OP449 inhibits breast cancer growth without adverse metabolic effects

OP449 inhibits breast cancer growth without adverse metabolic effects

Hyperinsulinemia is associated with a decrease in breast cancer recurrence-free survival and overall survival. Inhibition of insulin receptor signaling is associated with glycemic dysregulation. SET is a direct modulator of PP2A, which negatively regulates the PI3K/AKT/mTOR pathway. OP449, a SET inh...

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Veröffentlicht in:Endocrine-related cancer 2017-10, Vol.24 (10), p.519-529
Hauptverfasser: Shlomai, Gadi, Zelenko, Zara, Antoniou, Irini Markella, Stasinopoulos, Marilyn, Tobin-Hess, Aviva, Vitek, Michael P, LeRoith, Derek, Gallagher, Emily Jane
Format: Artikel
Sprache:eng
Schlagworte:
Animals
Breast Neoplasms - etiology
Breast Neoplasms - metabolism
Breast Neoplasms - mortality
Diabetes Complications
Disease Models, Animal
Female
Humans
Hyperinsulinism - complications
Mice
Obesity - complications
Peptides - metabolism
Survival Analysis
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Zusammenfassung:Hyperinsulinemia is associated with a decrease in breast cancer recurrence-free survival and overall survival. Inhibition of insulin receptor signaling is associated with glycemic dysregulation. SET is a direct modulator of PP2A, which negatively regulates the PI3K/AKT/mTOR pathway. OP449, a SET inhibitor, decreases AKT/mTOR activation. The effects of OP449 treatment on breast cancer growth in the setting of pre-diabetes, and its metabolic implications are currently unknown. We found that the volumes and weights of human MDA-MB-231 breast cancer xenografts were greater in hyperinsulinemic mice compared with controls (P 
ISSN:1351-0088
1479-6821
DOI:10.1530/ERC-17-0077