Transforming bivalent ligands into retractable enzyme inhibitors through polypeptide-protein interactions.

Tolkatchev D; Vinogradova A; Ni F

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Transforming bivalent ligands into retractable enzyme inhibitors through polypeptide-protein interactions.

机译：通过多肽-蛋白质相互作用将二价配体转化为可伸缩的酶抑制剂。

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The concept of bivalent polypeptides with controllable flexible linkers is demonstrated through the design of a new generation of 'antidote'-reversible inhibitors of thrombin. These molecules contain two binding moieties, each of which in isolation has only a moderate affinity of binding, which are linked together by a flexible peptide bridge. We show that activities of the potent bivalent inhibitors of thrombin can be reversed by the specific, but much weaker, binding of the linker moiety to protein 'antidotes'.

机译：通过设计新一代的“解毒剂”可逆性凝血酶抑制剂，可以证明具有可控柔性接头的二价多肽的概念。这些分子含有两个结合部分，每个结合部分仅具有中等的结合亲和力，它们通过柔性肽桥连接在一起。我们表明，凝血酶的有效二价抑制剂的活性可以通过连接子部分与蛋白质“解毒剂”的特异性结合（但弱得多）来逆转。

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《Bioorganic and Medicinal Chemistry Letters》 |2005年第23期|共4页
作者
Tolkatchev D; Vinogradova A; Ni F;
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正文语种 eng
中图分类基础医学;
关键词
Peptides; binding; Proteins; inhibitors; Thrombin; 肽类; 蛋白质类; 凝血酶;

机译：Peptides;binding;Proteins;inhibitors;Thrombin;肽类;蛋白质类;凝血酶;

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1. Transforming bivalent ligands into retractable enzyme inhibitors through polypeptide-protein interactions. [J] . Tolkatchev D, Vinogradova A, Ni F Bioorganic and Medicinal Chemistry Letters . 2005,第23期

机译：通过多肽-蛋白质相互作用将二价配体转化为可伸缩的酶抑制剂。
2. A set of phosphatase-inert "molecular rulers" to probe for bivalent mannose 6-phosphate ligand-receptor interactions. [J] . Fei X, Connelly CM, MacDonald RG, Bioorganic and Medicinal Chemistry Letters . 2008,第10期

机译：一组磷酸酶惰性的“分子尺”，用于探测二价甘露糖6-磷酸配体-受体的相互作用。
3. A set of phosphatase-inert "molecular rulers" to probe for bivalent mannose 6-phosphate ligand-receptor interactions. [J] . Fei X, Connelly CM, MacDonald RG, Bioorganic and Medicinal Chemistry Letters . 2008,第10期

机译：一组磷酸酶惰性的“分子尺”，用于探测二价甘露糖6-磷酸配体-受体的相互作用。
4. Polypeptide Ligands Containing Switchable Flexible Linkers Retractable Inhibitors of Protein-Protein Interactions [C] . Dmitri Tolkatchev, Anna Vinogradova, Rana Filfil American Peptide Symposium . 2006

机译：多肽配体含有可切换的柔性接头，可伸缩蛋白质 - 蛋白质相互作用的抑制剂
5. Part One. Synthesis of optically active tryptophan derivatives with potential activity as indoleamine 2,3-dioxygenase inhibitors: An approach via asymmetric catalytic hydrogenation. Part Two. Design, synthesis and pharmacology of selective ligands for alpha1-containing GABA(A)/benzodiazepine receptor subtypes: SAR studies of beta-carbolines at positions -3 and -6 and their corresponding bivalent ligands. Part Three. First enantiospecific total synthesis of the important biogenetic intermediates, (+)-polyneuridine and (+)-polyneuridine aldehyde, as well as 16-epi-vellosimine and macusine A. [D] . Yin, Wenyuan. 2007

机译：第一部分。具有吲哚胺2,3-二加氧酶抑制剂潜在活性的旋光色氨酸衍生物的合成：一种通过不对称催化氢化的方法。第二部分。含α1的GABA（A）/苯并二氮杂receptor受体亚型的选择性配体的设计，合成和药理作用：位于-3和-6位的β-咔啉及其相应的二价配体的SAR研究。第三部分。重要生物遗传中间体，（+）-聚神经氨酸和（+）-聚神经氨酸醛，以及16-表-维西辛和Macusine A的首次对映体全合成。
6. Examining the influence of specificity ligands and ATP-competitive ligands on the overall effectiveness of bivalent kinase inhibitors [O] . Margaret L. Wong, Jason Murphy, Edmund Harrington, 2016

机译：检查特异性配体和ATP竞争性配体对二价激酶抑制剂总体有效性的影响
7. Towards the Selective Inhibition of Glycolytic Pathway Enzymes: A Computational Analysis of Plasmodium falciparum and Human Triosephosphate Isomerase Ligand Interactions. [O] . Alexandru Nicoleta, Forlemu Neville Y 2016

机译：糖酵解途径酶的选择性抑制：恶性疟原虫和人三磷酸磷酸异构酶配体相互作用的计算分析。

Transforming bivalent ligands into retractable enzyme inhibitors through polypeptide-protein interactions.

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