Back to Search Start Over

Discovery of a fluorescigenic pyrazoline derivative targeting ubiquitin.

Authors :
Chen X
Lin Z
Su L
Cui X
Zhao B
Miao J
Source :
Biochemical and biophysical research communications [Biochem Biophys Res Commun] 2020 Jul 23; Vol. 528 (2), pp. 256-260. Date of Electronic Publication: 2020 May 27.
Publication Year :
2020

Abstract

Despite significant process in ubiquitin modification by using traditional genetic methods, chemical small molecules that directly target and modify ubiquitin are little reported. Here, we find that a fluorescigenic pyrazoline derivative (FPD5) could do so effectively. Molecule docking revealed that lysine 11 of ubiquitin was the key contact residue. FPD5, with stronger fluorescence, elevated the ubiquitination of beclin 1 (BECN1) and promoted autophagy. This study highlights that targeting ubiquitin by chemical small molecules enables us to modulate ubiquitination and the downstream signaling in the ubiquitin system.<br />Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper. The authors declare the following financial interests/personal relationships which may be considered as potential competing interests:<br /> (Copyright © 2020 Elsevier Inc. All rights reserved.)

Details

Language :
English
ISSN :
1090-2104
Volume :
528
Issue :
2
Database :
MEDLINE
Journal :
Biochemical and biophysical research communications
Publication Type :
Academic Journal
Accession number :
32473753
Full Text :
https://doi.org/10.1016/j.bbrc.2020.05.142