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Overcoming AlbD Protease Resistance and Improving Potency: Synthesis and Bioactivity of Antibacterial Albicidin Analogues with Amide Bond Isosteres
Organic Letters ( IF 5.2 ) Pub Date : 2021-08-16 , DOI: 10.1021/acs.orglett.1c02312
Leonardo Kleebauer 1 , Lieby Zborovsky 1 , Kay Hommernick 1 , Maria Seidel 1 , John B Weston 1 , Roderich D Süssmuth 1
Affiliation  

Albicidin is a potent antibacterial oligoaromatic peptide that is susceptible to the protease AlbD, a resistance factor. This potentially restricts the use of albicidin as a drug. To overcome this obstacle, we synthesized and evaluated six analogues with isosteric replacement of the key amide link. Protease stability was established while maintaining the antibacterial activity, including three analogues with up to eight times higher activity compared with the natural albicidin.

中文翻译:

克服 AlbD 蛋白酶抗性并提高效力:具有酰胺键等排体的抗菌 Albicidin 类似物的合成和生物活性

Albicidin 是一种有效的抗菌寡芳香肽,对蛋白酶 AlbD(一种抗性因子)敏感。这可能会限制使用albicidin作为药物。为了克服这一障碍,我们合成并评估了六种具有等排取代关键酰胺键的类似物。在保持抗菌活性的同时建立了蛋白酶稳定性,其中包括三种类似物,其活性比天然albicidin 高出八倍。
更新日期:2021-09-17
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