In 2013,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. published 《Structural Basis for Inhibition of the Fat Mass and Obesity Associated Protein (FTO)》.Journal of Medicinal Chemistry published the findings.Reference of Methyl 5-bromopicolinate The information in the text is summarized as follows:
The fat mass and obesity associated protein (FTO) is a potential target for anti-obesity medicines. FTO is a 2-oxoglutarate (2OG)-dependent N-Me 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 analogs and related compounds using differential scanning fluorometry- and liquid chromatog.-based assays. The results revealed sets of both cyclic and acyclic 2OG analogs that are FTO inhibitors. Identified inhibitors include small mols. that have been used in clin. studies for the inhibition of other 2OG oxygenases. Crystallog. analyses reveal inhibition by 2OG cosubstrate or primary substrate competitors as well as compounds that bind across both cosubstrate and primary substrate binding sites. The results will aid the development of more potent and selective FTO inhibitors.Methyl 5-bromopicolinate(cas: 29682-15-3Reference of Methyl 5-bromopicolinate) was used in this study.
Methyl 5-bromopicolinate(cas: 29682-15-3) belongs to pyridine. Pyridine is very deactivated towards electrophilic substitution with respect to benzene. For this reason classical formylation, using methods such as the Gattermann or Vilsmeier reactions, are not generally successful. Reference of Methyl 5-bromopicolinate