Modulation of the Interaction between a Peptide Ligand and a G Protein-Coupled Receptor by Halogen Atoms

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• 作者：M貌nica Rosa ; Gianluigi Caltabiano ; Katy Barreto-Valer ; Ver贸nica Gonzalez-Nunez ; Jos茅 C. G贸mez-Tamayo ; Ana Ard谩 ; Jes煤s Jim茅nez-Barbero ; Leonardo Pardo ; Raquel E. Rodr铆guez ; Gemma Arsequell ; Gregorio Valencia
• 刊名：ACS Medicinal Chemistry Letters
• 出版年：2015
• 出版时间：August 13, 2015
• 年：2015
• 卷：6
• 期：8
• 页码：872-876
• 全文大小：351K
• ISSN：1948-5875

文摘

Systematic halogenation of two native opioid peptides has shown that halogen atoms can modulate peptide鈥搑eceptor 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 蟽-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.