Issue 44, 2010
From the journal:

Chemical Communications

Click-based synthesis and proteomic profiling of lipstatin analogues†

Mun H. Ngai,a   Peng-Yu Yang,a   Kai Liu,b   Yuan Shen,b   Markus R. Wenk,bc   Shao Q. Yao*ab  and  Martin J. Lear*a  

* Corresponding authors

a Department of Chemistry, and Medicinal Chemistry Program of the Life Sciences Institute, National University of Singapore, 3 Science Drive 3, Singapore 117543
E-mail: Martin.Lear@nus.edu.sg
Tel: (+65) 65163998

b Department of Biological Sciences, National University of Singapore, 14 Science Drive 4, Singapore 117543
E-mail: chmyaosq@nus.edu.sg
Fax: (+65) 67791691
Tel: (+65) 65162925

c Department of Biochemistry, Yong Loo Lin School of Medicine, National University of Singapore, Singapore 117597

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.

Graphical abstract: Click-based synthesis and proteomic profiling of lipstatin analogues

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Article information

DOI
https://doi.org/10.1039/C0CC01276A
Article type
Communication
Submitted
07 May 2010
Accepted
10 Jun 2010
First published
24 Jun 2010

Chem. Commun., 2010,46, 8335-8337

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Click-based synthesis and proteomic profiling of lipstatin analogues

M. H. Ngai, P. Yang, K. Liu, Y. Shen, M. R. Wenk, S. Q. Yao and M. J. Lear, Chem. Commun., 2010, 46, 8335 DOI: 10.1039/C0CC01276A

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