• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

植物化学物 neo 吉托苷元和沙米苷元有望成为肝细胞生长因子受体靶向癌症治疗的药物。

Phytochemicals Neogitogenin and Samogenin Hold Potentials for Hepatocyte Growth Factor Receptor-Targeted Cancer Treatment.

机构信息

Department of Clinical Laboratory Science, College of Applied Medical Sciences-Qurayyat, Jouf University, Qurayyat, KSA, Saudi Arabia.

Department of Clinical Laboratory Sciences, College of Applied Medical Sciences, Taif University, Taif, Saudi Arabia.

出版信息

OMICS. 2024 Nov;28(11):573-583. doi: 10.1089/omi.2024.0169. Epub 2024 Oct 10.

DOI:10.1089/omi.2024.0169
PMID:39388097
Abstract

Protein kinases are key targets for cancer therapies, with the c-Met receptor tyrosine kinase (MET) and its ligand, hepatocyte growth factor, playing a role in various cancers, including non-small cell lung cancer, gastric cancer, and hepatocellular carcinoma. Although small-molecule inhibitors have been designed to target MET, the development of drug resistance remains a significant challenge to advancing therapeutic strategies. In this study, we employed virtual screening of plant-based compounds sourced from the IMPPAT 2.0 databank to identify potent inhibitors of MET. Preliminary filtering based on the physicochemical parameters following Lipinski's rule of five and pan-assay interference compounds criteria were applied to prioritize hits. Subsequent molecular docking, pharmacokinetic evaluation, prediction of activity spectra for biologically active substances, and specificity assessments facilitated the identification of two promising phytochemicals, neogitogenin and samogenin. Both phytochemicals exhibited considerable drug-like properties with notable binding affinity and selectivity toward MET. Molecular dynamics simulation studies showed the conformational stability of MET with neogitogenin and samogenin. Taken together, these findings suggest that neogitogenin and samogenin hold potential as lead molecules for the development of MET-targeted therapeutics. We call for further evaluations of these phytochemicals in preclinical and experimental studies for anticancer drug discovery and development.

摘要

蛋白激酶是癌症治疗的关键靶点,其中 c-Met 受体酪氨酸激酶(MET)及其配体肝细胞生长因子在多种癌症中发挥作用,包括非小细胞肺癌、胃癌和肝细胞癌。尽管已经设计了针对 MET 的小分子抑制剂,但药物耐药性的发展仍然是推进治疗策略的重大挑战。在这项研究中,我们利用源自 IMPPAT 2.0 数据库的植物化合物进行虚拟筛选,以鉴定 MET 的有效抑制剂。根据 Lipinski 的五规则和 pan-assay interference compounds 标准的物理化学参数进行初步筛选,以优先考虑命中。随后的分子对接、药代动力学评估、生物活性物质的活性谱预测和特异性评估有助于确定两种有前途的植物化学物质,新甘草苷和芝麻素。这两种植物化学物质都表现出相当的类药性,对 MET 具有显著的结合亲和力和选择性。分子动力学模拟研究表明,新甘草苷和芝麻素使 MET 的构象稳定。综上所述,这些发现表明新甘草苷和芝麻素有潜力成为开发 MET 靶向治疗的先导分子。我们呼吁进一步评估这些植物化学物质在癌症药物发现和开发的临床前和实验研究中的作用。

相似文献

1
Phytochemicals Neogitogenin and Samogenin Hold Potentials for Hepatocyte Growth Factor Receptor-Targeted Cancer Treatment.植物化学物 neo 吉托苷元和沙米苷元有望成为肝细胞生长因子受体靶向癌症治疗的药物。
OMICS. 2024 Nov;28(11):573-583. doi: 10.1089/omi.2024.0169. Epub 2024 Oct 10.
2
Identification of Phytochemicals Targeting c-Met Kinase Domain using Consensus Docking and Molecular Dynamics Simulation Studies.利用一致性对接和分子动力学模拟研究鉴定靶向c-Met激酶结构域的植物化学物质。
Cell Biochem Biophys. 2018 Jun;76(1-2):135-145. doi: 10.1007/s12013-017-0821-6. Epub 2017 Aug 29.
3
Structure-guided identification of potent inhibitors of ROS1 kinase for therapeutic development against non-small cell lung cancer.基于结构的 ROS1 激酶强效抑制剂鉴定,用于开发治疗非小细胞肺癌的药物。
J Biomol Struct Dyn. 2024 May;42(8):3837-3847. doi: 10.1080/07391102.2023.2217450. Epub 2023 May 30.
4
identification of potential protein kinase C alpha inhibitors from phytochemicals from IMPPAT database for anticancer therapeutics: a virtual screening approach.从 IMPPAT 数据库中的植物化学物质中鉴定潜在的蛋白激酶 Cα抑制剂,用于癌症治疗:虚拟筛选方法。
J Biomol Struct Dyn. 2024 Nov;42(18):9463-9474. doi: 10.1080/07391102.2023.2252086. Epub 2023 Aug 29.
5
Studying the Binding Modes of Novel 2-Aminopyridine Derivatives as Effective and Selective c-Met Kinase Type 1 Inhibitors Using Molecular Modeling Approaches.采用分子模拟方法研究新型 2-氨基吡啶衍生物作为有效和选择性 c-Met 激酶型 1 抑制剂的结合模式。
Molecules. 2020 Dec 24;26(1):52. doi: 10.3390/molecules26010052.
6
Large-Scale Virtual Screening Against the MET Kinase Domain Identifies a New Putative Inhibitor Type.针对 MET 激酶结构域的大规模虚拟筛选鉴定出一种新型潜在抑制剂类型。
Molecules. 2020 Feb 19;25(4):938. doi: 10.3390/molecules25040938.
7
Searching for Novel Anaplastic Lymphoma Kinase Inhibitors: Structure-Guided Screening of Natural Compounds for a Tyrosine Kinase Therapeutic Target in Cancers.寻找新型间变性淋巴瘤激酶抑制剂:基于结构的天然化合物筛选用于癌症中酪氨酸激酶治疗靶点
OMICS. 2022 Aug;26(8):461-470. doi: 10.1089/omi.2022.0067. Epub 2022 Aug 4.
8
3D-QSAR-aided design of potent c-Met inhibitors using molecular dynamics simulation and binding free energy calculation.基于分子动力学模拟和结合自由能计算的高活性 c-Met 抑制剂的 3D-QSAR 辅助设计。
J Biomol Struct Dyn. 2019 May;37(8):2165-2178. doi: 10.1080/07391102.2018.1479309. Epub 2018 Nov 1.
9
Discovery of promising B lymphocyte kinase inhibitors using structure-guided virtual screening.基于结构引导的虚拟筛选发现有前景的 B 淋巴细胞激酶抑制剂。
J Biomol Struct Dyn. 2024 Aug;42(13):7054-7064. doi: 10.1080/07391102.2023.2256397. Epub 2023 Sep 8.
10
Developing Antagonists for the Met-HGF/SF Protein-Protein Interaction Using a Fragment-Based Approach.采用基于片段的方法开发针对Met-HGF/SF蛋白质-蛋白质相互作用的拮抗剂。
Mol Cancer Ther. 2016 Jan;15(1):3-14. doi: 10.1158/1535-7163.MCT-15-0446. Epub 2015 Dec 28.