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Targeting allosteric regulation of cancer metabolism
Nature Chemical Biology ( IF 14.8 ) Pub Date : 2022-04-28 , DOI: 10.1038/s41589-022-00997-6
Daniel M Kremer 1, 2, 3 , Costas A Lyssiotis 1, 4, 5
Affiliation  

Metabolic reprogramming is observed across all cancer types. Indeed, the success of many classic chemotherapies stems from their targeting of cancer metabolism. Contemporary research in this area has refined our understanding of tumor-specific metabolic mechanisms and has revealed strategies for exploiting these vulnerabilities selectively. Based on this growing understanding, new small-molecule tools and drugs have been developed to study and target tumor metabolism. Here, we highlight allosteric modulation of metabolic enzymes as an attractive mechanism of action for small molecules that target metabolic enzymes. We then discuss the mechanistic insights garnered from their application in cancer studies and highlight the achievements of this approach in targeting cancer metabolism. Finally, we discuss technological advances in drug discovery for allosteric modulators of enzyme activity.



中文翻译:

靶向癌症代谢的变构调节

在所有癌症类型中都观察到代谢重编程。事实上,许多经典化疗的成功源于它们对癌症代谢的靶向治疗。该领域的当代研究加深了我们对肿瘤特异性代谢机制的理解,并揭示了选择性利用这些漏洞的策略。基于这种不断增长的理解,已经开发出新的小分子工具和药物来研究和靶向肿瘤代谢。在这里,我们强调代谢酶的变构调节是针对代谢酶的小分子的一种有吸引力的作用机制。然后,我们讨论了从它们在癌症研究中的应用中获得的机制见解,并强调了这种方法在靶向癌症代谢方面的成就。最后,

更新日期:2022-04-29
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