s:numberOfPages
1
n17:hasPublisher
Blackwel Publisher
n9:organizacniJednotka
21340