P1‐307: Inhibition of protein misfolding by optimization of small molecules targeted to both beta‐amyloid and tau peptides | Zendy

Taylor Marcia | Zendy; Banfield Scott | Zendy; Barden Christopher | Zendy; Lu Erhu | Zendy; Reed Mark | Zendy; Sweeting Braden | Zendy; Wang Yanfei | Zendy; Yadav Arun | Zendy; Yang Seung-Pil | Zendy; Weaver Donald F. | Zendy; Wu Fan | Zendy

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P1‐307: Inhibition of protein misfolding by optimization of small molecules targeted to both beta‐amyloid and tau peptides

Author(s) -

Taylor Marcia,

Banfield Scott,

Barden Christopher,

Lu Erhu,

Reed Mark,

Sweeting Braden,

Wang Yanfei,

Yadav Arun,

Yang Seung-Pil,

Weaver Donald F.,

Wu Fan

Publication year - 2015

Publication title -

alzheimer's and dementia

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 6.713

H-Index - 118

eISSN - 1552-5279

pISSN - 1552-5260

DOI - 10.1016/j.jalz.2015.06.522

Subject(s) - chemistry , amyloid (mycology) , amyloid beta , in vitro , small molecule , in silico , surface plasmon resonance , amyloid precursor protein , pharmacology , biochemistry , peptide , biophysics , alzheimer's disease , medicine , biology , disease , pathology , gene , nanotechnology , materials science , inorganic chemistry , nanoparticle

with bromochloropropane to obtain an intermediate which was subsequently treated with various cyclic amines (1a-1f). Docking study of the compounds was performed using vlife 4.3 having crystal structure of TcAChE. Results: Docking study of the analogs revealed that they could bind to both the catalytic and peripheral sites as they interacts with various amino acid residues of the gorge like Trp279, Tyr121, Gly118, Gly119, Glu99 and Trp84. Conclusions:Coumarin analogues may alter the progression of disease as the analogs interact with both the sites of enzyme.

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