Biomimetic synthesis of gramicidin s and analogues by enzymatic cyclization of linear precursors on solid support |
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| Authors: | Wu Xiaoming Bu Xianzhang Wong Ka Man Yan Weili Guo Zhihong |
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| Institution: | Department of Chemistry and Biotechnology Research Institute, The Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong SAR, China. |
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| Abstract: | reaction: see text] Gramicidin S is a potent decapeptide antibiotic with high hemolytic activity but is unlikely to provoke microbial resistance. Here we demonstrate that gramicidin thioesterase (GrsB TE) correctly cyclizes immobilized linear decapeptide precursors into head-to-tail products, indicating its suitability for parallel solid-phase synthesis of gramicidin analogues from linear precursors on solid support. This chemoenzymatic method will enable the optimization of the therapeutic index of the natural product to fight microbial resistance. |
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