Hormonal
Unimolecular tetra-receptor agonists (TC4) simultaneously activate GLP-1R, GIPR, GcgR, and Y2R, resulting in superior metabolic efficacy (weight loss and glycemic control) compared to mono- or dual-agonists by leveraging synergistic receptor engagement.
This research describes a new class of peptide drugs that target four metabolic receptors (GLP-1, GIP, Glucagon, and PYY) simultaneously. In preclinical studies, this approach showed strong potential for treating obesity and type 2 diabetes with fewer side effects like nausea than older drugs. It is not yet available for human use.
These TC constructs were rationally designed toward retaining high potency and efficacy across all four target receptors... The ability to achieve broad-spectrum receptor activation within a single peptide framework represents a promising advancement in the field of metabolic therapeutics, with implications for the treatment of obesity, T2D, and associated comorbidities.
Why this rating
Preclinical in vitro and in vivo data; no human clinical trial results are presented in this manuscript.
Source
Molecular Design of Unimolecular Tetra-Receptor Agonists
Tristan C. Dinsmore et al. · Journal of the American Chemical Society · 2025
DOI 10.1021/jacs.5c04095
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