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Orexin Antagonists: A Wake-Up Call for Medicinal Chemists?
Journal of Medicinal Chemistry ( IF 7.3 ) Pub Date : 2020-02-19 , DOI: 10.1021/acs.jmedchem.0c00190
D Eric Walters 1
Affiliation  

Orexin receptors are G protein coupled receptors that may be useful targets for sleep disorders, eating disorders, or addictive behavior. Recent work shows that binding of antagonists to these receptors is complex, with strong dependence on hydrophobic hot spots and networks of water-mediated hydrogen bonds. Despite the minimal structural differences between receptor types, selectivity can be achieved in a number of different ways.

中文翻译:

Orexin拮抗剂:药物化学家的警钟?

食欲素受体是G蛋白偶联受体,可能是睡眠障碍,进食障碍或成瘾行为的有用靶标。最近的工作表明,拮抗剂与这些受体的结合是复杂的,强烈依赖于疏水性热点和水介导的氢键网络。尽管受体类型之间的结构差异最小,但是可以通过许多不同方式实现选择性。
更新日期:2020-02-19
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