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Substrate Peptidomimetic Inhibitors of P. falciparum Plasmepsin X with Potent Antimalarial Activity
ChemMedChem ( IF 3.4 ) Pub Date : 2022-07-29 , DOI: 10.1002/cmdc.202200306
Lachlan W Richardson 1, 2 , Trent D Ashton 1, 2 , Madeline G Dans 1, 2 , Nghi Nguyen 1, 2 , Paola Favuzza 1, 2 , Tony Triglia 1 , Anthony N Hodder 1, 2 , Anna Ngo 1 , Kate E Jarman 1, 2 , Alan F Cowman 1, 2 , Brad E Sleebs 1, 2
Affiliation  

Substrate mimicry: Substrate peptidomimetics were designed and showed potent inhibition of plasmepsin X (PMX). The peptidomimetics block PMX ligand processing, arrest asexual parasites at the schizont stage and potently kill P. falciparum parasites. The peptidomimetics will further assist in the understanding of PMX selectivity and in the development of PMX targeted antimalarials.

中文翻译:

具有强效抗疟活性的恶性疟原虫 Plasmepsin X 的底物拟肽抑制剂

底物拟态:设计了底物拟肽并显示出对血浆蛋白酶 X (PMX) 的有效抑制作用。肽模拟物阻断 PMX 配体加工,在裂殖体阶段阻止无性寄生虫并有效杀死恶性疟原虫寄生虫。肽模拟物将进一步帮助理解 PMX 选择性和开发 PMX 靶向抗疟药。
更新日期:2022-07-29
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