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  • One of several potential approaches to study mechanisms of action of biologically active compounds is to develop their agonists and antagonists. In the present study, we report the identification of the first known molecule antagonizing the activity of the plant hormone cytokinin at the receptor level. This compound, 6-(2-hydroxy-3-methylbenzylamino)purine, designated PI-55 in the present study, is structurally closely related to cytokinin 6-benzylaminopurine, but substitutions at specific positions of the aromatic side chain strongly diminished its cytokinin activity and conferred antagonistic properties. PI-55 competitively inhibited the binding of the natural ligand trans-zeatin to the Arabidopsis cytokinin receptors cytokinin response 1 (CRE1)/Arabidopsis histidine kinase (AHK) 4 and AHK3 and repressed induction of the cytokinin response gene ARR5:GUS. Genetic analysis revealed that CRE1/AHK4 is the primary target of PI-55. Cytokinin bioassays also demonstrated the anticytokinin
  • One of several potential approaches to study mechanisms of action of biologically active compounds is to develop their agonists and antagonists. In the present study, we report the identification of the first known molecule antagonizing the activity of the plant hormone cytokinin at the receptor level. This compound, 6-(2-hydroxy-3-methylbenzylamino)purine, designated PI-55 in the present study, is structurally closely related to cytokinin 6-benzylaminopurine, but substitutions at specific positions of the aromatic side chain strongly diminished its cytokinin activity and conferred antagonistic properties. PI-55 competitively inhibited the binding of the natural ligand trans-zeatin to the Arabidopsis cytokinin receptors cytokinin response 1 (CRE1)/Arabidopsis histidine kinase (AHK) 4 and AHK3 and repressed induction of the cytokinin response gene ARR5:GUS. Genetic analysis revealed that CRE1/AHK4 is the primary target of PI-55. Cytokinin bioassays also demonstrated the anticytokinin (en)
Title
  • The purine derivative PI-55 blocks cytokinin action via receptor inhibition
  • The purine derivative PI-55 blocks cytokinin action via receptor inhibition (en)
skos:prefLabel
  • The purine derivative PI-55 blocks cytokinin action via receptor inhibition
  • The purine derivative PI-55 blocks cytokinin action via receptor inhibition (en)
skos:notation
  • RIV/61989592:15310/09:00009953!RIV10-MSM-15310___
http://linked.open...avai/riv/aktivita
http://linked.open...avai/riv/aktivity
  • P(GP522/07/P197), P(LC06034), Z(AV0Z50380511), Z(MSM6198959216)
http://linked.open...iv/cisloPeriodika
  • 1
http://linked.open...vai/riv/dodaniDat
http://linked.open...aciTvurceVysledku
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http://linked.open...iv/duvernostUdaju
http://linked.open...titaPredkladatele
http://linked.open...dnocenehoVysledku
  • 337700
http://linked.open...ai/riv/idVysledku
  • RIV/61989592:15310/09:00009953
http://linked.open...riv/jazykVysledku
http://linked.open.../riv/klicovaSlova
  • anticytokinin; cytokinin; cytokinin receptor; cytokinin receptor antagonist; hormone signaling (en)
http://linked.open.../riv/klicoveSlovo
http://linked.open...odStatuVydavatele
  • GB - Spojené království Velké Británie a Severního Irska
http://linked.open...ontrolniKodProRIV
  • [90848B008C0D]
http://linked.open...i/riv/nazevZdroje
  • F E B S Journal
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http://linked.open...ichTvurcuVysledku
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http://linked.open...vavai/riv/projekt
http://linked.open...UplatneniVysledku
http://linked.open...v/svazekPeriodika
  • 276
http://linked.open...iv/tvurceVysledku
  • Strnad, Miroslav
  • Spíchal, Lukáš
  • Popa, Igor
  • Werner, Tomáš
  • Schmülling, Thomas
  • Riefler, Michael
http://linked.open...n/vavai/riv/zamer
issn
  • 1742-464X
number of pages
http://localhost/t...ganizacniJednotka
  • 15310
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