TY - JOUR
T1 - Shedding light on tau protein aggregation
T2 - The progress in developing highly selective fluorophores
AU - Verwilst, Peter
AU - Kim, Hyeong Seok
AU - Kim, Soobin
AU - Kang, Chulhun
AU - Kim, Jong Seung
N1 - Funding Information:
This work was supported by the National Research Foundation of Korea (NRF) (2017R1A2A2A05069805, CK), funded by the Ministry of Science and ICT (CRI project no. 2009-0081566, JSK), and the Basic Science Research Program (NRF-2017R1D1A1B03032561, PV) funded by the Ministry of Education, as well as the Korea Research Fellowship Program funded by the Ministry of Science and ICT through the National Research Foundation of Korea (2016H1D3A1938052, PV).
Publisher Copyright:
© 2018 The Royal Society of Chemistry.
PY - 2018/4/7
Y1 - 2018/4/7
N2 - Historically, in Alzheimer's disease research, a lot of attention has been paid to the development of highly selective fluorophores for beta amyloid plaques. With a shift in the understanding of the disease and the importance of a network of cross-talk interactions, the development of small-molecule fluorescent dyes with high selectivity for (hyperphosphorylated) tau protein aggregates in neurofibrillary tangles has been gaining increasing attention. Fluorescent dyes for the selective labelling of tau aggregates in histological AD brain sections have been described, spanning the entire visible range of the electromagnetic spectrum. Despite the relatively early stages of the development of the field, a large diversity in probe architectures has been reported. Importantly, a handful of near-infrared-emissive dyes have been described as well, and some of these have exhibited good pharmacological profiles, with a significant blood-brain-barrier permeability, and a demonstrated ability to label tau tangles in vivo in small-animal models of Alzheimer's disease and other tauopathies. The developments summarized in the current work are expected to aid the unravelling of the diverse set of players in the etiology of Alzheimer's disease. In this tutorial review, we seek to provide the reader with an overview of the most important recent developments and hope to provide some guidelines for the design of future probes.
AB - Historically, in Alzheimer's disease research, a lot of attention has been paid to the development of highly selective fluorophores for beta amyloid plaques. With a shift in the understanding of the disease and the importance of a network of cross-talk interactions, the development of small-molecule fluorescent dyes with high selectivity for (hyperphosphorylated) tau protein aggregates in neurofibrillary tangles has been gaining increasing attention. Fluorescent dyes for the selective labelling of tau aggregates in histological AD brain sections have been described, spanning the entire visible range of the electromagnetic spectrum. Despite the relatively early stages of the development of the field, a large diversity in probe architectures has been reported. Importantly, a handful of near-infrared-emissive dyes have been described as well, and some of these have exhibited good pharmacological profiles, with a significant blood-brain-barrier permeability, and a demonstrated ability to label tau tangles in vivo in small-animal models of Alzheimer's disease and other tauopathies. The developments summarized in the current work are expected to aid the unravelling of the diverse set of players in the etiology of Alzheimer's disease. In this tutorial review, we seek to provide the reader with an overview of the most important recent developments and hope to provide some guidelines for the design of future probes.
UR - http://www.scopus.com/inward/record.url?scp=85044942997&partnerID=8YFLogxK
U2 - 10.1039/c7cs00706j
DO - 10.1039/c7cs00706j
M3 - Review article
C2 - 29484335
AN - SCOPUS:85044942997
VL - 47
SP - 2249
EP - 2265
JO - Chemical Society Reviews
JF - Chemical Society Reviews
SN - 0306-0012
IS - 7
ER -