摘要
背景:烟曲霉毒素是霉菌毒素,但也可以抑制癌细胞并逆转其耐药性。 目的:讨论异戊烯化的环-Trp-Pro二肽及其衍生物在抗癌治疗中的应用的生物活性。 方法:这个类别的真菌化合物的发现和评估的报告是从谷歌学术和PubMed文献汇编。讨论天然化合物的生物活性,目的在于改善癌症疗法。 结果:虽然已经发现了一些这类化合物,但是在应用的生物测定中只有少数表现出了生物活性。烟曲霉毒素和相关化合物对各种癌细胞有活性,但它们也是霉菌毒素。这些天然化合物中的一些可以阻止癌细胞在其细胞周期中,并且一些可以阻断ABC转运蛋白并且在化学疗法中逆转耐药性。已经推断出结构活性关系导致预测高活性化合物。已经发现这些天然产物的几种易得到的衍生物具有高选择性和无毒性。 结论:高级筛选方法,高通量筛选,代谢工程和合成生物学是寻找高活性药物的新颖有前途的技术。与工程生物合成途径相结合的快速基因测序应该对新型制药学有重大贡献。
关键词: 二酮哌嗪,环二肽,烟曲霉毒素,cyclotryprostatin,norgeamide,抗癌,耐药性,ABCG2转运蛋白
Current Medicinal Chemistry
Title:Fumitremorgins and Relatives – From Tremorgenic Compounds to Valuable Anti-Cancer Drugs
Volume: 25 Issue: 2
关键词: 二酮哌嗪,环二肽,烟曲霉毒素,cyclotryprostatin,norgeamide,抗癌,耐药性,ABCG2转运蛋白
摘要: Background: Fumitremorgins are mycotoxins but can also inhibit cancer cells and reverse their drug resistance.
Objective: The bioactivity of prenylated cyclo-Trp-Pro dipeptides and their derivatives concerning their application in anti-cancer therapies will be discussed.
Methods: Reports on the discovery and assessment of this class of fungal compounds are compiled from literature using Google Scholar and PubMed. The bioactivities of the natural compounds are discussed with the aim of their improvement for cancer therapy.
Results: Although a number of compounds of this class have been found, only a minority of them showed bioactivity in the applied bioassays. Fumitremorgins and related compounds are active against various cancer cells but they are also mycotoxins. Some of these natural compounds can arrest cancer cells in their cell cycle and some can block ABC-transporters and reverse resistance in chemotherapy. Structure activity relationships have been deduced leading to the prediction of highly active compounds. Several easily accessible derivatives of these natural products have been discovered being highly selective and non-toxic.
Conclusion: Sophisticated screening methods, high throughput screening, metabolic engineering, and synthetic biology are novel and promising technologies for the search for highly active drugs. Rapid gene sequencing in combination with engineered biosynthetic pathways should contribute substantially to novel pharmaceutics.
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Cite this article as:
Fumitremorgins and Relatives – From Tremorgenic Compounds to Valuable Anti-Cancer Drugs, Current Medicinal Chemistry 2018; 25 (2) . https://dx.doi.org/10.2174/0929867324666170724103410
DOI https://dx.doi.org/10.2174/0929867324666170724103410 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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