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Azepinone-Containing Tetrapeptide Analogues of MelanotropinLead to Selective hMC4R Agonists and hMC5R Antagonist

机译：褪黑激素的含庚酮的四肽类似物导致选择性的hMC4R激动剂和hMC5R拮抗剂

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摘要

To address the need for highly potent, metabolically stable, and selective agonists, antagonists, and inverse agonists at the melanocortin receptor subtypes, conformationally constrained indolo- and benzazepinone residues were inserted into the α-MSH pharmacophore, His⁶-Phe⁷-Arg⁸-Trp⁹-domain. Replacement of His⁶ by an aminoindoloazepinone (Aia) or aminobenzazepinone (Aba) moiety led to hMC4R and hMC5R selective agonist and antagonist ligands, respectively (tetrapeptides >1 to >3 and >4, respectively). In peptides >1 to >3 and depending on the para-substituent of the d-Phe residue in position 2, the activity goes from allosteric partial agonism (>1, R = H) to allosteric full agonism (>2, R = F) and finally allosteric partial agonism (>3, R = Br).

机译：为了解决对黑皮质素受体亚型的高效，代谢稳定和选择性激动剂，拮抗剂和反向激动剂的需求，将构象受限的吲哚和苯并ze庚酮残基插入α-MSH药效团His ^{6 -Phe ^{7 -Arg ^{8 -Trp ^{9 域。用氨基吲哚并ze庚酮（Aia）或氨基苯并ze庚酮（Aba）部分取代His ^{6 分别导致hMC4R和hMC5R选择性激动剂和拮抗剂配体（四肽> 1 至> 3 和> 4 ）。在肽段> 1 至> 3 中，取决于位置2的d-Phe残基的对位取代，其活性来自变构部分激动作用（> 1 ，R = H）变构完全激动（> 2 ，R = F），最后是变构部分激动（> 3 ，R = Br）。}}}}}

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期刊名称 ACS Medicinal Chemistry Letters
作者
Olivier Van der Poorten; ∥; Krisztina Fehér; ∥; Koen Buysse; Debby Feytens; Ioanna Zoi; StevenD. Schwartz; José C. Martins; Dirk Tourwé; Minying Cai; Victor J. Hruby; Steven Ballet; *;
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作者单位

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年(卷),期 2015(6),2
年度 2015
页码 192–197
总页数 6
原文格式 PDF
正文语种
中图分类药物化学;
关键词
Melanocortin ligands constrained aminoazepinones hMC4R and hMC5R molecular modeling and ligand docking fluorine peptidomimetics allosteric hMC4R ligands;

机译：黑皮质素配体;受约束的氨基氮杂环丁酮;hMC4R和hMC5R分子建模和配体对接;氟肽模拟物;变构hMC4R配体;

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专利

1. Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist [J] . Van der Poorten Olivier, Feher Krisztina, Buysse Koen, ACS medicinal chemistry letters . 2015,第2期

机译：褪黑素的含ze庚酮的四肽类似物导致选择性的hMC4R激动剂和hMC5R拮抗剂
2. Structure-Activity Relationships of γ-MSH Analogues at the Human Melanocortin MC3, MC4, and MC5 Receptors. Discovery of Highly Selective hMC3R, hMC4R, and hMC5R Analogues [J] . Preeti Balse-Srinivasan, Paolo Grieco, Minying Cai, Journal of Medicinal Chemistry . 2003,第23期

机译：γ-MSH类似物在人类黑皮质素MC3，MC4和MC5受体上的结构活性关系。发现高度选择性的hMC3R，hMC4R和hMC5R类似物
3. Structure-activity relationships of gamma-MSH analogues at the human melanocortin MC3, MC4, and MC5 receptors. discovery of highly selective hMC3R, hMC4R, and hMC5R analogues. [J] . Balse Srinivasan P, Grieco P, Cai M, Journal of Medicinal Chemistry . 2003,第23期

机译：γ-MSH类似物在人类黑皮质素MC3，MC4和MC5受体上的构效关系。发现高度选择性的hMC3R，hMC4R和hMC5R类似物。
4. Potent and selective peptide agonist/antagonist analogues at human melanocortin receptor-4 [C] . Minying Cai, Paolo Grieco, Dev Trivedi, European Peptide Symposium . 2002

机译：有效和选择性肽激动剂/拮抗剂类似物在人黑色主义素受体-4
5. Tetrapeptide Melanocortin Agonist Ligands Exploring Selectivity of the mMC3R Using DPhe Substitutions in the Ac-His-Arg-DPhe-Tic-NH2 Scaffold [D] . Schlasner, Katherine N. 2018

机译：四肽Melanocortin激动剂配体在AC-HIS-ARG-DPHE-NH2支架中使用DPHE取代探索MMC3R的选择性
6. Development of Cyclic γ-MSH Analogues with Selective hMC3R Agonist and hMC3R/hMC5R Antagonist Activities [O] . Alexander V. Mayorov, Minying Cai, Kevin B. Chandler, -1

机译：具有选择性hMC3R激动剂和hMC3R / hMC5R拮抗活性的环状γ-MSH类似物的开发
7. Azepinone-containing tetrapeptide analogues of melanotropin lead to selective hMC4R agonists and hMC5R antagonist [O] . Van der Poorten, Olivier, Fehér, Krisztina, Buysse, Koen, 2015

机译：含有azepinone的melanotropin四肽类似物导致选择性hmC4R激动剂和hmC5R拮抗剂

Azepinone-Containing Tetrapeptide Analogues of MelanotropinLead to Selective hMC4R Agonists and hMC5R Antagonist

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