Abstract
A number of fluorinated γ-carboline derivatives were studied as potential agents that block the development of FUS protein aggregation, which underlies proteinopathy in amyotrophic lateral sclerosis. Compounds exhibiting high anti-aggregation potential against the FUS protein were identified by fluorescence microscopy. Lead compounds that reduce aggregation by a factor of two or more and have relatively low cytotoxicity were identified among the most active structures.
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Dedicated to Academician of the Russian Academy of Sciences V. N. Charushin on the occasion of his 70th birthday.
Published in Russian in Izvestiya Akademii Nauk. Seriya Khimicheskaya, No. 5, pp. 982–986, May, 2021.
This study was financially supported by the Russian Science Foundation (Project No. 19-13-00378; synthesis of compounds) and by the Ministry of Science and Higher Education of the Russian Federation (agreement No. 075-15-2020-795, internal number 13.1902.21.0027). The cell culture visualization was carried out using the equipment of the Center for Collective Use of the Institute of Physiologically Active Compounds, Russian Academy of Sciences, within the framework of the state assignment for the Institute of Physiologically Active Compounds, Russian Academy of Sciences (No. 0090-2019-0005).
This paper does not contain descriptions of studies on animals or humans.
The authors declare no conflict of interest in financial or any other sphere.
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Ustyugov, A.A., Aksinenko, A.Y., Steinberg, D.A. et al. Fluorinated γ-carbolines as a promising class of neuroprotective drugs. Russ Chem Bull 70, 982–986 (2021). https://doi.org/10.1007/s11172-021-3176-5
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DOI: https://doi.org/10.1007/s11172-021-3176-5