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.
Chemoproteomic fishing identifies arzanol as a positive modulator of brain glycogen phosphorylase / Del Gaudio, Federica; Pollastro, Federica; Mozzicafreddo, Matteo; Riccio, Raffaele; Minassi, Alberto; Monti, Maria Chiara. - In: CHEMICAL COMMUNICATIONS. - ISSN 1359-7345. - 54:(2018), pp. 12863-12866-12866. [10.1039/c8cc07692h]
Chemoproteomic fishing identifies arzanol as a positive modulator of brain glycogen phosphorylase
Riccio, Raffaele;Monti, Maria Chiara
2018
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.File | Dimensione | Formato | |
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