An, Jusung Verwilst, Peter Hira Aziz Shin, Jinwoo Lim, Sung su Kim, Ilwha Kim, Yun Kyung Kim, Jong Seung 2024-01-19T12:00:07Z 2024-01-19T12:00:07Z 2022-01-10 2022-07 2452-199X https://pubs.kist.re.kr/handle/201004/115090 The pathological origin of Alzheimer's disease (AD) is still shrouded in mystery, despite intensive worldwide research efforts. The selective visualization of β-amyloid (Aβ), the most abundant proteinaceous deposit in AD, is pivotal to reveal AD pathology. To date, several small-molecule fluorophores for Aβ species 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 Aβ1-42 fibrils —while concurrently preventing poor aqueous solubility—via biannulate donor motifs in D-π-A dyes. An unprecedented sub-nanomolar affinity was found (Kd = 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. English Elsevier Picomolar-sensitive β-amyloid fibril fluorophores by tailoring the hydrophobicity of biannulated π-elongated dioxaborine-dyes Article 10.1016/j.bioactmat.2021.10.047 1 Bioactive Materials, v.13, pp.239 - 248 Bioactive Materials 13 239 248 Y scie scopus 000766627300002 2-s2.0-85118746971 Engineering, Biomedical Materials Science, Biomaterials Engineering Materials Science Article TAU AGGREGATION IN-VIVO DETECTION NEAR-INFRARED FLUOROPHORES ALZHEIMERS-DISEASE FLUORESCENT-PROBE RATIONAL DESIGN PROGRESS PLAQUES Alzheimer&apos s disease Dioxaborine-dye Hydrophobicity tailoring Small-molecular fluorescent probe β-Amyloid