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Design of Histone Deacetylase Inhibitors with Chlamydocin Framework containing Various Imino Acids instead of Proline Residue

机译:用含有各种亚氨基酸代替脯氨酸残基的衣原体甲酰胺骨架组蛋白脱乙酰酶抑制剂的设计

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The cyclic tetrapeptide chlamydocin, originally isolated from fungus Diheterospora chlamydosphoria, is one of the naturally-occurring inhibitors of histone deacetylases [1]. Strucure of chlammydocin is cyclo(-L-Aoe-Aib-L-Phe- D-Pro-), where Aoe is L-amino-8-oxo-9,10-epoxydecanoic acid. Recently we have synthesized and tested histone deacetylase inhibitory activities of chlamydocin hydroxamic acid analogs [2,3].
机译:循环四肽衣原体最初从真菌二孢子孢子醇氯酰磷酰磷酰磷苷中分离,是组蛋白脱乙酰酶的天然存在的抑制剂中的一种[1]。 Chlammydocin的结构是Cyclo(-L-AOE-AIB-L-PHE-),其中AoE是L-氨基-8-氧代-9,10-环氧二烷酸。最近我们已经合成和测试了衣原体羟肟酸类似物的组蛋白脱乙酰酶抑制活性[2,3]。

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