The cannabinoid receptor inverse agonist AM251 regulates the expression of the EGF receptor and its ligands via destabilization of oestrogen-related receptor α protein.

Abstract

AM251 up-regulates EGFR expression and signalling via a novel non-CB(1)R-mediated pathway involving destabilization of ERRα protein in selected cancer cell lines.

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Subjects

• Cell Line, Tumor
• Epidermal Growth Factor
• Genistein
• HCT116 Cells
• Humans
• Intercellular Signaling Peptides and Proteins
• Ligands
• Nitriles
• Orphan Nuclear Receptors
• Piperidines
• Protein Binding
• Pyrazoles
• RNA, Messenger
• Receptor, Cannabinoid, CB1
• Receptor, Epidermal Growth Factor
• Receptors, Estrogen
• Thiazoles
• Up-Regulation

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Authors

• J L Fiori
• M Sanghvi
• M P O'Connell
• S M Krzysik-Walker
• R Moaddel
• M Bernier

Publication date

2011-09-09

Journal

Journal topics

• Drug Therapy
• Pharmacology

Language

Eng.

Copyright

Laboratory of Clinical Investigation, National Institute on Aging, National Institutes of Health, Baltimore, MD, USA.

Release reference

Br J Pharmacol. 2011 Oct;164(3):1026-40

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