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== | ==Orally active aminopyridines as inhibitors of tetrameric fructose 1,6- bisphosphatase== | ||
[[http://www.uniprot.org/uniprot/F16P1_HUMAN F16P1_HUMAN | <StructureSection load='2y5k' size='340' side='right'caption='[[2y5k]], [[Resolution|resolution]] 2.10Å' scene=''> | ||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[2y5k]] is a 4 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2Y5K OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2Y5K FirstGlance]. <br> | |||
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.1Å</td></tr> | |||
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=YCU:1-[5-(2-METHOXYETHYL)-4-METHYL-THIOPHEN-2-YL]SULFONYL-3-[4-METHOXY-6-(METHYLCARBAMOYLAMINO)PYRIDIN-2-YL]UREA'>YCU</scene></td></tr> | |||
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=2y5k FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2y5k OCA], [https://pdbe.org/2y5k PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2y5k RCSB], [https://www.ebi.ac.uk/pdbsum/2y5k PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2y5k ProSAT]</span></td></tr> | |||
</table> | |||
== Disease == | |||
[https://www.uniprot.org/uniprot/F16P1_HUMAN F16P1_HUMAN] Defects in FBP1 are the cause of fructose-1,6-bisphosphatase deficiency (FBPD) [MIM:[https://omim.org/entry/229700 229700]. FBPD is inherited as an autosomal recessive disorder mainly in the liver and causes life-threatening episodes of hypoglycemia and metabolic acidosis (lactacidemia) in newborn infants or young children.<ref>PMID:9382095</ref> <ref>PMID:12126934</ref> | |||
== Function == | |||
[https://www.uniprot.org/uniprot/F16P1_HUMAN F16P1_HUMAN] | |||
<div style="background-color:#fffaf0;"> | |||
== Publication Abstract from PubMed == | |||
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. | |||
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-Sanchez R, Gubler M, Schott B, Benardeau A, Tozzo E, Kitas E Bioorg Med Chem Lett. 2011 Jun 1;21(11):3237-42. Epub 2011 Apr 20. PMID:21550236<ref>PMID:21550236</ref> | |||
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |||
</div> | |||
<div class="pdbe-citations 2y5k" style="background-color:#fffaf0;"></div> | |||
==See Also== | ==See Also== | ||
*[[Fructose-1%2C6-bisphosphatase|Fructose-1%2C6-bisphosphatase]] | *[[Fructose-1%2C6-bisphosphatase 3D structures|Fructose-1%2C6-bisphosphatase 3D structures]] | ||
== References == | |||
== | <references/> | ||
__TOC__ | |||
</StructureSection> | |||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Alvarez-Sanchez | [[Category: Large Structures]] | ||
[[Category: Benardeau | [[Category: Alvarez-Sanchez R]] | ||
[[Category: Benz | [[Category: Benardeau A]] | ||
[[Category: Gubler | [[Category: Benz J]] | ||
[[Category: Haap | [[Category: Gubler M]] | ||
[[Category: Hebeisen | [[Category: Haap W]] | ||
[[Category: Joseph | [[Category: Hebeisen P]] | ||
[[Category: Kirchner | [[Category: Joseph C]] | ||
[[Category: Kitas | [[Category: Kirchner S]] | ||
[[Category: Kuhn | [[Category: Kitas E]] | ||
[[Category: Mohr | [[Category: Kuhn B]] | ||
[[Category: Ruf | [[Category: Mohr P]] | ||
[[Category: Schott | [[Category: Ruf A]] | ||
[[Category: Tozzo | [[Category: Schott B]] | ||
[[Category: Wessel | [[Category: Tozzo E]] | ||
[[Category: Zutter | [[Category: Wessel HP]] | ||
[[Category: Zutter U]] | |||
Latest revision as of 13:45, 20 December 2023
Orally active aminopyridines as inhibitors of tetrameric fructose 1,6- bisphosphataseOrally active aminopyridines as inhibitors of tetrameric fructose 1,6- bisphosphatase
Structural highlights
DiseaseF16P1_HUMAN Defects in FBP1 are the cause of fructose-1,6-bisphosphatase deficiency (FBPD) [MIM:229700. FBPD is inherited as an autosomal recessive disorder mainly in the liver and causes life-threatening episodes of hypoglycemia and metabolic acidosis (lactacidemia) in newborn infants or young children.[1] [2] FunctionPublication Abstract from PubMedA 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. 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-Sanchez R, Gubler M, Schott B, Benardeau A, Tozzo E, Kitas E Bioorg Med Chem Lett. 2011 Jun 1;21(11):3237-42. Epub 2011 Apr 20. PMID:21550236[3] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See AlsoReferences
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