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首页> 外文期刊>The Journal of Antibiotics: An International Journal >Oleamycins A and B: New antibacterial cyclic hexadepsipeptides isolated from a terrestrial Streptomyces sp.
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Oleamycins A and B: New antibacterial cyclic hexadepsipeptides isolated from a terrestrial Streptomyces sp.

机译:Oleamycins A和B:从陆地链霉菌属(Streptomyces sp。)分离出的新的抗菌环六​​肽肽。

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摘要

Menin is an essential co-factor of oncogenic MLL fusion proteins and the menin-MLL interaction is critical for development of acute leukemia in vivo. Targeting the menin-MLL interaction with small molecules represents an attractive strategy to develop new anticancer agents. Recent developments, including determination of menin crystal structure and development of potent small molecule and peptidomimetic inhibitors, demonstrate the feasibility of targeting the menin-MLL interaction. On the other hand, biochemical and structural studies revealed that MLL binds to menin in a complex bivalent mode engaging two MLL motifs, and therefore inhibition of this protein-protein interaction represents a challenge. This review summarizes the most recent achievements in targeting the menin-MLL interaction as well as discusses potential benefits of blocking menin in cancer.
机译:Menin是致癌MLL融合蛋白的重要辅助因子,而Menin-MLL相互作用对于体内急性白血病的发展至关重要。靶向与小分子的脑膜蛋白-MLL相互作用代表了开发新的抗癌药的有吸引力的策略。最近的发展,包括确定Menin晶体结构以及开发有效的小分子和拟肽抑制剂,证明了靶向Menin-MLL相互作用的可行性。另一方面,生化和结构研究表明,MLL以参与两个MLL基序的复杂的二价模式与Menin结合,因此抑制这种蛋白-蛋白相互作用是一个挑战。这篇综述总结了针对menin-MLL相互作用的最新成就,并讨论了阻断menin在癌症中的潜在益处。

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