295358-45-1Relevant academic research and scientific papers
Modulation of the Interaction between a Peptide Ligand and a G Protein-Coupled Receptor by Halogen Atoms
Rosa, Mònica,Caltabiano, Gianluigi,Barreto-Valer, Katy,Gonzalez-Nunez, Verónica,Gómez-Tamayo, José C.,Ardá, Ana,Jiménez-Barbero, Jesús,Pardo, Leonardo,Rodríguez, Raquel E.,Arsequell, Gemma,Valencia, Gregorio
, p. 872 - 876 (2015)
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.
