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Hydroxamic acid – A novel molecule for anticancer therapy

机译:异羟肟酸-一种用于抗癌治疗的新型分子

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Hydroxamic acid is a potent moiety not only in the field of cancer therapy but also as a mutagenic agent. Among the various derivatives of hydroxamic acid, SAHA (Suberoylanilide Hydroxamic Acid) is considered as a potent anticancer agent. Scientists from the different corner synthesized different hydroxamic acid moieties with some straight chain oxazole, thiadiazole, biphenyl moieties in the terminal position. Acetylation and deacetylation of histones of the core proteins of nucleosomes in chromatin play an important role in the regulation of gene expression. The level of acetylation of histones is established and maintained by two classes of enzymes, histone acetyltransferase and histone deacetylases, which have been identified as transcriptional coactivators and transcriptional corepressors, respectively. There is increasing evidence that aberrant histone acetylation has been linked to various malignant diseases. Great efforts are currently underway for the design of more potent and less toxic candidates for the treatment of cancer. In recent years, hydroxamic acid derivatives have attracted increasing attention for their potential as highly efficacious in combating various etiological factors associated with cancer. Our main intention to draw an attention is that this single functional moiety has not only fit in the receptor but also create a diversified activity.Keywords: Cancer, histone deacetylase, hydroxamic acid, MMP inhibitor
机译:异羟肟酸不仅是癌症治疗领域中的有效部分,而且还是诱变剂。在异羟肟酸的各种衍生物中,SAHA(Suberoylanilide Hydroxamic Acid)被认为是有效的抗癌剂。来自不同角落的科学家合成了不同的异羟肟酸部分,其末端位置带有一些直链恶唑,噻二唑,联苯部分。染色质中核小体核心蛋白组蛋白的乙酰化和去乙酰化在调节基因表达中起重要作用。组蛋白的乙酰化水平由两类酶(组蛋白乙酰转移酶和组蛋白脱乙酰基酶)确定和维持,这两类酶分别被确定为转录共激活因子和转录共加压因子。越来越多的证据表明异常的组蛋白乙酰化已与各种恶性疾病有关。目前正在进行巨大的努力来设计用于治疗癌症的更有效和更低毒性的候选药物。近年来,异羟肟酸衍生物因其在对抗与癌症相关的各种病因方面具有高度功效的潜力而受到越来越多的关注。我们要引起注意的主要目的是,这个单一功能部分不仅适合受体,而且还具有多种活性。关键词:癌症,组蛋白脱乙酰基酶,异羟肟酸,MMP抑制剂

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