Grb2, Growth factor receptor-bound protein 2

  • 文章类型: Journal Article
    未经批准:2019年12月,一种新型冠状病毒,SARS-CoV-2在全球范围内引起一系列急性非典型呼吸道疾病。然而,仍然缺乏疗效明确的药物,疫苗的临床试验研究尚未完全完成。
    UASSIGNED:LH胶囊是批准的中药成药,广泛用于治疗由感冒和流感引起的呼吸道传染病。2020年4月12日,根据通过多中心证明的安全性和有效性,中国食品药品监督管理局(CFDA)正式将LH胶囊和颗粒重新用于轻度COVID-19患者,随机化,对照临床试验。我们希望通过现代药学方法对其进行全面回顾,并试图解释其可能的机制。
    未经授权:使用连花清温黄体胶囊的全称,连花清温和SARS-COV-2、COVID-19作为搜索词的关键词,在各种数据库(如WebofScience和PubMed)中系统地搜索现有的相关论文。并在ClinicalTrials.gov和中国临床试验注册中心完成了临床数据的收集。最后但并非最不重要的,我们通过文献和Selleck整理了LH胶囊的抗炎和抗病毒机制。
    UNASSIGNED:这篇综述系统地梳理了LH胶囊中的活性成分。此外,详细讨论了LH胶囊对SARS-CoV-2,IAV和IBV的相关药理和临床试验。此外,本综述首次概述了LH胶囊中特定物质参与SARS-COV-2感染抗性和抑制IL-6引起的细胞因子风暴综合征(CSS)的潜在分子机制。
    UNASSIGNED:本综述总结了支持使用LH胶囊作为预防和治疗COVID-19的潜在候选药物的现有报告和证据。然而,中医通过多靶点、多途径发挥作用,LH胶囊也不例外。因此,相关机制有待进一步完善和实验验证。
    UNASSIGNED: In December 2019, a novel coronavirus, SARS-CoV-2 caused a series of acute atypical respiratory diseases worldwide. However, there is still a lack of drugs with clear curative effects, and the clinical trial research of vaccines has not been completely finished.
    UNASSIGNED: LH capsules are approved TCM patent medicine that are widely used for the treatment of respiratory tract infectious diseases caused by colds and flu. On April 12, 2020, LH capsules and granules were officially repurposed by the China Food and Drug Administration (CFDA) for patients with mild COVID-19 based on their safety and efficacy demonstrated through multicentre, randomized, controlled clinical trials. We hope to conduct a comprehensive review of it through modern pharmacy methods, and try to explain its possible mechanism.
    UNASSIGNED: Using the full names of LH capsules Lianhuaqingwen, Lianhua Qingwen andSARS-COV-2, COVID-19 as the keywords of the search terms, systemically search for existing related papers in various databases such as Web of Science and PubMed. And completed the collection of clinical data in ClinicalTrials.gov and Chinese Clinical Trial Registry. Last but not least, we have sorted out the anti-inflammatory and antiviral mechanisms of LH capsules through literature and Selleck.
    UNASSIGNED: This review systematically sorted out the active ingredients in LH capsules. Furthermore, the related pharmacological and clinical trials of LH capsule on SARS-CoV-2, IAV and IBV were discussed in detail. Moreover, the present review provides the first summary of the potential molecular mechanism of specific substances in LH capsules involved in resistance to SARS-COV-2 infection and the inhibition of cytokine storm syndrome (CSS) caused by IL-6.
    UNASSIGNED: This review summarizes the available reports and evidence that support the use of LH capsules as potential drug candidates for the prevention and treatment of COVID-19. However, TCM exerts its effects through multiple targets and multiple pathways, and LH capsules are not an exception. Therefore, the relevant mechanisms need to be further improved and experimentally verified.
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  • 文章类型: Journal Article
    含有蛋白酪氨酸磷酸酶2(SHP2)的Src同源性代表了各种疾病的值得注意的靶标,在癌症中作为一种众所周知的致癌磷酸酶。由于细胞渗透性低和生物利用度差,靶向蛋白酪氨酸磷酸催化位点的传统抑制剂通常具有不令人满意的应用功效。最近,已经鉴定出特别大量的对SHP2具有惊人抑制效力的变构抑制剂。特别是,很少有临床试验通过使用SHP2变构抑制剂治疗实体瘤取得重大进展.本文综述了用于肿瘤治疗的小分子SHP2抑制剂的发展和构效关系研究。为了帮助未来开发具有改进选择性的SHP2抑制剂,更高的口服生物利用度和更好的理化性质。
    Src homology containing protein tyrosine phosphatase 2 (SHP2) represents a noteworthy target for various diseases, serving as a well-known oncogenic phosphatase in cancers. As a result of the low cell permeability and poor bioavailability, the traditional inhibitors targeting the protein tyrosine phosphate catalytic sites are generally suffered from unsatisfactory applied efficacy. Recently, a particularly large number of allosteric inhibitors with striking inhibitory potency on SHP2 have been identified. In particular, few clinical trials conducted have made significant progress on solid tumors by using SHP2 allosteric inhibitors. This review summarizes the development and structure-activity relationship studies of the small-molecule SHP2 inhibitors for tumor therapies, with the purpose of assisting the future development of SHP2 inhibitors with improved selectivity, higher oral bioavailability and better physicochemical properties.
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  • 文章类型: Journal Article
    多形性胶质母细胞瘤(GBM)是最常见的脑肿瘤类型,并且是致命的。这种疾病的社区治疗标准是肿瘤的总切除或次全切除,其次是辐射和替莫唑胺。在复发时,可以添加贝伐单抗以增加无进展生存期。在试图设计治疗GBM的新药时遇到了许多挑战,例如血脑屏障的存在是大多数药物不可渗透的。因此,在过去的几年中,注意力转向用于治疗这种破坏性疾病的免疫手段。EGFRvIII靶向已被证明是通过使用免疫系统攻击胶质母细胞瘤细胞的好方法。虽然还在发展中,这种方法有望成为免疫定制药物治疗脑癌的第一步。
    Glioblastoma Multiforme (GBM) is the most common type of brain tumor and it is uniformly fatal. The community standard of treatment for this disease is gross or subtotal resection of the tumor, followed by radiation and temozolomide. At recurrence bevacizumab can be added for increased progression free survival. Many challenges are encountered while trying to devise new drugs to treat GBM, such as the presence of the blood brain barrier which is impermeable to most drugs. Therefore in the past few years attention was turned to immunological means for the treatment of this devastating disease. EGFRvIII targeting has proven a good way to attack glioblastoma cells by using the immune system. Although in still in development, this approach holds the promise as a great first step toward immune-tailored drugs for the treatment of brain cancers.
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