View source for 2y5l


==orally active aminopyridines as inhibitors of tetrameric fructose 1,6- bisphosphatase==
<StructureSection load='2y5l' size='340' side='right'caption='[[2y5l]], [[Resolution|resolution]] 2.20&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[2y5l]] is a 8 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=2Y5L OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2Y5L 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]] 2.2&#8491;</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=RO8:N-{[(2Z)-5-BROMO-1,3-THIAZOL-2(3H)-YLIDENE]CARBAMOYL}-3-CHLOROBENZENESULFONAMIDE'>RO8</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=2y5l FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2y5l OCA], [https://pdbe.org/2y5l PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2y5l RCSB], [https://www.ebi.ac.uk/pdbsum/2y5l PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2y5l 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&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
<div class="pdbe-citations 2y5l" style="background-color:#fffaf0;"></div>

==See Also==
*[[Fructose-1%2C6-bisphosphatase 3D structures|Fructose-1%2C6-bisphosphatase 3D structures]]
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Homo sapiens]]
[[Category: Large Structures]]
[[Category: Alvarez-sanchez r]]
[[Category: Benardeau a]]
[[Category: Benz j]]
[[Category: Gubler m]]
[[Category: Haap w]]
[[Category: Hebeisen p]]
[[Category: Joseph c]]
[[Category: Kirchner s]]
[[Category: Kitas e]]
[[Category: Kuhn b]]
[[Category: Mohr p]]
[[Category: Ruf a]]
[[Category: Schott b]]
[[Category: Tozzo e]]
[[Category: Wessel hp]]
[[Category: Zutter u]]