Development of sulfonamide compounds as potent methionine aminopeptidase type II inhibitors with antiproliferative properties

Bioorganic & Medicinal Chemistry Letters
Megumi KawaiGeorge S Sheppard

Abstract

We have screened molecules for inhibition of MetAP2 as a novel approach toward antiangiogenesis and anticancer therapy using affinity selection/mass spectrometry (ASMS) employing MetAP2 loaded with Mn(2+) as the active site metal. After a series of anthranilic acid sulfonamides with micromolar affinities was identified, chemistry efforts were initiated. The micromolar hits were quickly improved to potent nanomolar inhibitors by chemical modifications guided by insights from X-ray crystallography.

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Citations

Feb 7, 2008·Proceedings of the National Academy of Sciences of the United States of America·Jieyi WangRandy L Bell
Apr 21, 2007·American Journal of Respiratory Cell and Molecular Biology·Daniel KassSteven Greenberg
Jul 14, 2011·Analytical and Bioanalytical Chemistry·Sayaka ShibataErkang Fan
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Dec 3, 2016·Chemical & Pharmaceutical Bulletin·Mostafa Mohammed GhorabSheikh Fayaz Ahmed
Jul 12, 2018·Organic & Biomolecular Chemistry·Ramanathan Devenderan, Pitchumani Kasi
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Aug 28, 2021·Trends in Pharmacological Sciences·Andrea Goya GrocinEdward W Tate
Jan 11, 2012·Bioorganic & Medicinal Chemistry·Melissa M KempAngela N Koehler

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