Peptide ligand discovery of G protein-coupled receptors

J. Hermes Marin Matic H. Yeung Qianru Jiang Lauri Urvas Elizaveta Korchevaya Tomek Stepniewski A. Murza J. Selent Michael Freissmuth C. Heinis Pierre-Luc Boudreault Jens Carlsson Tao Che Helena Safavi-Hemami A. S. Hauser Christian W. Gruber

Jul 2026 · Nature Reviews Methods Primers · Vol 6 · 0 citations · 251 references

TL;DR

This Primer outlines experimental and computational workflows tailored to peptide–GPCR interactions, including in silico peptide mining, deorphanization strategies, library-based screening platforms, modern pathway-resolved biosensor assays, and approaches for peptide stabilization and optimization strategies to address their pharmacokinetic limitations.

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