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, F.; Pollastro, F.; Mozzicafreddo, M.; Riccio, R.; Minassi, A.; Monti, M. C.. - In: CHEMICAL COMMUNICATIONS. - ISSN 1359-7345. - 54:91(2018), pp. 12863-12866. [10.1039/c8cc07692h]
Chemoproteomic fishing identifies arzanol as a positive modulator of brain glycogen phosphorylase
Mozzicafreddo M.;
2018-01-01
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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
