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2y5k

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Revision as of 12:36, 22 July 2020

Orally active aminopyridines as inhibitors of tetrameric fructose 1,6- bisphosphatase

Structural highlights

2y5k is a 4 chain structure with sequence from Human. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:
Related:	2jjk, 2wbd, 2fix, 2fhy, 1fta, 2vt5, 2fie, 2wbb, 2y5l
Activity:	Fructose-bisphosphatase, with EC number 3.1.3.11
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

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 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^[3]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

References

↑ Kikawa Y, Inuzuka M, Jin BY, Kaji S, Koga J, Yamamoto Y, Fujisawa K, Hata I, Nakai A, Shigematsu Y, Mizunuma H, Taketo A, Mayumi M, Sudo M. Identification of genetic mutations in Japanese patients with fructose-1,6-bisphosphatase deficiency. Am J Hum Genet. 1997 Oct;61(4):852-61. PMID:9382095
↑ Matsuura T, Chinen Y, Arashiro R, Katsuren K, Tamura T, Hyakuna N, Ohta T. Two newly identified genomic mutations in a Japanese female patient with fructose-1,6-bisphosphatase (FBPase) deficiency. Mol Genet Metab. 2002 Jul;76(3):207-10. PMID:12126934
↑ 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. Orally active aminopyridines as inhibitors of tetrameric fructose-1,6-bisphosphatase. Bioorg Med Chem Lett. 2011 Jun 1;21(11):3237-42. Epub 2011 Apr 20. PMID:21550236 doi:10.1016/j.bmcl.2011.04.044

1 Structural highlights
2 Disease
3 Publication Abstract from PubMed
4 See Also
5 References

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/2y5k"

@@ Line 1: / Line 1: @@
 ==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=''>
+<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 [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://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2Y5K FirstGlance]. <br>
+<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='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://oca.weizmann.ac.il/oca-docs/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>
+<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>
 == Disease ==
@@ Line 22: / Line 22: @@
 ==See Also==
-*[[Fructose-1%2C6-bisphosphatase|Fructose-1%2C6-bisphosphatase]]
+*[[Fructose-1%2C6-bisphosphatase 3D structures|Fructose-1%2C6-bisphosphatase 3D structures]]
 == References ==
 <references/>
@@ Line 29: / Line 29: @@
 [[Category: Fructose-bisphosphatase]]
 [[Category: Human]]
+[[Category: Large Structures]]
 [[Category: Alvarez-Sanchez, R]]
 [[Category: Benardeau, A]]

2y5k

From Proteopedia

Revision as of 12:36, 22 July 2020

Orally active aminopyridines as inhibitors of tetrameric fructose 1,6- bisphosphatase

Structural highlights

Disease

Publication Abstract from PubMed

See Also

References

Contents

Proteopedia Page Contributors and Editors (what is this?)

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