Discovery of NIRF theranostic probes targeting amyloid-β and cholinesterases in Alzheimer's disease models.

ABSTRACT: Alzheimer's disease (AD) remains a major unmet medical challenge, with limited tools that integrate early diagnosis and therapeutic intervention. Considering the pivotal roles of amyloid-β (Aβ) and cholinesterases (ChEs) in AD etiology, we report dual-functional theranostic NIR-I probes. The lead candidate, I-43, exhibits favorable NIR optical properties (Stokes shift ≥ 220 nm) and binds strongly to Aβ fibrils, with K_d values of 58.2 ± 9.7 nM for Aβ_1-40 and 104 ± 25 nM for Aβ_1-42. Histological staining of brain tissues from transgenic APP-PS1 mice and human autopsy samples confirms selective detection of Aβ plaques with a high signal-to-noise ratio and minimal cross-reactivity toward pathogenic tau tangles and α-synuclein. In addition, I-43 exhibits fluores

SUBMITTER: Rai H 

PROVIDER: S-EPMC12915651 | biostudies-literature | 2026 Jan

REPOSITORIES: biostudies-literature