Role of the conformational rigidity in the design of biomimetic antimicrobial compounds.

Role of the conformational rigidity in the design of biomimetic antimicrobial compounds.
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DOI:
10.1002/anie.201003104
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发表时间:
2010-11-02
影响因子:
16.6
通讯作者:
Gidalevitz, David
Gidalevitz, David
中科院分区:
化学1区
文献类型:
--
作者:
Ivankin, Andrey;Livne, Liran;Mor, Amram;Caputo, Gregory A.;DeGrado, William F.;Meron, Mati;Lin, Binhua;Gidalevitz, David

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抗菌肽(AMP)是一种天然存在的抗生素,几乎存在于所有生物体中。[1]在过去的二十年里,AMP因其作为抗感染药物的潜在治疗用途而引起了人们的极大兴趣。然而,阻碍AMP进入医药市场的一些严重挑战包括它们在体内的快速降解、高昂的生产成本以及在生理条件下活性降低。[2]为了克服这些问题,同时保持多肽的天然抗感染特性,抗菌肽的非天然模拟物的领域迅速扩大。
Antimicrobial peptides (AMPs) are naturally occurring antibiotics found in essentially all living organisms.[1] In the past two decades, AMPs have attracted considerable interest because of their potential therapeutic use as anti-infective agents.[1, 2] There exists, however, a number of serious challenges preventing AMP from reaching a pharmaceutical market including their rapid in vivo degradation, high production costs, and reduced activity in physiological conditions.[2] Efforts to overcome these problems while retaining the peptides natural antiinfective properties resulted in the emergence of a rapidly expanding field of nonnatural mimics of antimicrobial peptides.
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