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==Orally active aminopyridines as inhibitors of tetrameric fructose 1,6- bisphosphatase== | ==Orally active aminopyridines as inhibitors of tetrameric fructose 1,6- bisphosphatase== | ||
<StructureSection load='2y5k' size='340' side='right' caption='[[2y5k]], [[Resolution|resolution]] 2.10Å' scene=''> | <StructureSection load='2y5k' size='340' side='right'caption='[[2y5k]], [[Resolution|resolution]] 2.10Å' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
<table><tr><td colspan='2'>[[2y5k]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. 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 [http:// | <table><tr><td colspan='2'>[[2y5k]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. 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 [http://proteopedia.org/fgij/fg.htm?mol=2Y5K FirstGlance]. <br> | ||
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><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> | </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='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[2jjk|2jjk]], [[2wbd|2wbd]], [[2fix|2fix]], [[2fhy|2fhy]], [[1fta|1fta]], [[2vt5|2vt5]], [[2fie|2fie]], [[2wbb|2wbb]], [[2y5l|2y5l]]</td></tr> | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[2jjk|2jjk]], [[2wbd|2wbd]], [[2fix|2fix]], [[2fhy|2fhy]], [[1fta|1fta]], [[2vt5|2vt5]], [[2fie|2fie]], [[2wbb|2wbb]], [[2y5l|2y5l]]</td></tr> | ||
<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Fructose-bisphosphatase Fructose-bisphosphatase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.3.11 3.1.3.11] </span></td></tr> | <tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Fructose-bisphosphatase Fructose-bisphosphatase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.3.11 3.1.3.11] </span></td></tr> | ||
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http:// | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://proteopedia.org/fgij/fg.htm?mol=2y5k FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2y5k OCA], [http://pdbe.org/2y5k PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=2y5k RCSB], [http://www.ebi.ac.uk/pdbsum/2y5k PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=2y5k ProSAT]</span></td></tr> | ||
</table> | </table> | ||
== Disease == | == Disease == | ||
| Line 22: | Line 22: | ||
==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 == | ||
<references/> | <references/> | ||
| Line 29: | Line 29: | ||
[[Category: Fructose-bisphosphatase]] | [[Category: Fructose-bisphosphatase]] | ||
[[Category: Human]] | [[Category: Human]] | ||
[[Category: Large Structures]] | |||
[[Category: Alvarez-Sanchez, R]] | [[Category: Alvarez-Sanchez, R]] | ||
[[Category: Benardeau, A]] | [[Category: Benardeau, A]] | ||
Revision as of 15:36, 22 July 2020
Orally active aminopyridines as inhibitors of tetrameric fructose 1,6- bisphosphataseOrally active aminopyridines as inhibitors of tetrameric fructose 1,6- bisphosphatase
Structural highlights
Disease[F16P1_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] Publication 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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