Design and synthesis of macrocyclic peptomers as mimics of a quorum sensing signal from Staphylococcus aureus
Design and synthesis of macrocyclic peptomers as mimics of a quorum sensing signal from Staphylococcus aureus
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DOI：
10.1021/ol800908h
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发表时间：
2008-06-19
期刊：
影响因子：
5.2
通讯作者：
Blackwell, Helen E.
中科院分区：
文献类型：
--
作者：
Fowler, Sarah A.;Stacy, Danielle M.;Blackwell, Helen E.
我们报道了设计和合成的大环肽-类肽杂合体（peptomers）作为金黄色葡萄球菌的自诱导肽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，我们通过生成一个集中的肽体库来证明它与平行合成的兼容性。其中一个肽体能够刺激金黄色葡萄球菌的生物膜形成，这是一种与AIP-I受体（agc - i）抑制有关的表型。
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.