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首页> 外文OA文献 >Inhibition of triosephosphate isomerase from Trypanosoma brucei with cyclic hexapeptides.
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Inhibition of triosephosphate isomerase from Trypanosoma brucei with cyclic hexapeptides.

机译：用环状六肽抑制布鲁氏锥虫的磷酸三糖异构酶。

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摘要

Two series of oligopeptides have been synthesized. Their effects on the activity of purified triosephosphate isomerase from Trypanosoma brucei and various other organisms have been studied. Using detailed three-dimensional structure information, the first series consisted of both cyclic and linear hydrophilic peptides that were designed to mimic the beta turns of the subunit interface loops of the trypanosome triosephosphate isomerase dimer. None of these exerted any inhibitory effect. The second series consisted of more hydrophobic cyclic peptides, originally designed to inhibit a hepatic transport system. Several of these were very effective in inhibiting the trypanosome triosephosphate isomerase, but not the homologous enzymes from rabbit, dog, yeast or Escherichia coli. The most active peptide, cyclo[-Trp-Phe-D-Pro-Phe-Phe-Lys(Z)-], exerted 50% inhibitory activity at a concentration of 3 microM. The nature of the inhibitory action of one of these compounds cyclo[-Trp-Tyr(OSO3Na)-D-Pro-Phe-Thr(OSO3Na)-Lys(Z)-] was studied in more detail. Its inhibition was noncompetitive and reversible and more than one peptide was able to bind/active site.
机译：已经合成了两个系列的寡肽。已经研究了它们对来自布鲁氏锥虫和各种其他生物的纯化的磷酸丙糖异构酶活性的影响。使用详细的三维结构信息，第一个系列由环状和线性亲水性肽组成，这些肽被设计为模仿锥虫三糖磷酸异构酶二聚体的亚基界面环的β角。这些都没有发挥任何抑制作用。第二个系列由更多的疏水性环肽组成，最初设计为抑制肝转运系统。其中一些对抑制锥虫磷酸三糖异构酶非常有效，但对抑制兔，狗，酵母或大肠杆菌的同源酶无效。活性最高的肽环[-Trp-Phe-D-Pro-Phe-Phe-Lys（Z）-]在3 microM的浓度下具有50％的抑制活性。对这些化合物之一的环[-Trp-Tyr（OSO3Na）-D-Pro-Phe-Thr（OSO3Na）-Lys（Z）-]的抑制作用的性质进行了更详细的研究。其抑制作用是非竞争性的和可逆的，并且一种以上的肽能够结合/激活位点。

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