Gu Yuanyuan, Zhu Dongya
Department of Pharmacology, School of Pharmacy, Nanjing Medical University, Nanjing, Jiangsu 211166, China.
Institution of Stem Cell and Neuroregeneration, School of Pharmacy, Nanjing Medical University, Nanjing, Jiangsu 211166, China.
J Biomed Res. 2020 Dec 10;35(1):1-10. doi: 10.7555/JBR.34.20200108.
Neurological and neuropsychiatric disorders are one of the leading causes of disability worldwide and affect the health of billions of people. Nitric oxide (NO), a free gas with multitudinous bioactivities, is mainly produced from the oxidation of L-arginine by neuronal nitric oxide synthase (nNOS) in the brain. Inhibiting nNOS benefits a variety of neurological and neuropsychiatric disorders, including stroke, depression and anxiety disorders, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, chronic pain, and drug addiction. Due to critical roles of nNOS in learning and memory and synaptic plasticity, direct inhibition of nNOS may cause severe side effects. Importantly, interactions of several proteins, including post-synaptic density 95 (PSD-95), carboxy-terminal PDZ ligand of nNOS (CAPON) and serotonin transporter (SERT), with the PSD/Disc-large/ZO-1 homologous (PDZ) domain of nNOS have been demonstrated to influence the subcellular distribution and activity of the enzyme in the brain. Therefore, it will be a preferable means to interfere with nNOS-mediated protein-protein interactions (PPIs), which do not lead to undesirable effects. Herein, we summarize the current literatures on nNOS-mediated PPIs involved in neurological and neuropsychiatric disorders, and the discovery of drugs targeting the PPIs, which is expected to provide potential targets for developing novel drugs and new strategy for the treatment of neurological and neuropsychiatric disorders.
神经和神经精神疾病是全球致残的主要原因之一,影响着数十亿人的健康。一氧化氮(NO)是一种具有多种生物活性的游离气体,主要由大脑中的神经元型一氧化氮合酶(nNOS)将L-精氨酸氧化产生。抑制nNOS对多种神经和神经精神疾病有益,包括中风、抑郁症和焦虑症、创伤后应激障碍、帕金森病、阿尔茨海默病、慢性疼痛和药物成瘾。由于nNOS在学习、记忆和突触可塑性中起关键作用,直接抑制nNOS可能会导致严重的副作用。重要的是,已经证明包括突触后致密蛋白95(PSD-95)、nNOS的羧基末端PDZ配体(CAPON)和5-羟色胺转运体(SERT)在内的几种蛋白质与nNOS的PSD/盘状大蛋白/ZO-1同源(PDZ)结构域相互作用,会影响该酶在大脑中的亚细胞分布和活性。因此,干扰nNOS介导的蛋白质-蛋白质相互作用(PPI)将是一种更可取的方法,这种方法不会产生不良影响。在此,我们总结了目前关于nNOS介导的参与神经和神经精神疾病的PPI的文献,以及靶向这些PPI的药物的发现,有望为开发新型药物提供潜在靶点,并为神经和神经精神疾病的治疗提供新策略。