New opioid affinity labels containing maleoyl moiety

Ildiko Szatmari; Gyorgy Orosz; Andras Z. Ronai; Eva Mako; Kalman Medzihradszky; Anna Borsodi

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New opioid affinity labels containing maleoyl moiety

机译：含有马来酰基部分的新型阿片样物质亲和标记

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Opioid receptor binding properties and pharmacological profiles of novel peptides containing maleoyl function were determined in order to develop new affinity labels. Based on the enkephalin structure peptide ligands were synthesized and tested. Both in in vitro receptor binding experiments and pharmacological studies, all ligands showed agonist character with relatively high affinity (K_i values in the nanomolar range) and good to moderate selectivity. Replacement of Gly~2 in the enkephalin frame with D-Ala led to higher affinities with a small decrease in selectivity. The loner peptide chains resulted in compounds with high percentage (up to 86%) of irreversible binding. The selectivity pattern of the ligands is in good agreement with the data obtained from the pharmacological assays (guinea pig ileum and mouse vas deferens bioassays). The newly synthesized peptides could be used in further studies in order to determined more detailed characteristics of the ligand-receptor interaction.

机译：确定阿片样物质受体结合特性和含有马来酰功能的新型肽的药理作用，以开发新的亲和标记。基于脑啡肽结构，合成并测试了肽配体。在体外受体结合实验和药理学研究中，所有配体均表现出激动剂特性，具有较高的亲和力（K_i值在纳摩尔范围内）和良好至中等的选择性。用D-Ala取代脑啡肽框架中的Gly〜2导致更高的亲和力，选择性略有下降。孤独的肽链导致化合物具有不可逆结合的高百分比（高达86％）。配体的选择性模式与从药理测定（豚鼠回肠和小鼠输精管生物测定）获得的数据高度吻合。新合成的肽可用于进一步的研究中，以便确定配体-受体相互作用的更详细的特征。

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《Life sciences》 |1999年第17期|共11页
作者
Ildiko Szatmari; Gyorgy Orosz; Andras Z. Ronai; Eva Mako; Kalman Medzihradszky; Anna Borsodi;
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正文语种 eng
中图分类生命的起源;生命科学总论;
关键词
opioid receptor; affinity labels; maleoyl peptide; ligand binding;

机译：阿片受体;亲和标记;马来酰肽;配体结合;

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1. New opioid affinity labels containing maleoyl moiety [J] . Ildiko Szatmari, Gyorgy Orosz, Andras Z. Ronai, Life sciences . 1999,第17期

机译：含有马来酰基部分的新型阿片样物质亲和标记
2. Dual Labeled Peptides as Tools to Study Receptors:Nanomolar Affinity Derivatives of TIPP(Tyr-Tic-Phe-Phe)Containing an Affinity Label and Biotin as Probes of delta Opioid Receptors [J] . Jane V.Aldrich, Vivek Kumar, Thomas F.Murray Bioconjugate Chemistry . 2009,第2期

机译：双标记肽作为研究受体的工具：TIPP（Tyr-Tic-Phe-Phe）的纳摩尔亲和衍生物，包含亲和标签和生物素作为阿片类鸦片受体的探针
3. Discovery of Dermorphin-Based Affinity Labels with Subnanomolar Affinity for Mu Opioid Receptors [J] . Bhaswati Sinha, Zhengyu Cao, Thomas F. Murray, Journal of Medicinal Chemistry . 2009,第23期

机译：Mu阿片受体的亚纳摩尔亲和力的基于Dermorphin的亲和标记的发现。
4. Twenty years among opioid peptides.Affinity labeling of the opioid receptors [C] . Kalman Medzihradszky European Peptide Symposium . 2002

机译：阿片类药物肽二十年。阿片类药物的贴标
5. SYNTHESIS OF "C-GLYCOSIDES" AND THEIR POTENTIAL APPLICATION TO AFFINITY LABELING OF O-GLYCOSIDASES (PHOTOAFFINITY LABELING, GLYCOSYL CYANIDES). [D] . MYERS, ROBERT WALTER. 1986

机译：“ C-糖苷”的合成及其在O-糖苷酶亲和性标签（光亲和性标签，糖基氰化物）上的潜在应用。
6. Dual Labeled Peptides as Tools to Study Receptors: Nanomolar Affinity Derivatives of TIPP (Tyr-Tic-Phe-Phe) Containing an Affinity Label and Biotin as Probes of δ Opioid Receptors [O] . Jane V. Aldrich, Vivek Kumar, Thomas F. Murray, -1

机译：双标记肽作为研究受体的工具：含有亲和标记的TIPP（Tyr-Tic-Phe-Phe）纳摩尔亲和衍生物和生物素作为δ阿片受体的探针
7. Fentanyl derivatives bearing aliphatic alkaneguanidinium moieties: A new series of hybrid molecules with significant binding affinity for μ-opioid receptors and I2-imidazoline binding sites [O] . Dardonville, Christophe, Jagerovic, Nadine, Callado, Luis F., 2013

机译：带有脂肪族链烷胍基部分的芬太尼衍生物：对μ阿片受体和I2-咪唑啉结合位点具有显着结合亲和力的一系列新杂化分子
8. Synthesis of Cryptophycin Affinity Labels and Tubulin Labeling [R] . Yang, K. , Georg, G. I. 2006

机译：Cryptophycin亲和标记和微管蛋白标记的合成

New opioid affinity labels containing maleoyl moiety

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