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.
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。
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本文引用的文献
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