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Exploring Pairwise Chemical Crosslinking To Study Peptide-Receptor Interactions.

Lisa Seidel1, Barbara Zarzycka2, Vsevolod Katritch2,3

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|December 20, 2018
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Summary

Thiol trapping is a new method for studying G protein-coupled receptor interactions. This technique offers a reliable alternative to disulfide trapping, providing valuable spatial data for molecular modeling.

Keywords:
crosslinkingmolecular modelingpeptide-protein interactionspeptidessulfur

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Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • G protein-coupled receptors (GPCRs) are crucial drug targets.
  • Characterizing GPCR-ligand interactions in live cells is essential.
  • Existing crosslinking methods have limitations.

Purpose of the Study:

  • To evaluate the
  • thiol trapping
  • method for pairwise crosslinking of GPCRs and ligands.
  • To compare thiol trapping with traditional disulfide trapping.
  • To assess the utility of thiol trapping for molecular modeling.

Main Methods:

  • Incorporation of cysteine into the corticotropin-releasing factor receptor.
  • Attachment of haloacetamide groups (α-chloro- or α-bromoacetamide) to ligands.
  • Proximity-enhanced reaction between cysteine and haloacetamides.
  • Modulation of Gs protein coupling using recombinant mini-Gs, GTPγS, and Gαs-depleted HEK293 cells.

Main Results:

  • Thiol trapping demonstrated highly reproducible signals and low background.
  • The method proved to be a valid alternative to disulfide trapping.
  • Thiol trapping offers advantages when reducing agents are needed.
  • Distinct spatial constraints were obtained, enhancing molecular modeling datasets.
  • Crosslinking yields increased with elevated Gs protein levels.

Conclusions:

  • Thiol trapping is a robust and effective method for studying GPCR-ligand interactions in live cells.
  • It provides complementary spatial information to existing techniques.
  • The method's efficiency is influenced by Gs protein coupling levels.