网络药理学和分子对接分析揭示KarXT和氯氮平治疗精神分裂症的共同和独特的治疗靶点:对差异临床反应的影响

IF 6.9 2区 医学 Q1 CLINICAL NEUROLOGY
Chuanjun Zhuo, Chao Li, Hongjun Tian, Lina Wang, Xiaoyan Ma, Ranli Li, Ximing Chen, Yachen Li, Qiuyu Zhang, Lei Yang
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引用次数: 0

摘要

Xanomeline + trospium (KarXT)是一种靶向毒蕈碱受体的联合药物,对精神分裂症的阳性、阴性和认知症状都有疗效,尽管对阳性和阴性症状的治疗效果与利培酮和奥氮平没有显著差异。氯氮平仍然是对其他抗精神病药物无反应的精神分裂症最有效的治疗方法,与利培酮和奥氮平相比,氯氮平对阳性和阴性症状的疗效更佳。然而,这些对KarXT和氯氮平的不同临床反应背后的共同和独特的分子靶点尚不完全清楚。通过搜索PharmMapper、SwissTargetPrediction、GeneCards和SuperPred确定潜在的xanomeline和氯氮平靶点,通过搜索GeneCards、OMIM和TTD确定与精神分裂症相关的靶点。构建蛋白-蛋白相互作用(PPI)网络来识别枢纽靶点,并使用DAVID对前25个靶点进行GO和KEGG途径富集分析。Cytoscape用于构建连接药物、途径、靶点和疾病的网络。通过分子对接模拟来评估药物与核心靶点的结合亲和力。结合数据库搜索,确定了103个xanomeline和精神分裂症的重叠靶点,285个氯氮平和精神分裂症的重叠靶点。PPI网络和KEGG通路分析发现,FOS、CASP3、NFKB1、AKT1、IGF1、KDR和CDC42这些与凋亡、炎症、神经保护和MAPK信号相关的蛋白是异丙素的核心靶点,而FOS、CASP3、NFKB1、TNF、IL6、IFNG和CXCL8这些与凋亡、炎症、免疫反应和IL-17信号相关的蛋白是氯氮平的核心靶点。分子对接证实了药物与核心靶点的强结合。KarXT和氯氮平有共同的核心靶点FOS、CASP3和NFKB1。不同的KarXT靶点如AKT1、IGF1、KDR和CDC42,以及氯氮平靶点包括TNF、IL6、IFNG和CXCL8可能解释了治疗效果的差异。这些生物信息学发现支持了最近的荟萃分析,并为更合适的药物选择提供了指导。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Shared and unique therapeutic targets of KarXT and clozapine for schizophrenia treatment revealed by network pharmacology and molecular docking analyses: Implications for differential clinical responses.

Xanomeline plus trospium (KarXT) is a combination drug targeting muscarinic receptors with demonstrated efficacy against positive, negative, and cognitive symptoms of schizophrenia, although therapeutic effects on positive and negative symptoms do not differ significantly from risperidone and olanzapine. Clozapine remains the most effective treatment for schizophrenia unresponsive to other antipsychotics and demonstrates superior efficacy for positive and negative symptoms compared to risperidone and olanzapine. However, the common and distinct molecular targets underlying these different clinical responses to KarXT and clozapine are not fully understood. Potential xanomeline and clozapine targets were identified by searching PharmMapper, SwissTargetPrediction, GeneCards, and SuperPred, and schizophrenia-related targets by searching GeneCards, OMIM, and TTD. Protein-protein interaction (PPI) networks were constructed to identify hub targets, and GO and KEGG pathway enrichment analyses were conducted for the top 25 targets using DAVID. Cytoscape was used to build a network linking drugs, pathways, targets, and disease. Molecular docking simulations were conducted to assess drug binding affinities to core targets. Combined database searches identified 103 overlapping targets for xanomeline and schizophrenia, and 285 overlapping targets for clozapine and schizophrenia. PPI network and KEGG pathway analyses identified FOS, CASP3, NFKB1, AKT1, IGF1, KDR, and CDC42, proteins related to apoptosis, inflammation, neuroprotection, and MAPK signaling, as core xanomeline targets, and FOS, CASP3, NFKB1, TNF, IL6, IFNG, and CXCL8, proteins involved in apoptosis, inflammation, immune responses, and IL-17 signaling, as core clozapine targets. Molecular docking confirmed strong binding between drugs and core targets. KarXT and clozapine share core targets FOS, CASP3, and NFKB1. Distinct KarXT targets such as AKT1, IGF1, KDR, and CDC42, and clozapine targets including TNF, IL6, IFNG, and CXCL8 may explain differences in therapeutic efficacy. These bioinformatics findings support recent meta-analyses and provide guidance for more appropriate drug selection.

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来源期刊
Neurotherapeutics
Neurotherapeutics 医学-神经科学
CiteScore
11.00
自引率
3.50%
发文量
154
审稿时长
6-12 weeks
期刊介绍: Neurotherapeutics® is the journal of the American Society for Experimental Neurotherapeutics (ASENT). Each issue provides critical reviews of an important topic relating to the treatment of neurological disorders written by international authorities. The Journal also publishes original research articles in translational neuroscience including descriptions of cutting edge therapies that cross disciplinary lines and represent important contributions to neurotherapeutics for medical practitioners and other researchers in the field. Neurotherapeutics ® delivers a multidisciplinary perspective on the frontiers of translational neuroscience, provides perspectives on current research and practice, and covers social and ethical as well as scientific issues.
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