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Synthesis and Biological Activities of Proline Rich Cyclic Heptapeptide Hymemanide B Analogs

机译:脯氨酸富循环肽Hexapeptide HymeManide B类似物的合成与生物活性

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The isolation of a great variety of biological active materials from marine organisms has been reported. Many types of these bioactive compounds are cyclic peptides. Cyclic peptides have metabolic stabilities and restricted conformations. Since these characters play a key role for biological activities, cyclic peptides have been the focus as pharmacological targets. One class of these cyclic peptides, named hymenamides, has been isolated from Okinawan marine sponge Hymeniacidon sp. . This peptide family contains proline and hydrophobic residues with high frequency and shows high cytotoxic activity, antifungal activity, and occasionally works as enzymatic inhibitor. However, it is difficult to secure enough amounts of natural product for physiological estimation by isolation. Therefore, to further explore these peptides, it is necessary to chemically synthesize them to obtain sufficient amounts to perform structure-function relationships studies.
机译:报道了分离来自海洋生物的各种各样的生物活性材料。 许多类型的这些生物活性化合物是环肽。 环状肽具有代谢稳定性和限制构象。 由于这些角色为生物活性发挥着关键作用,因此循环肽已成为药理靶标的焦点。 这些循环肽的一类名为Hymenamides,已从冲绳海洋海绵Hymeniacidon Sp中分离出来。 。 该肽家族含有高频率的脯氨酸和疏水性残基,并显示出高细胞毒性活性,抗真菌活性,偶尔作为酶促抑制剂。 然而,难以通过隔离来确保足够量的天然产物进行生理估计。 因此,为了进一步探索这些肽,需要化学合成它们以获得足够的量以进行结构 - 功能关系研究。

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