Issue 91, 2018

Chemoproteomic fishing identifies arzanol as a positive modulator of brain glycogen phosphorylase

Abstract

The interactome of arzanol was investigated by MS-based chemical proteomics, a pioneering technology for small molecule target discovery. Brain glycogen phosphorylase (bGP), a key regulator of glucose metabolism so far refractory to small molecule modulation, was identified as the main high-affinity target of arzanol. Competitive affinity-based proteomics, DARTS, molecular docking, surface plasmon resonance and in vitro biological assays provided molecular mechanistic insights into the arzanol–enzyme interaction, qualifying this positive modulator of bGP for further studies in the realm of neurodegeneration and cancer.

Graphical abstract: Chemoproteomic fishing identifies arzanol as a positive modulator of brain glycogen phosphorylase

Supplementary files

Article information

Article type
Communication
Submitted
25 Sep 2018
Accepted
18 Oct 2018
First published
19 Oct 2018

Chem. Commun., 2018,54, 12863-12866

Chemoproteomic fishing identifies arzanol as a positive modulator of brain glycogen phosphorylase

F. del Gaudio, F. Pollastro, M. Mozzicafreddo, R. Riccio, A. Minassi and M. C. Monti, Chem. Commun., 2018, 54, 12863 DOI: 10.1039/C8CC07692H

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