2Y5K

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

Summary for 2Y5K

Entry DOI	10.2210/pdb2y5k/pdb
Related	1FTA 2FHY 2FIE 2FIX 2JJK 2VT5 2WBB 2WBD 2Y5L
Descriptor	FRUCTOSE-1,6-BISPHOSPHATASE 1, 1-[5-(2-METHOXYETHYL)-4-METHYL-THIOPHEN-2-YL]SULFONYL-3-[4-METHOXY-6-(METHYLCARBAMOYLAMINO)PYRIDIN-2-YL]UREA (3 entities in total)
Functional Keywords	hydrolase
Biological source	HOMO SAPIENS (HUMAN)
Total number of polymer chains	4
Total formula weight	149267.77
Authors	Ruf, A.,Hebeisen, P.,Haap, W.,Kuhn, B.,Mohr, P.,Wessel, H.P.,Zutter, U.,Kirchner, S.,Benz, J.,Joseph, C.,Alvarez-Sanchez, R.,Gubler, M.,Schott, B.,Benardeau, A.,Tozzo, E.,Kitas, E. (deposition date: 2011-01-14, release date: 2011-05-18, Last modification date: 2023-12-20)
Primary citation	Hebeisen, P.,Haap, W.,Kuhn, B.,Mohr, P.,Wessel, H.P.,Zutter, U.,Kirchner, S.,Ruf, A.,Benz, J.,Joseph, C.,Alvarez-Sanchez, R.,Gubler, M.,Schott, B.,Benardeau, A.,Tozzo, E.,Kitas, E. Orally Active Aminopyridines as Inhibitors of Tetrameric Fructose-1,6-Bisphosphatase. Bioorg.Med.Chem.Lett., 21:3237-, 2011 Cited by PubMed 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. PubMed: 21550236 DOI: 10.1016/J.BMCL.2011.04.044 PDB entries with the same primary citation
Experimental method	X-RAY DIFFRACTION (2.1 Å)

Structure validation