title: Click-based synthesis and proteomic profiling of lipstatin analogues.
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.
authors.affiliation: Department of Chemistry, and Medicinal Chemistry Program of the Life Sciences Institute, National University of Singapore, 3 Science Drive 3, Singapore 117543.
authors.forename: Mun H
authors.initials: MH
authors.lastname: Ngai
authors.forename: Peng-Yu
authors.initials: PY
authors.lastname: Yang
authors.forename: Kai
authors.initials: K
authors.lastname: Liu
authors.forename: Yuan
authors.initials: Y
authors.lastname: Shen
authors.forename: Markus R
authors.initials: MR
authors.lastname: Wenk
authors.forename: Shao Q
authors.initials: SQ
authors.lastname: Yao
authors.forename: Martin J
authors.initials: MJ
authors.lastname: Lear
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D045744:Cell Line, Tumor; D057930:Click Chemistry; D064429:Fatty Acid Synthases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006801:Humans; D007783:Lactones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D000077403:Orlistat; D020543:Proteome / Q000737:chemistry* / Q000378:metabolism
chemical_list: D000970:Antineoplastic Agents; D007783:Lactones; D020543:Proteome; D000077403:Orlistat; C054164:lipstatin; D064429:Fatty Acid Synthases