Molecular targeted approaches to cancer therapy and prevention using chalcones.
Molecular targeted approaches to cancer therapy and prevention using chalcones.
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DOI：
10.2174/1568009614666140122160515
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发表时间：
2014
影响因子：
3
通讯作者：
Zi X
中科院分区：
文献类型：
--
作者：
Jandial DD;Blair CA;Zhang S;Krill LS;Zhang YB;Zi X
在肿瘤学中，正在出现一种新的范式转变，试图强调癌症预防和治疗的分子靶向方法。查尔酮(1，3-二苯基-2-丙酮-1-酮)是一种天然存在的化合物，广泛存在于香料、茶叶、啤酒、水果和蔬菜中，由开链类黄酮组成，其中两个芳环由三碳α，β-不饱和羰基体系连接。由于它们的结构多样性、相对容易的化学操作以及α，β不饱和的羰基部分与蛋白质中的半胱氨酸残基的反应，一些来自天然产物和合成产物的铅查尔酮已在各种筛选方法中被鉴定出来，用于调节癌症中的重要途径或分子靶标。这些受查尔酮影响的通路和靶点包括MDM2/P53、微管蛋白、蛋白酶体、核因子-kappaB、试验/死亡受体和线粒体介导的凋亡通路、细胞周期、STAT3、AP-1、NRF2、AR、ER、PPAR-γ和β-Catenin/Wnt。与目前的癌症靶向治疗药物相比，查尔酮具有价格低廉、容易获得和毒性小的优点；从取代的苯甲醛和苯乙酮合成查尔酮也使其成为一种有吸引力的药物支架。因此，本文就查尔酮类化合物的分子靶点及其在癌症防治中的潜在意义作一综述。
There is an emerging paradigm shift in oncology that seeks to emphasize molecularly targeted approaches for cancer prevention and therapy. Chalcones (1,3-diphenyl-2-propen-1-ones), naturally-occurring compounds with widespread distribution in spices, tea, beer, fruits and vegetables, consist of open-chain flavonoids in which the two aromatic rings are joined by a three-carbon α, β-unsaturated carbonyl system. Due to their structural diversity, relative ease of chemical manipulation and reaction of α, β-unsaturated carbonyl moiety with cysteine residues in proteins, some lead chalcones from both natural products and synthesis have been identified in a variety of screening assays for modulating important pathways or molecular targets in cancers. These pathways and targets that are affected by chalcones include MDM2/p53, tubulin, proteasome, NF-kappa B, TRIAL/death receptors and mitochondria mediated apoptotic pathways, cell cycle, STAT3, AP-1, NRF2, AR, ER, PPAR-γ and β-catenin/Wnt. Compared to current cancer targeted therapeutic drugs, chalcones have the advantages of being inexpensive, easily available and less toxic; the ease of synthesis of chalcones from substituted benzaldehydes and acetophenones also makes them an attractive drug scaffold. Therefore, this review is focused on molecular targets of chalcones and their potential implications in cancer prevention and therapy.
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影响因子：
3
作者：
De Vincenzo, R;Ferlini, C;Scambia, G
通讯作者：
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3.2
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