When Macrocyclic Peptides Meet the Crystal Structure of a Melanocortin Receptor

Grieco Paolo

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When Macrocyclic Peptides Meet the Crystal Structure of a Melanocortin Receptor

机译：当宏环肽满足黑色主义受体的晶体结构时

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摘要

This work reveals some key factors for the design of a novel generation of selective melanocortin ligands at the MC4 receptor.

机译：这项工作揭示了在MC4受体上设计新一代选择性黑素皮质素配体的一些关键因素。

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来源
《Journal of Medicinal Chemistry》 |2021年第1期|共3页
作者
Grieco Paolo;
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作者单位

Univ Naples Federico II Ctr Interuniv Ric Peptidi Bioatt Dept Pharm CIRPEB I-80131 Naples Italy;

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正文语种 eng
中图分类药学;
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1. Crystal structure of PXY-TDIF complex reveals a conserved recognition mechanism among CLE peptide-receptor pairs [J] . Heqiao Zhang, Xiaoya Lin, Zhifu Han, 细胞研究（英文版） . 2016,第005期
2. Structures of active melanocortin-4 receptor-Gs-protein complexes with NDP-α-MSH and setmelanotide [J] . Nicolas A.Heyder, Dennis Kwiatkowski, J(o)rg Bürger, 细胞研究（英文版） . 2021,第011期
3. Structure-activity relationships of peptides incorporating a bioactive reverse-turn heterocycle at the melanocortin receptors: Identification of a 5800-fold mouse melanocortin-3 receptor (mMC3R) selective antagonist/partial agonist versus the mouse melanocortin-4 receptor (mMC4R) [J] . Singh A., Dirain M., Witek R., Journal of Medicinal Chemistry . 2013,第7期

机译：在黑皮质素受体上结合有生物活性反向杂环的肽的结构活性关系：鉴定5800倍小鼠黑皮质素-3受体（mMC3R）选择性拮抗剂/部分激动剂对小鼠黑皮质素4受体（mMC4R）
4. Structure-Activity Relationship Studies on a Macrocyclic Agouti-Related Protein (AGRP) Scaffold Reveal Agouti Signaling Protein (ASP) Residue Substitutions Maintain Melanocortin-4 Receptor Antagonist Potency and Result in Inverse Agonist Pharmacology at the Melanocortin-5 Receptor [J] . Ericson Mark D., Freeman Katie T., Schnell Sathya M., Journal of Medicinal Chemistry . 2017,第19期

机译：宏环agouti相关蛋白（AgrP）支架的结构 - 活性关系研究显示agouti信号蛋白（ASP）残留物拮抗剂拮抗剂效力维持Melanocortin-4受体拮抗剂效力并导致Melanocortin-5受体的反向激动剂药理学
5. Design and microwave-assisted synthesis of novel macrocyclic peptides active at melanocortin receptors: Discovery of potent and selective hMC5R receptor antagonists [J] . Grieco P, Cai MY, Liu L, Journal of Medicinal Chemistry . 2008,第9期

机译：设计和微波辅助合成对黑皮质素受体具有活性的新型大环肽：有效和选择性的hMC5R受体拮抗剂的发现
6. Novel Macrocyclic Peptides Active at Human Melanocortin Receptors: A Preliminary SAR Study [C] . A.M. Yousif, M. Cai, F. Merlino American Peptide Symposium . 2015

机译：新型大环肽活性在人黑色主义素受体中：初步SAR研究
7. Structure of the melanocortin-2 receptor accessory protein MRAP and its roles in the regulation of melanocortin receptors trafficking and signaling. [D] . Sebag, Julien A. 2009

机译：melanocortin-2受体辅助蛋白MRAP的结构及其在调节melanocortin受体运输和信号传导中的作用。
8. Structure-Activity Relationship Studies of a Macrocyclic AGRP-Mimetic Scaffold cPro-Arg-Phe-Phe-Asn-Ala-Phe-DPro Yield Potent and Selective Melanocortin-4 Receptor Antagonists and Melanocortin-5 Receptor Inverse Agonists that Increase Food Intake in Mice [O] . Katlyn A. Fleming, Mark D. Ericson, Katie T. Freeman, -1

机译：大环AGRP模拟支架c Pro-Arg-Phe-Phe-Asn-Ala-Phe-DPro的结构活性关系研究提高了选择性和增强食物摄入量的Melanocortin-4受体拮抗剂和Melanocortin-5受体反向激动剂的活性。在老鼠
9. Design and Microwave-Assisted Synthesis of Novel Macrocyclic Peptides Active at Melanocortin Receptors: Discovery of Potent and Selective hMC5R Receptor Antagonists [O] . GRIECO PAOLO, CAI MINYING, LIU LU, 2008

机译：设计和微波辅助合成在黑皮质素受体中活跃的新型大环肽：发现强效和选择性hmC5R受体拮抗剂
10. Crystal and Molecular Structures of a Tricyclic Phosphorus Ester, a Cobalt(III) Macrocyclic Complex and a Trans Coordinated Platinum(II) Compound [R] . Wintergrass, D. J. 1987

机译：三环磷酯，钴（III）大环配合物和反式配位铂（II）化合物的晶体和分子结构

When Macrocyclic Peptides Meet the Crystal Structure of a Melanocortin Receptor

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