Click-based synthesis and proteomic profiling of lipstatin analogues.
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.
Ngai
Mun H
MH
Department of Chemistry, and Medicinal Chemistry Program of the Life Sciences Institute, National University of Singapore, 3 Science Drive 3, Singapore 117543.
Yang
Peng-Yu
PY
Liu
Kai
K
Shen
Yuan
Y
Wenk
Markus R
MR
Yao
Shao Q
SQ
Lear
Martin J
MJ
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
D000970:Antineoplastic Agents; D007783:Lactones; D020543:Proteome; D000077403:Orlistat; C054164:lipstatin; D064429:Fatty Acid Synthases