类肽血管内皮生长因子受体2拮抗剂的药效基团包括侧链和主链残基。
The pharmacophore of a peptoid VEGF receptor 2 antagonist includes both side chain and main chain residues.
作者信息
Udugamasooriya D Gomika, Dunham Geoff, Ritchie Caroline, Brekken Rolf A, Kodadek Thomas
机构信息
Department of Internal Medicine and Molecular Biology, Division of Translational Research, University of Texas Southwestern Medical Center, 5323 Harry Hines Boulevard, Dallas, TX 75390-9185, USA.
出版信息
Bioorg Med Chem Lett. 2008 Nov 15;18(22):5892-4. doi: 10.1016/j.bmcl.2008.07.023. Epub 2008 Jul 10.
Abstract
Here we identify the pharmacophore in a peptoid that antagonizes Vascular Endothelial Growth Factor Receptor-2 (VEGFR2) in vitro and in vivo. Only three of the side chains in the peptoid are required for activity. Surprisingly, however, main chain atoms also form critical interactions with the receptor.
摘要
在此，我们确定了一种拟肽中的药效基团，该拟肽在体外和体内均能拮抗血管内皮生长因子受体2（VEGFR2）。该拟肽中只有三个侧链具有活性。然而，令人惊讶的是，主链原子也与受体形成关键相互作用。
相似文献
1
The pharmacophore of a peptoid VEGF receptor 2 antagonist includes both side chain and main chain residues.类肽血管内皮生长因子受体2拮抗剂的药效基团包括侧链和主链残基。
Bioorg Med Chem Lett. 2008 Nov 15;18(22):5892-4. doi: 10.1016/j.bmcl.2008.07.023. Epub 2008 Jul 10.
2
A peptoid antagonist of VEGF receptor 2 recognizes a 'hotspot' in the extracellular domain distinct from the hormone-binding site.一种血管内皮生长因子受体2的类肽拮抗剂识别出细胞外结构域中一个不同于激素结合位点的“热点”。
Bioorg Med Chem. 2008 Jun 15;16(12):6338-43. doi: 10.1016/j.bmc.2008.05.015. Epub 2008 May 9.
3
A peptoid "antibody surrogate" that antagonizes VEGF receptor 2 activity.一种拮抗血管内皮生长因子受体2活性的类肽“抗体替代物”。
J Am Chem Soc. 2008 Apr 30;130(17):5744-52. doi: 10.1021/ja711193x. Epub 2008 Apr 2.
4
GU81, a VEGFR2 antagonist peptoid, enhances the anti-tumor activity of doxorubicin in the murine MMTV-PyMT transgenic model of breast cancer.GU81，一种血管内皮生长因子受体 2（VEGFR2）拮抗剂肽，增强了多柔比星在乳腺癌 MMTV-PyMT 转基因模型小鼠中的抗肿瘤活性。
BMC Cancer. 2010 Jul 30;10:397. doi: 10.1186/1471-2407-10-397.
5
Potent and selective photo-inactivation of proteins with peptoid-ruthenium conjugates.肽-钌缀合物对蛋白质的高效和选择性光灭活。
Nat Chem Biol. 2010 Apr;6(4):258-60. doi: 10.1038/nchembio.333. Epub 2010 Mar 14.
6
Construction of peptoids with all trans-amide backbones and peptoid reverse turns via the tactical incorporation of N-aryl side chains capable of hydrogen bonding.通过战术性引入能够形成氢键的 N-芳基侧链，构建具有全反式酰胺骨架和肽反转的肽。
J Org Chem. 2010 Sep 17;75(18):6068-78. doi: 10.1021/jo101075a.
7
Effect of side chain hydrophobicity and cationic charge on antimicrobial activity and cytotoxicity of helical peptoids.侧链疏水性和阳离子电荷对螺旋类肽抗菌活性及细胞毒性的影响
Bioorg Med Chem Lett. 2018 Jan 15;28(2):170-173. doi: 10.1016/j.bmcl.2017.11.034. Epub 2017 Nov 23.
8
New strategies for the design of folded peptoids revealed by a survey of noncovalent interactions in model systems.新型折叠肽设计策略的揭示：模型体系中非共价相互作用研究
J Am Chem Soc. 2009 Nov 18;131(45):16555-67. doi: 10.1021/ja907184g.
9
MRI detection of VEGFR2 in vivo using a low molecular weight peptoid-(Gd)8-dendron for targeting.利用靶向低分子量肽-(Gd)8-树枝状大分子的方法在体检测 VEGFR2
J Am Chem Soc. 2010 Sep 22;132(37):12829-31. doi: 10.1021/ja105563a.
10
Effects of including an N-terminal insertion region and arginine-mimetic side chains in helical peptoid analogues of lung surfactant protein B.在肺表面活性物质蛋白B的螺旋类肽类似物中包含N端插入区域和精氨酸模拟侧链的影响。
Biochemistry. 2006 Oct 3;45(39):11809-18. doi: 10.1021/bi060617e.
引用本文的文献
1
Rational design of stapled antimicrobial peptides.订书肽抗菌肽的合理设计。
Amino Acids. 2023 Apr;55(4):421-442. doi: 10.1007/s00726-023-03245-w. Epub 2023 Feb 12.
