Structural basis for inhibition of the fat mass and obesity associated protein (FTO)

…, EAL Bagg, KK Yeoh, C Lejeune, Z Zhang…

Index: Aik, Weishen; Demetriades, Marina; Hamdan, Muhammad K. K.; Bagg, Eleanor. A. L.; Yeoh, Kar Kheng; Lejeune, Clarisse; Zhang, Zhihong; McDonough, Michael A.; Schofield, Christopher J. Journal of Medicinal Chemistry, 2013 , vol. 56, # 9 p. 3680 - 3688

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Citation Number: 51

Abstract

The fat mass and obesity associated protein (FTO) is a potential target for anti-obesity medicines. FTO is a 2-oxoglutarate (2OG)-dependent N-methyl nucleic acid demethylase that acts on substrates including 3-methylthymidine, 3-methyluracil, and 6-methyladenine. To identify FTO inhibitors, we screened a set of 2OG analogues and related compounds using differential scanning fluorometry-and liquid chromatography-based assays. The ...