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Capturing Peptide–GPCR Interactions and Their Dynamics

Faculty of Life Sciences, Institute of Biochemistry, Leipzig University, Brüderstr. 34, D-04103 Leipzig, Germany
Author to whom correspondence should be addressed.
Academic Editor: Paolo Ruzza
Molecules 2020, 25(20), 4724;
Received: 31 August 2020 / Revised: 8 October 2020 / Accepted: 9 October 2020 / Published: 15 October 2020
(This article belongs to the Special Issue Protein-Peptide and Protein-Small Molecule Interactions)
Many biological functions of peptides are mediated through G protein-coupled receptors (GPCRs). Upon ligand binding, GPCRs undergo conformational changes that facilitate the binding and activation of multiple effectors. GPCRs regulate nearly all physiological processes and are a favorite pharmacological target. In particular, drugs are sought after that elicit the recruitment of selected effectors only (biased ligands). Understanding how ligands bind to GPCRs and which conformational changes they induce is a fundamental step toward the development of more efficient and specific drugs. Moreover, it is emerging that the dynamic of the ligand–receptor interaction contributes to the specificity of both ligand recognition and effector recruitment, an aspect that is missing in structural snapshots from crystallography. We describe here biochemical and biophysical techniques to address ligand–receptor interactions in their structural and dynamic aspects, which include mutagenesis, crosslinking, spectroscopic techniques, and mass-spectrometry profiling. With a main focus on peptide receptors, we present methods to unveil the ligand–receptor contact interface and methods that address conformational changes both in the ligand and the GPCR. The presented studies highlight a wide structural heterogeneity among peptide receptors, reveal distinct structural changes occurring during ligand binding and a surprisingly high dynamics of the ligand–GPCR complexes. View Full-Text
Keywords: GPCR activation; peptide–GPCR interactions; structural dynamics of GPCRs; peptide ligands; crosslinking; NMR; EPR GPCR activation; peptide–GPCR interactions; structural dynamics of GPCRs; peptide ligands; crosslinking; NMR; EPR
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MDPI and ACS Style

Kaiser, A.; Coin, I. Capturing Peptide–GPCR Interactions and Their Dynamics. Molecules 2020, 25, 4724.

AMA Style

Kaiser A, Coin I. Capturing Peptide–GPCR Interactions and Their Dynamics. Molecules. 2020; 25(20):4724.

Chicago/Turabian Style

Kaiser, Anette, and Irene Coin. 2020. "Capturing Peptide–GPCR Interactions and Their Dynamics" Molecules 25, no. 20: 4724.

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