2
A peptoid interleukin-15 receptor antagonist suppresses inflammation and arthritis in mice.一种拟肽白细胞介素-15受体拮抗剂可抑制小鼠的炎症和关节炎。
Clin Transl Immunology. 2022 Nov 24;11(11):e1432. doi: 10.1002/cti2.1432. eCollection 2022.
3
Bent Into Shape: Folded Peptides to Mimic Protein Structure and Modulate Protein Function.塑形：折叠肽模拟蛋白质结构并调节蛋白质功能。
Pept Sci (Hoboken). 2020 Jan;112(1). doi: 10.1002/pep2.24145. Epub 2020 Jan 2.
4
Identification of the minimum pharmacophore of lipid-phosphatidylserine (PS) binding peptide-peptoid hybrid PPS1D1.脂质 - 磷脂酰丝氨酸（PS）结合肽 - 类肽杂合物PPS1D1最小药效团的鉴定。
Bioorg Med Chem. 2016 Sep 15;24(18):4470-4477. doi: 10.1016/j.bmc.2016.07.045. Epub 2016 Jul 21.
5
Tumor-targeting peptides from combinatorial libraries.来自组合文库的肿瘤靶向肽。
Adv Drug Deliv Rev. 2017 Feb;110-111:13-37. doi: 10.1016/j.addr.2016.05.009. Epub 2016 May 19.
6
Unbiased Selection of Peptide-Peptoid Hybrids Specific for Lung Cancer Compared to Normal Lung Epithelial Cells.与正常肺上皮细胞相比，对肺癌具有特异性的肽 - 类肽杂合物的无偏选择。
ACS Chem Biol. 2015 Dec 18;10(12):2891-9. doi: 10.1021/acschembio.5b00592. Epub 2015 Oct 28.
7
A readily applicable strategy to convert peptides to peptoid-based therapeutics.将肽转化为基于肽的治疗剂的一种易于应用的策略。
PLoS One. 2013;8(3):e58874. doi: 10.1371/journal.pone.0058874. Epub 2013 Mar 21.
8
Peptoid-based PET imaging of vascular endothelial growth factor receptor (VEGFR) expression.基于类肽的血管内皮生长因子受体（VEGFR）表达的正电子发射断层显像（PET）成像
Am J Nucl Med Mol Imaging. 2011;1(1):65-75. Epub 2011 Aug 1.
9
On-Bead Two-Color (OBTC) Cell Screen for Direct Identification of Highly Selective Cell Surface Receptor Ligands.用于直接鉴定高选择性细胞表面受体配体的磁珠上双色（OBTC）细胞筛选
Curr Protoc Chem Biol. 2012 Mar;4:35-48. doi: 10.1002/9780470559277.ch110199. Epub 2012 Mar 1.
10
Expanded polyglutamine-binding peptoid as a novel therapeutic agent for treatment of Huntington's disease.扩展型聚谷氨酰胺结合类肽作为治疗亨廷顿舞蹈病的新型治疗药物。
Chem Biol. 2011 Sep 23;18(9):1113-25. doi: 10.1016/j.chembiol.2011.06.010.
本文引用的文献
1
A peptoid "antibody surrogate" that antagonizes VEGF receptor 2 activity.一种拮抗血管内皮生长因子受体2活性的类肽“抗体替代物”。
J Am Chem Soc. 2008 Apr 30;130(17):5744-52. doi: 10.1021/ja711193x. Epub 2008 Apr 2.
2
Rapid identification of the pharmacophore in a peptoid inhibitor of the proteasome regulatory particle.蛋白酶体调节颗粒的拟肽抑制剂中药效基团的快速鉴定。
Chem Commun (Camb). 2008 Mar 7(9):1064-6. doi: 10.1039/b717861a. Epub 2008 Jan 24.
3
[Intravitreal anti-VEGF injections improve the visual prognosis of wet age related macular degeneration].玻璃体内注射抗血管内皮生长因子可改善湿性年龄相关性黄斑变性的视觉预后
Rev Med Suisse. 2007 Jan 17;3(94):137-41.
4
Antagonists to human and mouse vascular endothelial growth factor receptor 2 generated by directed protein evolution in vitro.通过体外定向蛋白质进化产生的人源和鼠源血管内皮生长因子受体2拮抗剂。
Chem Biol. 2006 May;13(5):549-56. doi: 10.1016/j.chembiol.2005.12.009.
5
Peptide-based molecules in angiogenesis.血管生成中基于肽的分子。
Chem Biol Drug Des. 2006 Feb;67(2):115-26. doi: 10.1111/j.1747-0285.2006.00356.x.
6
Role of the vascular endothelial growth factor pathway in tumor growth and angiogenesis.血管内皮生长因子通路在肿瘤生长和血管生成中的作用。
J Clin Oncol. 2005 Feb 10;23(5):1011-27. doi: 10.1200/JCO.2005.06.081. Epub 2004 Dec 7.
7
Vascular endothelial growth factor: basic science and clinical progress.血管内皮生长因子：基础科学与临床进展
Endocr Rev. 2004 Aug;25(4):581-611. doi: 10.1210/er.2003-0027.
8
Bevacizumab plus irinotecan, fluorouracil, and leucovorin for metastatic colorectal cancer.贝伐单抗联合伊立替康、氟尿嘧啶和亚叶酸钙治疗转移性结直肠癌。
N Engl J Med. 2004 Jun 3;350(23):2335-42. doi: 10.1056/NEJMoa032691.
9
Zotero 插件