2y5k: Difference between revisions

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[[Image:2y5k.png|left|200px]]


{{STRUCTURE_2y5k| PDB=2y5k | SCENE= }}
==Orally active aminopyridines as inhibitors of tetrameric fructose 1,6- bisphosphatase==
<StructureSection load='2y5k' size='340' side='right'caption='[[2y5k]], [[Resolution|resolution]] 2.10&Aring;' 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]] 2.1&#8491;</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===
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>


{{ABSTRACT_PUBMED_21550236}}
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
 
</div>
==About this Structure==
<div class="pdbe-citations 2y5k" style="background-color:#fffaf0;"></div>
[[2y5k]] is a 4 chain structure of [[Fructose-1%2C6-bisphosphatase]] 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].


==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 ==
==Reference==
<references/>
<ref group="xtra">PMID:021550236</ref><references group="xtra"/>
__TOC__
[[Category: Fructose-bisphosphatase]]
</StructureSection>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Alvarez-Sanchez, R.]]
[[Category: Large Structures]]
[[Category: Benardeau, A.]]
[[Category: Alvarez-Sanchez R]]
[[Category: Benz, J.]]
[[Category: Benardeau A]]
[[Category: Gubler, M.]]
[[Category: Benz J]]
[[Category: Haap, W.]]
[[Category: Gubler M]]
[[Category: Hebeisen, P.]]
[[Category: Haap W]]
[[Category: Joseph, C.]]
[[Category: Hebeisen P]]
[[Category: Kirchner, S.]]
[[Category: Joseph C]]
[[Category: Kitas, E.]]
[[Category: Kirchner S]]
[[Category: Kuhn, B.]]
[[Category: Kitas E]]
[[Category: Mohr, P.]]
[[Category: Kuhn B]]
[[Category: Ruf, A.]]
[[Category: Mohr P]]
[[Category: Schott, B.]]
[[Category: Ruf A]]
[[Category: Tozzo, E.]]
[[Category: Schott B]]
[[Category: Wessel, H P.]]
[[Category: Tozzo E]]
[[Category: Zutter, U.]]
[[Category: Wessel HP]]
[[Category: Hydrolase]]
[[Category: Zutter U]]
Retrieved from "https://proteopedia.org/2y5k"