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Review Article

瞄准读者！ Bromodomains作为对抗南美锥虫病的新目标

卷 26, 期 36, 2019

页: [6544 - 6563] 页: 20

弟呕挨: 10.2174/0929867325666181031132007

价格: $65

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摘要

溴结构域以特定方式识别并结合组蛋白和非组蛋白中存在的乙酰赖氨酸残基。在过去的十年中，由于人们对人类溴结构域的调控失调与多种疾病的发展有关，它们已成为药物开发的有吸引力的目标。但是，靶向真核病原菌bromodomains仍几乎未被开发。我们和其他人已经报道了原生动物中各种含溴结构域蛋白的必要性，这为抗寄生虫药物的开发提供了新的机遇，特别是恰加斯锥虫病（恰加斯氏病的病原体）。哺乳动物的溴结构域根据序列相似性分为八类，但寄生的溴结构域是非常不同的蛋白质，很难将它们分配给任何这些组，这表明可以得到选择性抑制剂。在这篇综述中，我们描述了T. cruzi中赖氨酸乙酰化和溴结构域的重要性以及关于哺乳动物溴结构域的当前知识。另外，我们总结了正在研究的用于治疗不同病理的无数小分子，其中哪些已在锥虫和其他原生动物中进行了测试。所有可用的信息促使我们提出，应将克鲁氏梭菌溴结构域视为重要的潜在靶标，并应寻求抑制它们的小分子。

关键词: 溴结构域，克氏锥虫，乙酰化，溴结构域抑制剂，恰加斯病，药物发现。

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