Article
K303⁶·⁵⁸ in the μ opioid (MOP) receptor is important in conferring selectivity for covalent binding of β-funaltrexamine (β-FNA).
European journal of pharmacology - 5 Feb 2015
DiMattio Kelly M, Chen Chongguang, Shi Lei, Liu-Chen Lee-Yuan
Abstract excerpt
β-funaltrexamine (β-FNA) is an irreversible μ opioid (MOP) receptor antagonist and a reversible agonist of κ opioid (KOP) receptor. β-FNA binds covalently to the MOP receptor at Lys233(5.39), which is conserved among opioid receptors. Molecular docking of β-FNA showed that K303(6.58) in the MOP receptor and E297(6.58) in the KOP receptor played distinct roles in positioning β-FNA. K303(6.58)E MOP receptor and...
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