Neher's Biophysics Laboratory for Innovative Drug Discovery, State Key Laboratory of Quality Research in Chinese Medicine, Macau University of Science and Technology, Macao SAR China; Department of Neurology, The Affiliated Hospital of Southwest Medical University, Luzhou, Sichuan, China.
Neher's Biophysics Laboratory for Innovative Drug Discovery, State Key Laboratory of Quality Research in Chinese Medicine, Macau University of Science and Technology, Macao SAR China.
Pharmacol Res. 2024 Oct;208:107395. doi: 10.1016/j.phrs.2024.107395. Epub 2024 Sep 4.
G protein-coupled receptors (GPCRs), widely expressed in the human central nervous system (CNS), perform numerous physiological functions and play a significant role in the pathogenesis of diseases. Consequently, identifying key therapeutic GPCRs targets for CNS-related diseases is garnering immense interest in research labs and pharmaceutical companies. However, using GPCRs drugs for treating neurodegenerative diseases has limitations, including side effects and uncertain effective time frame. Recognizing the rich history of herbal treatments for neurological disorders like stroke, Alzheimer's disease (AD), and Parkinson's disease (PD), modern pharmacological research is now focusing on the understanding of the efficacy of traditional Chinese medicinal herbs and compounds in modulating GPCRs and treatment of neurodegenerative conditions. This paper will offer a comprehensive, critical review of how certain natural products and compounds target GPCRs to treat neurological diseases. Conducting an in-depth study of herbal remedies and their efficacies against CNS-related disorders through GPCRs targeting will augment our strategies for treating neurological disorders. This will not only broaden our understanding of effective therapeutic methodologies but also identify the root causes of altered GPCRs signaling in the context of pathophysiological mechanisms in neurological diseases. Moreover, it would be informative for the creation of safer and more effective GPCR-mediated drugs, thereby establishing a foundation for future treatment of various neurological diseases.
G 蛋白偶联受体（GPCRs）广泛表达于人类中枢神经系统（CNS），执行多种生理功能，并在疾病发病机制中发挥重要作用。因此，鉴定与 CNS 相关疾病相关的关键治疗性 GPCR 靶点，在研究实验室和制药公司中引起了极大的兴趣。然而，使用 GPCRs 药物治疗神经退行性疾病存在局限性，包括副作用和不确定的有效时间框架。鉴于草药治疗中风、阿尔茨海默病（AD）和帕金森病（PD）等神经紊乱的悠久历史，现代药理学研究现在专注于理解传统中药和化合物调节 GPCRs 的功效，以及治疗神经退行性疾病。本文将全面、批判性地综述某些天然产物和化合物如何通过靶向 GPCR 来治疗神经疾病。通过靶向 GPCR 深入研究草药疗法及其对 CNS 相关疾病的疗效，将增强我们治疗神经疾病的策略。这不仅可以加深我们对有效治疗方法的理解，还可以确定神经疾病病理生理机制中 GPCR 信号改变的根本原因。此外，这对于开发更安全、更有效的 GPCR 介导药物也具有启示意义，从而为各种神经疾病的未来治疗奠定基础。
