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Click-based synthesis and proteomic profiling of lipstatin analogues
Mun H Ngai1, Peng-Yu Yang, Kai Liu
1Department of Chemistry, and Medicinal Chemistry Program of the Life Sciences Institute, National University of Singapore, 3 Science Drive 3, Singapore 117543.
Abstract:
Using click chemistry to enable both structural diversity and proteome profiling within a natural product derived library, two out of nineteen lipstatin analogues showed similar activity to Orlistat against fatty acid synthase (FAS), but with an improved ability to induce tumour cell death.
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