Partial agonism improves the anti-hyperglycaemic efficacy of an oxyntomodulin-derived GLP-1R/GCGR co-agonist

Molecular Metabolism(2021)

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摘要
•DPP-4-resistance-conferring amino acid substitutions affect pharmacological efficacy.•GLP-1R/GCGR co-agonists with reduced β-arrestin recruitment are more effective in vivo.•Partial agonism, rather than biased agonism, is sufficient to produce these benefits.
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关键词
GLP-1,Glucagon,Oxyntomodulin,Biased agonism,Partial agonism,β-arrestin
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