胆固醇对 G 蛋白偶联受体功能的影响：计算与实验研究的新视角。
Effects of Cholesterol on GPCR Function: Insights from Computational and Experimental Studies.
机构信息
Laboratory of Organic Chemistry, Department of Chemistry, National and Kapodistrian University of Athens, Athens, Greece.
Section of Pharmaceutical Chemistry, Department of Pharmacy, School of Health Sciences, National and Kapodistrian University of Athens, Athens, Greece.
出版信息
Adv Exp Med Biol. 2019;1135:89-103. doi: 10.1007/978-3-030-14265-0_5.
The extensive experimental and computational evidences revealed that cholesterol is involved in the drug binding to G protein-coupled receptor (GPCR) targets that is influenced by the membrane environment and external functions. These multifunctional factors make the understanding of the molecular mechanism of action in greater detail an entirely difficult task. Significant efforts have been made for better understanding the role of multi-directional specific, receptor-dependent interactions of cholesterol, and its effects on drug design and development. Additional efforts must be made in this complex system in order to shed more light on cholesterol molecular basis of action. The results of molecular simulations that complemented experimental data may reveal new aspects of GPCR-cholesterol interactions and may provide a comprehensive understanding of receptor function.
大量的实验和计算证据表明，胆固醇参与了药物与 G 蛋白偶联受体（GPCR）靶标的结合，这种结合受到膜环境和外部功能的影响。这些多功能因素使得更详细地了解作用的分子机制成为一项完全艰巨的任务。为了更好地理解胆固醇的多向特异性、受体依赖性相互作用及其对药物设计和开发的影响，人们做出了巨大的努力。在这个复杂的系统中，必须做出更多的努力，以便进一步阐明胆固醇作用的分子基础。补充实验数据的分子模拟结果可能揭示 GPCR-胆固醇相互作用的新方面，并可能提供对受体功能的全面理解。
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