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@ARTICLE{Maleeva:889058,
      author       = {Maleeva, Galyna and Nin-Hill, Alba and Rustler, Karin and
                      Petukhova, Elena and Ponomareva, Daria and Mukhametova,
                      Elvira and Gomila-Juaneda, Alexandre and Wutz, Daniel and
                      Alfonso-Prieto, Mercedes and König, Burkhard and Gorostiza,
                      Pau and Bregestovski, Piotr},
      title        = {{S}ubunit-specific photocontrol of glycine receptors by
                      azobenzene-nitrazepam photoswitcher},
      journal      = {eNeuro},
      volume       = {8},
      number       = {1},
      issn         = {2373-2822},
      address      = {Washington, DC},
      publisher    = {Society for Neuroscience},
      reportid     = {FZJ-2021-00002},
      pages        = {ENEURO.0294-20.2020},
      year         = {2021},
      abstract     = {Photopharmacology is a unique approach that through a
                      combination of photochemistry methods and advanced life
                      science techniques allows the study and control of specific
                      biological processes, ranging from intracellular pathways to
                      brain circuits. Recently, a first photochromic channel
                      blocker of anion-selective GABAA receptors, Azo-NZ1, has
                      been described. In the present study using patch-clamp
                      technique in heterologous system and in mice brain slices,
                      site-directed mutagenesis and molecular modelling we provide
                      evidence of the interaction of Azo-NZ1 with glycine
                      receptors (GlyRs) and determine the molecular basis of this
                      interaction. Glycinergic synaptic neurotransmission
                      determines an important inhibitory drive in the vertebrate
                      nervous system and plays a crucial role in the control of
                      neuronal circuits in the spinal cord and brain stem. GlyRs
                      are involved in locomotion, pain sensation, breathing and
                      auditory function, as well as in the development of such
                      disorders as hyperekplexia, epilepsy and autism. Here we
                      demonstrate that Azo-NZ1 blocks in a UV dependent manner the
                      activity of alpha2 GlyRs (GlyR2), while being barely active
                      on alpha1 GlyRs (GlyR1). The site of Azo-NZ1 action is in
                      the chloride-selective pore of GlyR at the 2’ position of
                      transmembrane helix 2 and amino acids forming this site
                      determine the difference in Azo-NZ1 blocking activity
                      between GlyR2 and GlyR1. This subunit specific modulation is
                      also shown on motoneurons of brainstem slices from neonatal
                      mice that switch during development from expressing "foetal"
                      GlyR2 to "adult" GlyR1 receptors.},
      cin          = {IAS-5 / INM-9},
      ddc          = {610},
      cid          = {I:(DE-Juel1)IAS-5-20120330 / I:(DE-Juel1)INM-9-20140121},
      pnm          = {5241 - Molecular Information Processing in Cellular Systems
                      (POF4-524) / 5251 - Multilevel Brain Organization and
                      Variability (POF4-525) / 5252 - Brain Dysfunction and
                      Plasticity (POF4-525)},
      pid          = {G:(DE-HGF)POF4-5241 / G:(DE-HGF)POF4-5251 /
                      G:(DE-HGF)POF4-5252},
      typ          = {PUB:(DE-HGF)16},
      pubmed       = {33298457},
      UT           = {WOS:000641967200007},
      doi          = {10.1523/ENEURO.0294-20.2020},
      url          = {https://juser.fz-juelich.de/record/889058},
}