2y5k

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{{STRUCTURE_2y5k| PDB=2y5k | SCENE= }}
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==ORALLY ACTIVE AMINOPYRIDINES AS INHIBITORS OF TETRAMERIC FRUCTOSE 1,6-BISPHOSPHATASE==
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===ORALLY ACTIVE AMINOPYRIDINES AS INHIBITORS OF TETRAMERIC FRUCTOSE 1,6-BISPHOSPHATASE===
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<StructureSection load='2y5k' size='340' side='right' caption='[[2y5k]], [[Resolution|resolution]] 2.10&Aring;' scene=''>
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{{ABSTRACT_PUBMED_21550236}}
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== Structural highlights ==
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<table><tr><td colspan='2'>[[2y5k]] is a 4 chain structure with sequence from [http://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 [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2Y5K FirstGlance]. <br>
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</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>
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<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>
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<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>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2y5k FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2y5k OCA], [http://www.rcsb.org/pdb/explore.do?structureId=2y5k RCSB], [http://www.ebi.ac.uk/pdbsum/2y5k PDBsum]</span></td></tr>
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</table>
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== Disease ==
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[[http://www.uniprot.org/uniprot/F16P1_HUMAN F16P1_HUMAN]] Defects in FBP1 are the cause of fructose-1,6-bisphosphatase deficiency (FBPD) [MIM:[http://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>
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== Function ==
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==Disease==
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<div style="background-color:#fffaf0;">
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[[http://www.uniprot.org/uniprot/F16P1_HUMAN F16P1_HUMAN]] Defects in FBP1 are the cause of fructose-1,6-bisphosphatase deficiency (FBPD) [MIM:[http://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>
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== Publication Abstract from PubMed ==
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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.
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==About this Structure==
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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-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>
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[[2y5k]] is a 4 chain structure with sequence from [http://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].
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
==See Also==
==See Also==
*[[Fructose-1%2C6-bisphosphatase|Fructose-1%2C6-bisphosphatase]]
*[[Fructose-1%2C6-bisphosphatase|Fructose-1%2C6-bisphosphatase]]
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== References ==
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==Reference==
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<references/>
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<ref group="xtra">PMID:021550236</ref><references group="xtra"/><references/>
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__TOC__
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</StructureSection>
[[Category: Fructose-bisphosphatase]]
[[Category: Fructose-bisphosphatase]]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Alvarez-Sanchez, R.]]
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[[Category: Alvarez-Sanchez, R]]
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[[Category: Benardeau, A.]]
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[[Category: Benardeau, A]]
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[[Category: Benz, J.]]
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[[Category: Benz, J]]
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[[Category: Gubler, M.]]
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[[Category: Gubler, M]]
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[[Category: Haap, W.]]
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[[Category: Haap, W]]
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[[Category: Hebeisen, P.]]
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[[Category: Hebeisen, P]]
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[[Category: Joseph, C.]]
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[[Category: Joseph, C]]
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[[Category: Kirchner, S.]]
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[[Category: Kirchner, S]]
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[[Category: Kitas, E.]]
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[[Category: Kitas, E]]
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[[Category: Kuhn, B.]]
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[[Category: Kuhn, B]]
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[[Category: Mohr, P.]]
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[[Category: Mohr, P]]
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[[Category: Ruf, A.]]
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[[Category: Ruf, A]]
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[[Category: Schott, B.]]
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[[Category: Schott, B]]
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[[Category: Tozzo, E.]]
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[[Category: Tozzo, E]]
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[[Category: Wessel, H P.]]
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[[Category: Wessel, H P]]
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[[Category: Zutter, U.]]
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[[Category: Zutter, U]]
[[Category: Hydrolase]]
[[Category: Hydrolase]]

Revision as of 14:22, 18 December 2014

ORALLY ACTIVE AMINOPYRIDINES AS INHIBITORS OF TETRAMERIC FRUCTOSE 1,6-BISPHOSPHATASE

2y5k, resolution 2.10Å

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