Development of Macrocyclic Peptidomimetics Containing Constrained alpha,alpha-Dialkylated Amino Acids with Potent and Selective Activity at Human Melanocortin Receptors

Merlino Francesco; Zhou Yang; Cai Minying; Carotenuto Alfonso; Yousif Ali M.; Brancaccio Diego; Di Maro Salvatore; Zappavigna Silvia; Limatola Antonio; Novellino Ettore; Grieco Paolo; Hruby Victor J.

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Development of Macrocyclic Peptidomimetics Containing Constrained alpha,alpha-Dialkylated Amino Acids with Potent and Selective Activity at Human Melanocortin Receptors

机译：含有受约束α，α-二烷基化氨基酸的大环肽肽，具有有效和选择性活性的α-二烷基化氨基酸受体

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We report the development of macrocyclic melanocortin derivatives of MT-II and SHU-9119, achieved by modifying the cycle dimension and incorporating constrained amino acids in ring-closing. This study culminated in the discovery of novel agonists/antagonists with an unprecedented activity profile by adding pieces to the puzzle of the melanocortin receptor selectivity. Finally, the resulting 19- and 20-membered rings represent a suitable frame for the design of further therapeutic ligands as selective modulators of the melanocortin system.

机译：我们报道了通过改变循环尺寸和在闭环中掺入约束氨基酸来实现MT-II和SHU-9119的Macr环状黑色主酶衍生物的发展。本研究通过向Melanocortin受体选择性的难题添加碎片来发现新的激动剂/拮抗剂的发现，通过向难题添加到前所未有的活性谱。最后，由此产生的19-和20元环代表了一种适当的框架，用于设计其他治疗配体作为Melanocortin系统的选择性调节剂。

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《Journal of Medicinal Chemistry》 |2018年第9期|共7页
作者
Merlino Francesco; Zhou Yang; Cai Minying; Carotenuto Alfonso; Yousif Ali M.; Brancaccio Diego; Di Maro Salvatore; Zappavigna Silvia; Limatola Antonio; Novellino Ettore; Grieco Paolo; Hruby Victor J.;
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Univ Naples Federico II Dept Pharm Via D Montesano 49 I-80131 Naples Italy;

Univ Arizona Dept Chem &

Biochem 1306 E Univ Blvd Tucson AZ 85721 USA;

Univ Arizona Dept Chem &

Biochem 1306 E Univ Blvd Tucson AZ 85721 USA;

Univ Naples Federico II Dept Pharm Via D Montesano 49 I-80131 Naples Italy;

Univ Naples Federico II Dept Pharm Via D Montesano 49 I-80131 Naples Italy;

Univ Naples Federico II Dept Pharm Via D Montesano 49 I-80131 Naples Italy;

Univ Campania Luigi Vanvitelli DiSTABiF Via Vivaldi 43 I-81100 Caserta Italy;

Univ Campania Luigi Vanvitelli Dept Precis Med Via Costantinopoli 16 I-80138 Naples Italy;

Stanford Univ Dept Biol Stanford CA 94305 USA;

Univ Naples Federico II Dept Pharm Via D Montesano 49 I-80131 Naples Italy;

Univ Naples Federico II Dept Pharm Via D Montesano 49 I-80131 Naples Italy;

Univ Arizona Dept Chem &

Biochem 1306 E Univ Blvd Tucson AZ 85721 USA;

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正文语种 eng
中图分类药学;
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1. Development of Macrocyclic Peptidomimetics Containing Constrained alpha,alpha-Dialkylated Amino Acids with Potent and Selective Activity at Human Melanocortin Receptors [J] . Merlino Francesco, Zhou Yang, Cai Minying, Journal of Medicinal Chemistry . 2018,第9期

机译：含有受约束α，α-二烷基化氨基酸的大环肽肽，具有有效和选择性活性的α-二烷基化氨基酸受体
2. A convenient synthesis of tetrazole, precursors of alpha-dialkylated alpha-amino acids, by reaction of trimethylsilyl azide with alpha-dialkylated beta-ketoesters [J] . Henri-Jean Cristau, Xavier Marat, Jean-Luc Pirat, Tetrahedron letters: The International Journal for the Rapid Publication of Preliminary Communications in Organic Chemistry . 2003,第15期

机译：通过叠氮化三甲基甲硅烷基与α-二烷基化的β-酮酸酯的反应，方便地合成四唑，α-二烷基化的α-氨基酸的前体
3. Potent and selective agonists of alpha-melanotropin (alphaMSH) action at human melanocortin receptor 5; linear analogs of alpha-melanotropin. [J] . Bednarek MA, MacNeil T, Tang R, Peptides: An International Journal . 2007,第5期

机译：对人黑皮质素受体5的α-促黑素（αMSH）作用的强效和选择性激动剂; α-促黑素的线性类似物。
4. Octapeptide Analogs of Somatostatin Containing alpha,alpha-Dialkylated Amino Acids with Potent Anticancer Activity [C] . Sudhanand Prasad, Archna Mathur, Neena Gupta American Peptide Symposium . 2006

机译：含有α-二烷基化氨基酸的生长抑制素的八肽类似物，具有效率的抗癌活性
5. Asymmetric synthesis of conformationally and topographically constrained amino acids as peptidomimetics: An approach to design and synthesis of opioid receptor selective ligands. [D] . Xiong, Chiyi. 2003

机译：构象和地形约束氨基酸作为拟肽的不对称合成：一种设计和合成阿片受体选择性配体的方法。
6. Development of Macrocyclic Peptidomimetics Containing Constrained αα-Dialkylated Amino Acids with Potent and Selective Activity at Human Melanocortin Receptors [O] . Francesco Merlino, Yang Zhou, Minying Cai, -1

机译：具有约束力的对人黑皮质素受体具有选择性活性的αα-二烷基化氨基酸的大环拟肽的研究
7. Development of Macrocyclic Peptidomimetics Containing Constrained α,α-Dialkylated Amino Acids with Potent and Selective Activity at Human Melanocortin Receptors [O] . Francesco Merlino, Yang Zhou, Minying Cai, 2018

机译：含有受约束α，α-二烷基化氨基酸的大环肽肽的研制在人黑色主酶受体中具有有效和选择性活性的α-二烷基化氨基酸

Development of Macrocyclic Peptidomimetics Containing Constrained alpha,alpha-Dialkylated Amino Acids with Potent and Selective Activity at Human Melanocortin Receptors

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