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Endocrine/metabolic disease


Glucagon-like peptide-1 receptor (GLP-1R; GLP1R); estrogen receptor

In vitro and mouse studies identified a stable GLP-1-estrogen conjugate that could help treat type 2 diabetes. In mice, the conjugate increased weight loss compared with GLP-1 alone and led to improved insulin sensitivity and glycemic control. In mice, estradiol or an unstable GLP-1-estrogen conjugate induced hypertrophic activity in the uterus and stimulated the growth of tumor xenografts, whereas the stable GLP-1-estrogen conjugate did not. Next steps include additional safety studies to rule out an oncogenic effect on cells that express both GLP-1R and estrogen receptor.
Marcadia Biotech Inc., which was acquired by Roche in 2010, partially funded the study.

SciBX 5(46); doi:10.1038/scibx.2012.1207
Published online Nov. 29, 2012

Patent application filed; exclusively licensed to Roche

Finan, B. et al. Nat. Med.; published online Nov. 11, 2012;
Contact: Matthias H. Tschöp, German Research Center for Environmental Health, Munich, Germany
Contact: Richard D. DiMarchi, Indiana University, Bloomington, Ind.