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