TY  - JOUR
AU  - Funke, S.A.
AU  - Bartnik, D.
AU  - Glück, J.M.
AU  - Pirkowska, K.
AU  - Wiesehan, K.
AU  - Weber, U.
AU  - Gulyas, B.
AU  - Halldin, C.
AU  - Pfeifer, A.
AU  - Spenger, C.
AU  - Muhs, A.
AU  - Willbold, D.
TI  - Development of a small D-enantiomeric Alzheimer's amyloid-beta binding peptide ligand for future in vivo imaging applications
JO  - PLoS one
VL  - 7
IS  - 7
SN  - 1932-6203
CY  - Lawrence, Kan.
PB  - PLoS
M1  - PreJuSER-22156
SP  - e41457
PY  - 2012
N1  - Record converted from VDB: 12.11.2012
AB  - Alzheimer's disease (AD) is a devastating disease affecting predominantly the aging population. One of the characteristic pathological hallmarks of AD are neuritic plaques, consisting of amyloid-β peptide (Aβ). While there has been some advancement in diagnostic classification of AD patients according to their clinical severity, no fully reliable method for pre-symptomatic diagnosis of AD is available. To enable such early diagnosis, which will allow the initiation of treatments early in the disease progress, neuroimaging tools are under development, making use of Aβ-binding ligands that can visualize amyloid plaques in the living brain. Here we investigate the properties of a newly designed series of D-enantiomeric peptides which are derivatives of ACI-80, formerly called D1, which was developed to specifically bind aggregated Aβ1-42. We describe ACI-80 derivatives with increased stability and Aβ binding properties, which were characterized using surface plasmon resonance and enzyme-linked immunosorbent assays. The specific interactions of the lead compounds with amyloid plaques were validated by ex vivo immunochemistry in transgenic mouse models of AD. The novel compounds showed increased binding affinity and are promising candidates for further development into in vivo imaging compounds.
KW  - J (WoSType)
LB  - PUB:(DE-HGF)16
C6  - pmid:22848501
C2  - pmc:PMC3404088
UR  - <Go to ISI:>//WOS:000306751300042
DO  - DOI:10.1371/journal.pone.0041457
UR  - https://juser.fz-juelich.de/record/22156
ER  -