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ACS Med Chem Lett. 2016 Dec 2;8(2):206-210. doi: 10.1021/acsmedchemlett.6b00417. eCollection 2017 Feb 9.
2
Characterization of chemical features of potent myeloperoxidase inhibitors.强效髓过氧化物酶抑制剂的化学特征表征
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The soluble curcumin derivative NDS27 inhibits superoxide anion production by neutrophils and acts as substrate and reversible inhibitor of myeloperoxidase.可溶性姜黄素衍生物 NDS27 可抑制中性粒细胞超氧阴离子的产生，并作为髓过氧化物酶的底物和可逆抑制剂。
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本文引用的文献

1
MPO Inhibitors Selected by Virtual Screening.基于虚拟筛选的髓过氧化物酶抑制剂
Mol Inform. 2011 Jun;30(6-7):605-13. doi: 10.1002/minf.201100016. Epub 2011 Jun 28.
2
Characterization of chemical features of potent myeloperoxidase inhibitors.强效髓过氧化物酶抑制剂的化学特征表征
Future Med Chem. 2016 Jul;8(11):1163-77. doi: 10.4155/fmc-2016-0031. Epub 2016 Jul 12.
3
Myeloperoxidase Inhibitors as Potential Drugs.髓过氧化物酶抑制剂作为潜在药物
Curr Drug Metab. 2015;16(3):168-90. doi: 10.2174/138920021603150812120640.
4
Inhibition of myeloperoxidase: evaluation of 2H-indazoles and 1H-indazolones.髓过氧化物酶的抑制作用：2H-吲唑和1H-吲唑酮的评估
Bioorg Med Chem. 2014 Nov 15;22(22):6422-9. doi: 10.1016/j.bmc.2014.09.044. Epub 2014 Oct 2.
5
Hybrid molecules inhibiting myeloperoxidase activity and serotonin reuptake: a possible new approach of major depressive disorders with inflammatory syndrome.抑制髓过氧化物酶活性和5-羟色胺再摄取的杂合分子：伴有炎症综合征的重度抑郁症的一种可能新疗法。
J Pharm Pharmacol. 2014 Aug;66(8):1122-32. doi: 10.1111/jphp.12236. Epub 2014 Mar 27.
6
Neutrophil interactions with the vascular endothelium.中性粒细胞与血管内皮的相互作用。
Int Immunopharmacol. 2013 Dec;17(4):1167-75. doi: 10.1016/j.intimp.2013.05.034. Epub 2013 Jul 14.
7
Dynamic combinatorial libraries: from exploring molecular recognition to systems chemistry.动态组合化学库：从分子识别探索到系统化学。
J Am Chem Soc. 2013 Jun 26;135(25):9222-39. doi: 10.1021/ja402586c. Epub 2013 Jun 11.
8
Evaluation of new scaffolds of myeloperoxidase inhibitors by rational design combined with high-throughput virtual screening.通过合理设计与高通量虚拟筛选评价新型髓过氧化物酶抑制剂的支架。
J Med Chem. 2012 Aug 23;55(16):7208-18. doi: 10.1021/jm3007245. Epub 2012 Aug 7.
9
Serotonin as a physiological substrate for myeloperoxidase and its superoxide-dependent oxidation to cytotoxic tryptamine-4,5-dione.血清素作为髓过氧化物酶及其超氧依赖氧化生成细胞毒性色胺-4,5-二酮的生理底物。
Biochem J. 2009 Dec 14;425(1):285-93. doi: 10.1042/BJ20090776.
10
Myeloperoxidase: a target for new drug development?髓过氧化物酶：新药研发的靶点？
Br J Pharmacol. 2007 Nov;152(6):838-54. doi: 10.1038/sj.bjp.0707358. Epub 2007 Jun 25.

从动态组合化学到可逆和不可逆髓过氧化物酶抑制剂的评估

From Dynamic Combinatorial Chemistry to Evaluation of Reversible and Irreversible Myeloperoxidase Inhibitors.

作者信息

Soubhye Jalal, Gelbcke Michel, Van Antwerpen Pierre, Dufrasne François, Boufadi Mokhtaria Yasmina, Nève Jean, Furtmüller Paul G, Obinger Christian, Zouaoui Boudjeltia Karim, Meyer Franck

机构信息

Chimie Pharmaceutique Organique, Faculty of pharmacy, Université Libre de Bruxelles (ULB) , Boulevard du Triomphe, 1050 Bruxelles, Belgium.

Chimie Pharmaceutique Organique, Faculty of pharmacy, Université Libre de Bruxelles (ULB), Boulevard du Triomphe, 1050 Bruxelles, Belgium; Laboratory of Beneficial Microorganisms, Functional Food and Health (LMBAFS), Faculty of Natural Sciences and Life, Université de Abdelhamid Ibn Badis, 27000 Mostaganem, Algeria.

出版信息

ACS Med Chem Lett. 2016 Dec 2;8(2):206-210. doi: 10.1021/acsmedchemlett.6b00417. eCollection 2017 Feb 9.

DOI:10.1021/acsmedchemlett.6b00417
PMID:28197313
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5304337/
Abstract

The implementation of dynamic combinatorial libraries allowed the determination of highly active reversible and irreversible inhibitors of myeloperoxidase (MPO) at the nanomolar level. Docking experiments highlighted the interaction between the most active ligands and MPO, and further kinetic studies defined the mode of inhibition of these compounds. Finally, evaluation showed that one dose of irreversible inhibitors is able to suppress the activity of MPO after inducing inflammation.

摘要

动态组合库的应用使得能够在纳摩尔水平上确定髓过氧化物酶（MPO）的高活性可逆和不可逆抑制剂。对接实验突出了最具活性的配体与MPO之间的相互作用，进一步的动力学研究确定了这些化合物的抑制模式。最后，评估表明一剂不可逆抑制剂能够在诱发炎症后抑制MPO的活性。