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@ARTICLE{Pissarek:828052,
      author       = {Pissarek, Margit},
      title        = {{S}mall {M}olecule-{A}ssisted {PET}: {A}pproaches to
                      {I}maging of {C}onformational {D}iseases of the {B}rain},
      journal      = {World Journal of Neuroscience},
      volume       = {7},
      issn         = {2162-2000},
      address      = {Irvine, CA},
      publisher    = {Scientific Research Publ.},
      reportid     = {FZJ-2017-02066},
      pages        = {106-139},
      year         = {2017},
      abstract     = {PET (positron emission tomography) in vivo imaging of
                      cerebral conformationaldiseases is essentially based on
                      non-peptide small molecule ligands usedto detect early
                      alterations in peptide secondary structures and subsequent
                      accumulationof aberrant oligomers and protein deposits
                      involved in progressiveneurodegeneration, cognitive and
                      movement disorders. In this article, anoverview is given
                      about tracers currently available and lead structures of
                      potentialPET probes for detection of ß-amyloid (Aß), tau
                      protein, α-synuclein,constitutive (PrPc) and infectious
                      isoforms (PrPsc) of prions (proteinaceousinfectious
                      particles) as imaging targets. Whereas the styrylpyridine
                      derivativeflorbetapir, approved for clinical applications,
                      the stilbene derivative florbetabenand the benzoxazole
                      derivative BF227 show high affinity binding to
                      Aß,preclinical investigations promise improved
                      pharmacokinetics for benzoimidazothiazoles,aryloxazoles and
                      benzofuran derivatives. Tau protein imagingbased clinically,
                      presently, on the pyridine-pyridoindole T807 has got new
                      incentivesfollowing identification of a series of
                      pyrrolopyridine quinolines andpharmacokinetic improvements
                      of fluoropropoxy quinolines including for instanceTHK-5351.
                      The pyridine isoquinoline MK6240 is involved now inclinical
                      trials. Most forward-looking efforts apply to small molecule
                      ligands ofα-synuclein, which are expected to permit a
                      breakthrough in differential diagnosticsof Parkinson-related
                      dementia and Lewy body diseases. However, atthe moment the
                      proposed lead structures are in affinity and blood brain
                      barrierdelivery properties below the possibilities of Aß
                      and tau protein ligands.This is the case also for potential
                      tracers of prion proteins.},
      cin          = {INM-5},
      ddc          = {610},
      cid          = {I:(DE-Juel1)INM-5-20090406},
      pnm          = {315 - Imaging and radiooncology (POF3-315) / 342 - Disease
                      Mechanisms and Model Systems (POF3-342)},
      pid          = {G:(DE-HGF)POF3-315 / G:(DE-HGF)POF3-342},
      typ          = {PUB:(DE-HGF)16},
      doi          = {10.4236/wjns.2017.71010},
      url          = {https://juser.fz-juelich.de/record/828052},
}