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首页> 美国卫生研究院文献>other >Aromatic interactions impact ligand binding and function at serotonin 5-HT2C G protein-coupled receptors: Receptor homology modeling ligand docking and molecular dynamics results validated by experimental studies
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Aromatic interactions impact ligand binding and function at serotonin 5-HT2C G protein-coupled receptors: Receptor homology modeling ligand docking and molecular dynamics results validated by experimental studies

机译：芳香族相互作用影响5-羟色胺5-HT2C G蛋白偶联受体上的配体结合和功能：受体同源性建模配体对接和分子动力学结果通过实验研究得到验证

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摘要

The serotonin (5-hydroxytryptamine, 5-HT) 5-HT2 G protein-coupled receptor (GPCR) family consists of types 2A, 2B, and 2C that share ~75% transmembrane (TM) sequence identity. Agonists for 5-HT2C receptors are under development for psychoses, whereas, at 5-HT2A receptors, antipsychotic effects are associated with antagonists—in fact, 5-HT2A agonists can cause hallucinations and 5-HT2B agonists cause cardiotoxicity. It is known that 5-HT2A TM6 residues W6.48, F6.51, and F6.52 impact ligand binding and function, however, ligand interactions with these residues at the 5-HT2C receptor has not been reported. To predict and validate molecular determinants for 5-HT2C-specific activation, results from receptor homology modeling, ligand docking, and molecular dynamics (MD) simulation studies were compared with experimental results for ligand binding and function at wild type and W6.48A, F6.51A, and F6.52A point-mutated 5-HT2C receptors.
机译：血清素（5-羟色胺，5-HT）5-HT2 G蛋白偶联受体（GPCR）家族由2A，2B和2C类型组成，它们具有〜75％的跨膜（TM）序列同一性。 5-HT2C受体激动剂正在开发中，用于精神病，而在5-HT2A受体中，抗精神病作用与拮抗剂有关—实际上，5-HT2A激动剂可引起幻觉，而5-HT2B激动剂可引起心脏毒性。已知5-HT2A TM6残基W6.48，F6.51和F6.52影响配体的结合和功能，但是，尚未报道在5-HT2C受体上与这些残基的配体相互作用。为了预测和验证5-HT2C特异性激活的分子决定因素，将受体同源性建模，配体对接和分子动力学（MD）模拟研究的结果与野生型和W6.48A，F6上配体结合和功能的实验结果进行了比较.51A和F6.52A点突变的5-HT2C受体。

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