| 1 | Picomolar-sensitiveβ-amyloid fibril fluorophores by tailoring the hydrophobicity of biannulatedπ-elongated dioxaborine-dyes显示文摘The pathological origin of Alzheimer’s disease(AD)is still shrouded in mystery,despite intensive worldwide research efforts.The selective visualization ofβ-amyloid(Aβ),the most abundant proteinaceous deposit in AD,is pivotal to reveal AD pathology.To date,several small-molecule fluorophores for Aβspecies have been developed,with increasing binding affinities.In the current work,two organic small-molecule dioxaborine-derived fluorophores were rationally designed through tailoring the hydrophobicity with the aim to enhance the binding affinity for Aβ_(1-42) fibrils-while concurrently preventing poor aqueous solubility-via biannulate donor motifs in D-π-A dyes.An unprecedented sub-nanomolar affinity was found(K_(d)=0.62±0.33 nM)and applied to super-sensitive and red-emissive fluorescent staining of amyloid plaques in cortical brain tissue ex vivo.These fluorophores expand the dioxaborine-curcumin-based family of Aβ-sensitive fluorophores with a promising new imaging agent. | Jusung An Peter Verwilst Hira Aziz Jinwoo Shin Sungsu Lim Ilwha Kim Yun Kyung Kim Jong Seung Kim | 2022 | Bioactive Materials2022，7，7： | 1 |
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