Journal
PEPTIDES
Volume 100, Issue -, Pages 190-201Publisher
ELSEVIER SCIENCE INC
DOI: 10.1016/j.peptides.2017.12.021
Keywords
GLP-1/Glucagon Co-agonism; Polypharmacology; Type 2 diabetes; Gip
Funding
- Alexander von Humboldt Foundation
- Helmholtz Alliance ICEMED by Helmholtz Association
- Helmholtz cross-program topic Metabolic Dysfunction
- German Research Foundation [DFG-TS226/1-1, DFG-TS226/3-1]
- European Research Council ERC AdG HypoFlam [695054]
- German Center for Diabetes Research
- Helmholtz Initiative on Personalized Medicine iMed by Helmholtz Association
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Chemical derivatives of the gut-derived peptide hormone glucagon-like peptide 1 (GLP-1) are among the best-in-class pharmacotherapies to treat obesity and type 2 diabetes. However, GLP-1 analogs have modest weight lowering capacity, in the range of 5-10%, and the therapeutic window is hampered by dose-dependent side effects. Over the last few years, a new concept has emerged: combining the beneficial effects of several key metabolic hormones into a single molecular entity. Several unimolecular GLP-1-based polyagonists have shown superior metabolic action compared to GLP-1 monotherapies. In this review article, we highlight the history of polyagonists targeting the receptors for GLP-1, GIP and glucagon, and discuss recent progress in expanding of this concept to now allow targeted delivery of nuclear hormones via GLP-1 and other gut hormones, as a novel approach towards more personalized pharmacotherapies.
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