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首页> 外文期刊>RSC Advances >Prospects for multitarget lipid-raft-coated silica beads: a remarkable online biomaterial for discovering multitarget antitumor lead compounds
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Prospects for multitarget lipid-raft-coated silica beads: a remarkable online biomaterial for discovering multitarget antitumor lead compounds

机译：多目标脂质筏包覆的二氧化硅微珠的前景：发现多目标抗肿瘤铅化合物的卓越在线生物材料

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摘要

A recently discovered receptor-rich lipid raft, which is linked to numerous transmembrane signal transduction pathways, has emerged as a medically significant biomaterial for screening antitumor agents. Compounds that interact with the biomaterial might potentially inhibit cancer cell growth, and thus be valuable as antitumor agents. Two standard anticancer drugs, lestaurtinib and gefitinib, interacted with the tropomyosin-related tyrosine kinase A (TrkA) receptor-rich lipid raft. The fact that they are both well known inhibitors of TrkA receptor strengthened the observed linkage. There is now a considerable interest in developing other related biomaterials to serve a similar purpose, and more importantly, support the concept of multitarget drug discovery. It is expected that new anticancer drugs strategically act on multiple pathways to achieve optimal therapeutic efficacies and decreased stimulation of acquired resistance. However, the current conventional approaches such as chemical screening systems and in silico methods cannot fully satisfy the increasing demand for the therapeutic agents. It has therefore become imperative to explore other alternatives to increase the number of clinically important antitumor agents. Here, we report the prospect of establishing lipid raft biomaterial with well endowed multiple cancer-related receptors for screening antitumor leads that affect multiple pathways. This review also examines receptor-ligand interactions in the hunt for novel antitumor agents and the associated key receptors.
机译：与许多跨膜信号转导途径相关的最近发现的富含受体的脂质筏已经作为筛选抗肿瘤剂的医学上重要的生物材料出现。与生物材料相互作用的化合物可能潜在地抑制癌细胞的生长，因此作为抗肿瘤剂非常有价值。两种标准的抗癌药物，lestaurtinib和gefitinib，与原肌球蛋白相关的酪氨酸激酶A（TrkA）受体丰富的脂质筏相互作用。它们都是众所周知的TrkA受体抑制剂的事实加强了观察到的联系。现在，人们非常关注开发其他相关的生物材料以达到类似的目的，更重要的是，它支持多目标药物发现的概念。可以预期，新的抗癌药物将策略性地作用于多种途径，以达到最佳的治疗效果并减少对获得性耐药的刺激。但是，当前的常规方法，例如化学筛选系统和计算机模拟方法不能完全满足对治疗剂的日益增长的需求。因此，必须探索其他替代方法以增加临床上重要的抗肿瘤药物的数量。在这里，我们报告建立具有丰富的多种癌症相关受体的脂质筏生物材料以筛选影响多种途径的抗肿瘤药物的前景。这篇综述还探讨了寻找新的抗肿瘤药物和相关关键受体的受体-配体相互作用。

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