5jtt

From Proteopedia

(Difference between revisions)

Current revision

Crystal structure of GPb in complex with 8a

Structural highlights

5jtt is a 1 chain structure with sequence from Oryctolagus cuniculus. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:	X-ray diffraction, Resolution 1.85Å
Ligands:	, ,
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

PYGM_RABIT Phosphorylase is an important allosteric enzyme in carbohydrate metabolism. Enzymes from different sources differ in their regulatory mechanisms and in their natural substrates. However, all known phosphorylases share catalytic and structural properties.

Publication Abstract from PubMed

C-beta-d-Glucopyranosyl pyrrole derivatives were prepared in the reactions of pyrrole, 2-, and 3-aryl-pyrroles with O-peracetylated beta-d-glucopyranosyl trichloroacetimidate, while 2-(beta-d-glucopyranosyl) indole was obtained by a cross coupling of O-perbenzylated beta-d-glucopyranosyl acetylene with N-tosyl-2-iodoaniline followed by spontaneous ring closure. An improved synthesis of O-perbenzoylated 2-(beta-d-glucopyranosyl) imidazoles was achieved by reacting C-glucopyranosyl formimidates with alpha-aminoketones. The deprotected compounds were assayed with isoforms of glycogen phosphorylase (GP) to show no activity of the pyrroles against rabbit muscle GPb. The imidazoles proved to be the best known glucose derived inhibitors of not only the muscle enzymes (both a and b) but also of the pharmacologically relevant human liver GPa (Ki = 156 and 26 nM for the 4(5)-phenyl and -(2-naphthyl) derivatives, respectively). An X-ray crystallographic study of the rmGPb-imidazole complexes revealed structural features of the strong binding, and also allowed to explain the absence of inhibition for the pyrrole derivatives.

Synthetic, enzyme kinetic, and protein crystallographic studies of C-beta-d-glucopyranosyl pyrroles and imidazoles reveal and explain low nanomolar inhibition of human liver glycogen phosphorylase.,Kantsadi AL, Bokor E, Kun S, Stravodimos GA, Chatzileontiadou DS, Leonidas DD, Juhasz-Toth E, Szakacs A, Batta G, Docsa T, Gergely P, Somsak L Eur J Med Chem. 2016 Jul 12;123:737-745. doi: 10.1016/j.ejmech.2016.06.049. PMID:27522507^[1]

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

References

↑ Kantsadi AL, Bokor E, Kun S, Stravodimos GA, Chatzileontiadou DS, Leonidas DD, Juhasz-Toth E, Szakacs A, Batta G, Docsa T, Gergely P, Somsak L. Synthetic, enzyme kinetic, and protein crystallographic studies of C-beta-d-glucopyranosyl pyrroles and imidazoles reveal and explain low nanomolar inhibition of human liver glycogen phosphorylase. Eur J Med Chem. 2016 Jul 12;123:737-745. doi: 10.1016/j.ejmech.2016.06.049. PMID:27522507 doi:http://dx.doi.org/10.1016/j.ejmech.2016.06.049

1 Structural highlights
2 Function
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/5jtt"

@@ Line 1: / Line 1: @@
 ==Crystal structure of GPb in complex with 8a==
-<StructureSection load='5jtt' size='340' side='right' caption='[[5jtt]], [[Resolution|resolution]] 1.85&Aring;' scene=''>
+<StructureSection load='5jtt' size='340' side='right'caption='[[5jtt]], [[Resolution|resolution]] 1.85&Aring;' scene=''>
 == Structural highlights ==
-<table><tr><td colspan='2'>[[5jtt]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Oryctolagus_cuniculus Oryctolagus cuniculus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5JTT OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5JTT FirstGlance]. <br>
+<table><tr><td colspan='2'>[[5jtt]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Oryctolagus_cuniculus Oryctolagus cuniculus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5JTT OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5JTT FirstGlance]. <br>
-</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=6MY:(1S)-1,5-ANHYDRO-1-(5-PHENYL-1H-IMIDAZOL-2-YL)-D-GLUCITOL'>6MY</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene>, <scene name='pdbligand=PLP:PYRIDOXAL-5-PHOSPHATE'>PLP</scene></td></tr>
+</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.85&#8491;</td></tr>
-<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Phosphorylase Phosphorylase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.4.1.1 2.4.1.1] </span></td></tr>
+<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=6MY:(1S)-1,5-ANHYDRO-1-(5-PHENYL-1H-IMIDAZOL-2-YL)-D-GLUCITOL'>6MY</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene>, <scene name='pdbligand=PLP:PYRIDOXAL-5-PHOSPHATE'>PLP</scene></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=5jtt FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5jtt OCA], [http://pdbe.org/5jtt PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5jtt RCSB], [http://www.ebi.ac.uk/pdbsum/5jtt PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5jtt ProSAT]</span></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=5jtt FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5jtt OCA], [https://pdbe.org/5jtt PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5jtt RCSB], [https://www.ebi.ac.uk/pdbsum/5jtt PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5jtt ProSAT]</span></td></tr>
 </table>
 == Function ==
-[[http://www.uniprot.org/uniprot/PYGM_RABIT PYGM_RABIT]] Phosphorylase is an important allosteric enzyme in carbohydrate metabolism. Enzymes from different sources differ in their regulatory mechanisms and in their natural substrates. However, all known phosphorylases share catalytic and structural properties.
+[https://www.uniprot.org/uniprot/PYGM_RABIT PYGM_RABIT] Phosphorylase is an important allosteric enzyme in carbohydrate metabolism. Enzymes from different sources differ in their regulatory mechanisms and in their natural substrates. However, all known phosphorylases share catalytic and structural properties.
 <div style="background-color:#fffaf0;">
 == Publication Abstract from PubMed ==
@@ Line 19: / Line 19: @@
 </div>
 <div class="pdbe-citations 5jtt" style="background-color:#fffaf0;"></div>
+==See Also==
+*[[Glycogen phosphorylase 3D structures|Glycogen phosphorylase 3D structures]]
 == References ==
 <references/>
 __TOC__
 </StructureSection>
+[[Category: Large Structures]]
 [[Category: Oryctolagus cuniculus]]
-[[Category: Phosphorylase]]
+[[Category: Chatzileontiadou DSM]]
-[[Category: Chatzileontiadou, D S.M]]
+[[Category: Kantsadi AL]]
-[[Category: Kantsadi, A L]]
+[[Category: Leonidas DD]]
-[[Category: Leonidas, D D]]
+[[Category: Stravodimos GA]]
-[[Category: Stravodimos, G A]]
-[[Category: Alpha and beta protein transferase]]
-[[Category: Transferase]]

5jtt

From Proteopedia

Current revision

Crystal structure of GPb in complex with 8a

Structural highlights

Function

Publication Abstract from PubMed

See Also

References

Contents

Proteopedia Page Contributors and Editors (what is this?)

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