Micro Arrayed Compound Screening (μARCS) for Inhibitors of Methionine Aminopeptidase Type 2

Author(s): Yihong Fan, Jieyi Wang, Pingping Lou, Jack Henkin, James L. Kofron, David J. Burns, Usha Warrior, Steven N Anderson

Journal Name: Letters in Drug Design & Discovery

Volume 2 , Issue 6 , 2005

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Methionine aminopeptidase type 2 catalyzes the removal of the amino-terminal methionine from newly translated polypeptides and has been shown to be a promising target for anti-angiogenesis and anticancer drugs. We describe a novel μARCS HTS method to identify inhibitors of this target utilizing porous matrices to introduce reagents throughout the assay. A library of 250,000 compounds was screened and compounds with IC50 values of less than 10μM were identified. These compounds may serve as initial lead molecules for further medicinal chemistry optimization.

Keywords: arcs, cancer, metap2, membranes, methionine, aminopeptidase

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Article Details

Year: 2005
Page: [462 - 469]
Pages: 8
DOI: 10.2174/1570180054771518
Price: $65

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