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Antibiotic–cell-penetrating peptide conjugates targeting challenging drug-resistant and intracellular pathogenic bacteria
Chemical Biology & Drug Design ( IF 3 ) Pub Date : 2021-07-27 , DOI: 10.1111/cbdd.13930
Samantha M Zeiders 1 , Jean Chmielewski 1
Affiliation  

The failure to treat everyday bacterial infections is a current threat as pathogens are finding new ways to thwart antibiotics through mechanisms of resistance and intracellular refuge, thus rendering current antibiotic strategies ineffective. Cell-penetrating peptides (CPPs) are providing a means to improve antibiotics that are already approved for use. Through coadministration and conjugation of antibiotics with CPPs, improved accumulation and selectivity with alternative and/or additional modes of action against infections have been observed. Herein, we review the recent progress of this antibiotic–cell-penetrating peptide strategy in combatting sensitive and drug-resistant pathogens. We take a closer look into the specific antibiotics that have been enhanced, and in some cases repurposed as broad-spectrum drugs. Through the addition and conjugation of cell-penetrating peptides to antibiotics, increased permeation across mammalian and/or bacterial membranes and a broader range in bacterial selectivity have been achieved.

中文翻译:

靶向具有挑战性的耐药菌和细胞内病原菌的抗生素-细胞穿透肽偶联物

无法治疗日常细菌感染是当前的威胁,因为病原体正在寻找通过耐药性和细胞内避难所机制阻止抗生素的新方法,从而使当前的抗生素策略无效。细胞穿透肽 (CPP) 正在提供一种改进已获批准使用的抗生素的方法。通过抗生素与 CPP 的共同给药和结合,已经观察到通过替代和/或额外的抗感染作用模式提高了积累和选择性。在此,我们回顾了这种抗生素-细胞穿透肽策略在对抗敏感和耐药病原体方面的最新进展。我们仔细研究了已增强的特定抗生素,在某些情况下被重新用作广谱药物。
更新日期:2021-07-27
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