MDM2抑制剂的化学分类

Chiragkumar J. Gohil, M. Noolvi, C. Patel, D. Sen
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引用次数: 2

摘要

MDM2抑制剂类抗肿瘤药物是在nutlins等强效抑制剂的成功发现后发展起来的。MDM2抑制剂可以选择性地重新激活肿瘤细胞中被抑制的p53功能,从而特异性靶向体内的肿瘤细胞。该类化合物目前尚未上市,均处于临床试验阶段。因此,各种研究人员根据它们的p53拓扑模拟特性以及它们的肽型或非肽型对它们进行分类。合成的多肽型抑制剂可以模拟p53的螺旋构象。而有机小分子(非肽)型MDM2抑制剂又被进一步细分为非α-螺旋类抑制剂(小分子抑制剂)和α-螺旋类抑制剂。在合成抑制剂的行列中,许多有效的MDM2抑制剂来源于天然来源(海洋,真菌)。因此,考虑到所有这些特征,我们在这里根据我们所知的最好的知识对它们进行分类。
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Chemical classification of MDM2 inhibitors
MDM2 inhibitors class of anti-neoplastic drugs has been evolve after the successful discovery of the nutlins and other potent inhibitors. MDM2 inhibitors can specifically target the tumour cells in the body, by selectively reactivating the inhibited p53 function in the tumour cells.None of the compound of this class has been entered into the market till date, all are under clinical trials. Hence, various researcher classifies them according to their p53 topology mimetic property and as per their peptide type or non-peptide type.Synthetic peptide type of inhibitors can mimic the conformation of p53 helix. Whereas, small organic molecule (non-peptide) type of MDM2 inhibitors have been further subdivided as Non α-helix mimetics (small molecule inhibitors) and α-helix mimetics. In a line with synthetic inhibitors, many potent MDM2 inhibitors are derived from the natural origin (marine, fungus). Therefore, keeping in a view of all these characteristics, here we have classified them as per best of our knowledge.
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