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Publication : Antidiabetic actions of an estrogen receptor β selective agonist.

First Author  Alonso-Magdalena P Year  2013
Journal  Diabetes Volume  62
Issue  6 Pages  2015-25
PubMed ID  23349481 Mgi Jnum  J:208572
Mgi Id  MGI:5563722 Doi  10.2337/db12-1562
Citation  Alonso-Magdalena P, et al. (2013) Antidiabetic actions of an estrogen receptor beta selective agonist. Diabetes 62(6):2015-25
abstractText  The estrogen receptor beta (ERbeta) is emerging as an important player in the physiology of the endocrine pancreas. We evaluated the role and antidiabetic actions of the ERbeta selective agonist WAY200070 as an insulinotropic molecule. We demonstrate that WAY200070 enhances glucose-stimulated insulin secretion both in mouse and human islets. In vivo experiments showed that a single administration of WAY200070 leads to an increase in plasma insulin levels with a concomitant improved response to a glucose load. Two-week treatment administration increased glucose-induced insulin release and pancreatic beta-cell mass and improved glucose and insulin sensitivity. In addition, streptozotocin-nicotinamide-induced diabetic mice treated with WAY200070 exhibited a significant improvement in plasma insulin levels and glucose tolerance as well as a regeneration of pancreatic beta-cell mass. Studies performed in db/db mice demonstrated that this compound restored first-phase insulin secretion and enhanced pancreatic beta-cell mass. We conclude that ERbeta agonists should be considered as new targets for the treatment of diabetes.
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