Back to search

Article

Binding Kinetics, Bias, Receptor Internalization and Effects on Insulin Secretion <i>in vitro</i> and <i>in vivo</i> of a Novel GLP-1R/GIPR Dual Agonist, HISHS-2001

2025-01-17

Abstract excerpt

The use of incretin analogues has emerged in recent years as an effective approach to achieve both enhanced insulin secretion and weight loss in type 2 diabetes (T2D) patients. Agonists which bind and stimulate multiple receptors have shown particular promise. However, off target effects, including nausea and diarrhoea, remain a complication of using these agents, and modified versions with optimized pharmacologic...

Topics

Open a Topic to create a Post that cites this publication.

Identifiers and source

Literature Corpus work
80f44adb-4612-59ab-a9a0-7972f4f46e0a
DOI
10.1101/2025.01.13.632834
Open publication

Related research

Semantic proximity does not establish scientific evidence.

Click a neighbor to travelStep 1 · 12 closest
Interactive article relationship graphSelect a related publication card to move it into the centre and load its closest explainable connections. Solid lines are source-backed structured connections. Dashed lines are semantic discovery signals and are not scientific evidence.
Binding Kinetics, Bias, Receptor Internalization and Effects on Insulin Secretion <i>in vitro</i> and <i>in vivo</i> of a Novel GLP-1R/GIPR Dual Agonist, HISHS-2001DOI 10.1101/2025.01.13.632834
The GLP-1R as a model for understanding and exploiting biased agonism in next-generation medicinesSemantic proximity
Altered desensitization and internalization patterns of rodent versus human GIP receptors -- a major drug discovery challengeSemantic proximity
Insights into agonist-elicited activation of the human glucose-dependent insulinotropic polypeptide receptor.Semantic proximity
Modelling G protein-biased agonism using GLP-1 receptor C-terminal mutations.Semantic proximity
Biased agonism and polymorphic variation at the GLP-1 receptor: Implications for the development of personalised therapeuticsSemantic proximity
Tuning Insulin Receptor Signaling Using <i>De Novo</i> Designed AgonistsSemantic proximity
Molecular mechanisms underlying physiological and receptor pleiotropic effects mediated by GLP ‐ 1R activationSemantic proximity
Generation and use of new tools for the characterisation of gut hormone receptorsSemantic proximity
Ligand-independent modulation of GIPR signaling by splice variantsSemantic proximity
Molecular dynamics-guided optimization of BGM0504 enhances dual-target agonism for combating diabetes and obesitySemantic proximity
Glucagon-like peptide-1 receptor C-terminal tail phosphorylation determines signalling responses from pancreatic β-cellsSemantic proximity
GLP-1-mediated delivery of the PPAR𝛼/𝛾 dual-agonist Tesaglitazar improves obesity and glucose metabolism in miceSemantic proximity
Select a neighboring publication to make it the new centre.