GLP-1-estradiol conjugate

The GLP-1-estradiol conjugate, often identified as GE2 in preclinical research, is an experimental peptide-drug conjugate (PDC) developed by Novo Nordisk researchers. It consists of a glucagon-like peptide-1 (GLP-1) peptide covalently linked to 17β-estradiol (E2) via a specialized amide-ether linker at the C-terminal. This dual-action agent functions as a dual agonist for the Glucagon-like peptide 1 receptor (GLP-1R) and the Estrogen receptor (ER). The therapeutic strategy behind this molecule is to leverage GLP-1R-mediated delivery to transport estradiol specifically to tissues expressing GLP-1 receptors, such as the hypothalamus, hindbrain, and hippocampus. This targeted approach is intended to harness the synergistic metabolic and neuroprotective benefits of both hormones while minimizing the systemic estrogenic side effects typically associated with estrogen therapy, such as uterine stimulation. Preclinical studies in animal models have demonstrated its potential in promoting weight loss, improving glucose regulation, enhancing neurogenesis in the dentate gyrus, and reversing cognitive decline associated with Alzheimer's disease and aging.

Other names

Glucagon-like peptide-1-estradiol conjugateGLP-1-E2 conjugateGLP1-E2 conjugateGLP 1-E2 conjugateGLP-1-estradiolGLP1-estradiolGLP 1-estradiol