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Orally active aminopyridines as inhibitors of tetrameric fructose-1,6-bisphosphatase.

Hebeisen P, Haap W, Kuhn B, Mohr P, Wessel HP, Zutter U, Kirchner S, Ruf A, Benz J, Joseph C, Alvarez-Sánchez R, Gubler M, Schott B, Benardeau A, Tozzo E, Kitas E
Bioorg Med Chem Lett 21 3237-42 (2011)
Cited: 3 times
EuropePMC logo PMID: 21550236

Abstract

A novel sulfonylureido pyridine series exemplified by compound 19 yielded potent inhibitors of FBPase showing significant glucose reduction and modest glycogen lowering in the acute db/db mouse model for Type-2 diabetes. Our inhibitors occupy the allosteric binding site and also extend into the dyad interface region of tetrameric FBPase.

Reviews citing this publication (2)

  1. Transcription factors and coactivators controlling nutrient and hormonal regulation of hepatic gluconeogenesis. Jitrapakdee S. Int J Biochem Cell Biol 44 33-45 (2012)
  2. Emerging Computational Methods for the Rational Discovery of Allosteric Drugs. Wagner JR, Lee CT, Durrant JD, Malmstrom RD, Feher VA, Amaro RE. Chem Rev 116 6370-6390 (2016)

Articles citing this publication (1)

  1. Quadruple space-group ambiguity owing to rotational and translational noncrystallographic symmetry in human liver fructose-1,6-bisphosphatase. Ruf A, Tetaz T, Schott B, Joseph C, Rudolph MG. Acta Crystallogr D Struct Biol 72 1212-1224 (2016)


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