Potent mu-Opioid Receptor Agonists from Cyclic Peptides Tyr-c[D-Lys-Xxx-Tyr-Gly]: Synthesis, Biological, and Structural Evaluation

Li Yangmei; Cazares Margret; Wu Jinhua; Houghten Richard A.; Toll Laurence; Dooley Colette

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Potent mu-Opioid Receptor Agonists from Cyclic Peptides Tyr-c[D-Lys-Xxx-Tyr-Gly]: Synthesis, Biological, and Structural Evaluation

机译：环状肽Tyr-c [D-Lys-Xxx-Tyr-Gly]的强μ阿片受体激动剂：合成，生物学和结构评价。

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To optimize the structure of a mu-opioid receptor ligand, analogs H-Tyr-c[D-Lys-Xxx-Tyr-Gly] were synthesized and their biological activity was tested. The analog containing a Phe(3) was identified as not only exhibiting binding affinity 14-fold higher than the original hit but also producing agonist activity 3-fold more potent than morphine. NMR study suggested that a trans conformation at D-Lys(2)-Xxx(3) is crucial for these cyclic peptides to maintain high affinity, selectivity, and functional activity toward the mu-opioid receptor.

机译：为了优化μ阿片受体配体的结构，合成了类似物H-Tyr-c [D-Lys-Xxx-Tyr-Gly]，并测试了它们的生物学活性。含有Phe（3）的类似物不仅具有比原始命中高14倍的结合亲和力，而且还比吗啡产生3倍的激动剂活性。 NMR研究表明，D-Lys（2）-Xxx（3）处的反式构象对于这些环状肽维持对mu阿片受体的高亲和力，选择性和功能活性至关重要。

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《Journal of Medicinal Chemistry》 |2016年第3期|共7页
作者
Li Yangmei; Cazares Margret; Wu Jinhua; Houghten Richard A.; Toll Laurence; Dooley Colette;
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1. Potent mu-Opioid Receptor Agonists from Cyclic Peptides Tyr-c[D-Lys-Xxx-Tyr-Gly]: Synthesis, Biological, and Structural Evaluation [J] . Li Yangmei, Cazares Margret, Wu Jinhua, Journal of Medicinal Chemistry . 2016,第3期

机译：环状肽Tyr-c [D-Lys-Xxx-Tyr-Gly]的强μ阿片受体激动剂：合成，生物学和结构评价。
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Potent mu-Opioid Receptor Agonists from Cyclic Peptides Tyr-c[D-Lys-Xxx-Tyr-Gly]: Synthesis, Biological, and Structural Evaluation

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