About: Role of negatively charged amino acids in beta4 F-loop in activation and desensitization of alfa3beta4 rat neuronal nicotinic receptors     Goto   Sponge   NotDistinct   Permalink

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  • Mutation of aspartates in positions 191 and 192 of the F-loop of beta4 subunit to their uncharged analogs asparagines led to a receptor with lowered rate of desensitization and accelerated resensitization of responses to agonists as measured by whole-cell patch-clamp technique. Sensitivity of the mutated receptors to ligands is shifted towards higher concentrations, which is substantially more pronounced in case of agonists than in competitive antagonist. Some agonists did not activate the mutated variant of the receptor at all but their ability to bind was preserved and such ligands acted as competitive antagonists of the mutated receptors. Concluding: aspartates in the loop F do not directly take part in ligand binding but they are essential for proper receptor gating
  • Mutation of aspartates in positions 191 and 192 of the F-loop of beta4 subunit to their uncharged analogs asparagines led to a receptor with lowered rate of desensitization and accelerated resensitization of responses to agonists as measured by whole-cell patch-clamp technique. Sensitivity of the mutated receptors to ligands is shifted towards higher concentrations, which is substantially more pronounced in case of agonists than in competitive antagonist. Some agonists did not activate the mutated variant of the receptor at all but their ability to bind was preserved and such ligands acted as competitive antagonists of the mutated receptors. Concluding: aspartates in the loop F do not directly take part in ligand binding but they are essential for proper receptor gating (en)
  • Mutační změna aspartátů v pozici 191 a 192 nacházejících se v F-kličce beta4 podjednotky na nenabité asparaginy vedla k receptoru se sníženou rychlostí desenzitizace a zrychlenou resenzitizací odpovědí na aplikaci agonisty měřených metodou patch-clamp v režimu whole-cell. Závislost citlivosti mutovaných receptorů k ligandům byla posunuta k vyšším koncentracím oproti wild-typu a to podstatně více u agonistů než u kompetitivního antagonisty. Někteří agonisté neaktivovali mutovanou variantu receptoru vůbec, ačkoliv schopnost vazby byla zachována, a tyto látky se chovaly jako kompetitivní antagonisté mutovaných receptorů. Souhrnem: aspartáty v kličce F se nepodílí přímo na vazbě ligandů, jsou však nezbytné pro správné vrátkování (gating) receptoru (cs)
Title
  • Role of negatively charged amino acids in beta4 F-loop in activation and desensitization of alfa3beta4 rat neuronal nicotinic receptors
  • Role of negatively charged amino acids in beta4 F-loop in activation and desensitization of alfa3beta4 rat neuronal nicotinic receptors (en)
  • Role negativně nabitých aminokyselin v F-kličce beta4 podjednotky při aktivaci a desenzitizaci alfa3beta4 potkaního neuronálního nikotinického receptoru (cs)
skos:prefLabel
  • Role of negatively charged amino acids in beta4 F-loop in activation and desensitization of alfa3beta4 rat neuronal nicotinic receptors
  • Role of negatively charged amino acids in beta4 F-loop in activation and desensitization of alfa3beta4 rat neuronal nicotinic receptors (en)
  • Role negativně nabitých aminokyselin v F-kličce beta4 podjednotky při aktivaci a desenzitizaci alfa3beta4 potkaního neuronálního nikotinického receptoru (cs)
skos:notation
  • RIV/67985823:_____/08:00306860!RIV08-AV0-67985823
http://linked.open.../vavai/riv/strany
  • 864;871
http://linked.open...avai/riv/aktivita
http://linked.open...avai/riv/aktivity
  • P(IAA100110501), P(IAA5011411), P(LC554), Z(AV0Z50110509)
http://linked.open...iv/cisloPeriodika
  • 4
http://linked.open...vai/riv/dodaniDat
http://linked.open...aciTvurceVysledku
http://linked.open.../riv/druhVysledku
http://linked.open...iv/duvernostUdaju
http://linked.open...titaPredkladatele
http://linked.open...dnocenehoVysledku
  • 393198
http://linked.open...ai/riv/idVysledku
  • RIV/67985823:_____/08:00306860
http://linked.open...riv/jazykVysledku
http://linked.open.../riv/klicovaSlova
  • F-loop; alpha3 beta4; epibatidine (en)
http://linked.open.../riv/klicoveSlovo
http://linked.open...odStatuVydavatele
  • NL - Nizozemsko
http://linked.open...ontrolniKodProRIV
  • [DE16042B19E6]
http://linked.open...i/riv/nazevZdroje
  • Biochimica Et Biophysica Acta-Biomembranes
http://linked.open...in/vavai/riv/obor
http://linked.open...ichTvurcuVysledku
http://linked.open...cetTvurcuVysledku
http://linked.open...vavai/riv/projekt
http://linked.open...UplatneniVysledku
http://linked.open...v/svazekPeriodika
  • 1778
http://linked.open...iv/tvurceVysledku
  • Vyskočil, František
  • Kaniaková, Martina
  • Krůšek, Jan
  • Lindovský, Jiří
  • Svobodová, Lucie
http://linked.open...n/vavai/riv/zamer
issn
  • 0005-2736
number of pages
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