作为金黄色葡萄球菌群体感应信号模拟物的大环肽模拟物的设计与合成。
Design and synthesis of macrocyclic peptomers as mimics of a quorum sensing signal from Staphylococcus aureus.
作者信息
Fowler Sarah A, Stacy Danielle M, Blackwell Helen E
机构信息
Department of Chemistry, University of Wisconsin-Madison, Madison, WI 53706-1322, USA.
出版信息
Org Lett. 2008 Jun 19;10(12):2329-32. doi: 10.1021/ol800908h. Epub 2008 May 14.
We report the design and synthesis of macrocyclic peptide-peptoid hybrids (peptomers) as analogs of autoinducing peptide I (AIP-I) from Staphylococcus aureus. Our solid-phase synthetic route includes efficient microwave-assisted reactions and a tandem macrocyclization-cleavage step, and we demonstrate its compatibility with parallel synthesis through the generation of a focused peptomer library. One of the peptomers was capable of stimulating biofilm formation in S. aureus, a phenotype linked to AIP-I receptor (AgrC-I) inhibition.
我们报道了大环肽 - 类肽杂合物（肽聚物）的设计与合成，其作为金黄色葡萄球菌自诱导肽I（AIP - I）的类似物。我们的固相合成路线包括高效的微波辅助反应和串联大环化 - 裂解步骤，并且我们通过生成一个聚焦的肽聚物文库证明了其与平行合成的兼容性。其中一种肽聚物能够刺激金黄色葡萄球菌中的生物膜形成，这是一种与AIP - I受体（AgrC - I）抑制相关的表型。
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