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

Federica Del Gaudio; Federica Pollastro; Matteo Mozzicafreddo; Raffaele Riccio; Alberto Minassi; Maria Chiara Monti

doi:10.1039/c8cc07692h

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

Federica Del Gaudio
, Federica Pollastro
, Matteo Mozzicafreddo
, Raffaele Riccio
, Alberto Minassi
, Maria Chiara Monti

Department of Pharmaceutical Sciences

Research output: Contribution to journal › Article › peer-review

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.

Original language	English
Pages (from-to)	12863-12866
Number of pages	4
Journal	Chemical Communications
Volume	54
Issue number	91
DOIs	https://doi.org/10.1039/c8cc07692h
Publication status	Published - 2018

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10.1039/c8cc07692h

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title = "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.",

author = "\{Del Gaudio\}, Federica and Federica Pollastro and Matteo Mozzicafreddo and Raffaele Riccio and Alberto Minassi and Monti, \{Maria Chiara\}",

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year = "2018",

doi = "10.1039/c8cc07692h",

language = "English",

volume = "54",

pages = "12863--12866",

journal = "Chemical Communications",

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publisher = "Royal Society of Chemistry",

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T1 - Chemoproteomic fishing identifies arzanol as a positive modulator of brain glycogen phosphorylase

AU - Del Gaudio, Federica

AU - Pollastro, Federica

AU - Mozzicafreddo, Matteo

AU - Riccio, Raffaele

AU - Minassi, Alberto

AU - Monti, Maria Chiara

PY - 2018

Y1 - 2018

N2 - 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.

AB - 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.

UR - https://www.scopus.com/pages/publications/85056320511

U2 - 10.1039/c8cc07692h

DO - 10.1039/c8cc07692h

M3 - Article

SN - 1359-7345

VL - 54

SP - 12863

EP - 12866

JO - Chemical Communications

JF - Chemical Communications

IS - 91

ER -

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

Abstract

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