Modulation of the Interaction between a Peptide Ligand
and a G Protein-Coupled Receptor by Halogen Atoms
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Abstract
Systematic halogenation of two native
opioid peptides has shown
that halogen atoms can modulate peptide–receptor interactions
in different manners. First, halogens may produce a steric hindrance
that reduces the binding of the peptide to the receptor. Second, chlorine,
bromine, or iodine may improve peptide binding if their positive σ-hole
forms a halogen bond interaction with negatively charged atoms of
the protein. Lastly, the negative electrostatic potential of fluorine
can interact with positively charged atoms of the protein to improve
peptide binding