Abdelbaset Mohamed Elasbali, Farah Anjum, Bodour Ali Al-Ghabban, Alaa Shafie, Taj Mohammad, Md Imtaiyaz Hassan
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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.</p>","PeriodicalId":2,"journal":{"name":"ACS Applied Bio Materials","volume":null,"pages":null},"PeriodicalIF":4.6000,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Phytochemicals Neogitogenin and Samogenin Hold Potentials for Hepatocyte Growth Factor Receptor-Targeted Cancer Treatment.\",\"authors\":\"Abdelbaset Mohamed Elasbali, Farah Anjum, Bodour Ali Al-Ghabban, Alaa Shafie, Taj Mohammad, Md Imtaiyaz Hassan\",\"doi\":\"10.1089/omi.2024.0169\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>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. 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引用次数: 0
摘要
蛋白激酶是癌症疗法的关键靶点,c-MET受体酪氨酸激酶(MET)及其配体肝细胞生长因子在非小细胞肺癌、胃癌和肝细胞癌等多种癌症中发挥着作用。虽然已设计出针对 MET 的小分子抑制剂,但耐药性的产生仍是推进治疗策略的重大挑战。在本研究中,我们采用虚拟筛选的方法,从 IMPPAT 2.0 数据库中获取植物化合物,以确定 MET 的强效抑制剂。按照利宾斯基的 "5 "法则和泛试干扰化合物标准,根据理化参数进行初步筛选,以确定命中化合物的优先次序。随后进行的分子对接、药物动力学评估、生物活性物质活性光谱预测和特异性评估有助于鉴定出两种有前景的植物化学物质--新吉托苷元和翅果苷元。这两种植物化学物质都表现出相当强的类药物特性,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,MET 与新黑木皂苷元和翅果皂苷元的构象具有稳定性。综上所述,这些研究结果表明,新黑木耳苷元和翅果苷元有可能成为开发 MET 靶向治疗药物的先导分子。我们呼吁在抗癌药物发现和开发的临床前和实验研究中进一步评估这些植物化学物质。
Phytochemicals Neogitogenin and Samogenin Hold Potentials for Hepatocyte Growth Factor Receptor-Targeted Cancer Treatment.
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.