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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},
}