2y5l: Difference between revisions

Latest revision as of 13:45, 20 December 2023

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

Structural highlights

2y5l is a 8 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:	X-ray diffraction, Resolution 2.2Å
Ligands:
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]

Function

F16P1_HUMAN

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

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OCA

[1] 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

[2] 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

[3] 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]

[2]

[3]

@@ Line 1: / Line 1: @@
-[[Image:2y5l.jpg|left|200px]]
-<!--
+==orally active aminopyridines as inhibitors of tetrameric fructose 1,6- bisphosphatase==
-The line below this paragraph, containing "STRUCTURE_2y5l", creates the "Structure Box" on the page.
+<StructureSection load='2y5l' size='340' side='right'caption='[[2y5l]], [[Resolution|resolution]] 2.20&Aring;' scene=''>
-You may change the PDB parameter (which sets the PDB file loaded into the applet)
+== Structural highlights ==
-or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
+<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>
-or leave the SCENE parameter empty for the default display.
+</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>
-{{STRUCTURE_2y5l|  PDB=2y5l  |  SCENE=  }}
+<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===
+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>
-==About this Structure==
+==See Also==
-[[2y5l]] is a 8 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=2Y5L OCA].
+*[[Fructose-1%2C6-bisphosphatase 3D structures|Fructose-1%2C6-bisphosphatase 3D structures]]
-[[Category: Fructose-bisphosphatase]]
+== References ==
+<references/>
+__TOC__
+</StructureSection>
 [[Category: Homo sapiens]]
-[[Category: Alvarez, 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: Zutter u]]

2y5l: Difference between revisions

Latest revision as of 13:45, 20 December 2023

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

Structural highlights

Disease

Function

Publication Abstract from PubMed

See Also

References

Contents

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2y5l: Difference between revisions

Latest revision as of 13:45, 20 December 2023

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

Structural highlights

Disease

Function

Publication Abstract from PubMed

See Also

References

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