Estrogenic activity of E2-conjugated GLP-1 is mediated by intracellular endolysosomal acidification and estrone metabolism

Estrogenic activity of E2-conjugated GLP-1 is mediated by intracellular endolysosomal acidification and estrone metabolism

Objective: Recent modifications to glucagon-like peptide 1 (GLP-1), known for its insulinotropic and satiety-inducing effects, have focused on conjugating small molecules to enable selective delivery into GLP-1R+ tissues to achieve targeted synergy and improved metabolic outcomes. Despite continued...

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Main Authors: Callum Coupland, Na Sun, Ahmed Khalil, Özüm Ezgi Karaoglu, Arkadiusz Liskiewicz, Daniela Liskiewicz, Gerald Grandl, Seun Akindehin, Gandhari Maity, Bin Yang, Brian Finan, Patrick Knerr, Jonathan D. Douros, Axel Walch, Richard DiMarchi, Matthias H. Tschöp, Timo D. Müller, Aaron Novikoff
Format: Article
Language:English
Published: Elsevier 2025-06-01
Series:Molecular Metabolism
Subjects:
Glucagon-like peptide 1
Estradiol
Peptide conjugation
Pharmacology
Metabolomics
Bioluminescence resonance energy transfer (BRET)
Online Access:http://www.sciencedirect.com/science/article/pii/S2212877825000432
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