4ise: Difference between revisions

No edit summary
No edit summary
 
Line 4: Line 4:
== Structural highlights ==
== Structural highlights ==
<table><tr><td colspan='2'>[[4ise]] is a 1 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=4ISE OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4ISE FirstGlance]. <br>
<table><tr><td colspan='2'>[[4ise]] is a 1 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=4ISE OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4ISE FirstGlance]. <br>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=1FW:(2S)-3-CYCLOHEXYL-2-(6-FLUORO-4-OXOQUINAZOLIN-3(4H)-YL)-N-(1,3-THIAZOL-2-YL)PROPANAMIDE'>1FW</scene>, <scene name='pdbligand=GLC:ALPHA-D-GLUCOSE'>GLC</scene>, <scene name='pdbligand=IOD:IODIDE+ION'>IOD</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]] 1.78&#8491;</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=1FW:(2S)-3-CYCLOHEXYL-2-(6-FLUORO-4-OXOQUINAZOLIN-3(4H)-YL)-N-(1,3-THIAZOL-2-YL)PROPANAMIDE'>1FW</scene>, <scene name='pdbligand=GLC:ALPHA-D-GLUCOSE'>GLC</scene>, <scene name='pdbligand=IOD:IODIDE+ION'>IOD</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=4ise FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ise OCA], [https://pdbe.org/4ise PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4ise RCSB], [https://www.ebi.ac.uk/pdbsum/4ise PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4ise 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=4ise FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ise OCA], [https://pdbe.org/4ise PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4ise RCSB], [https://www.ebi.ac.uk/pdbsum/4ise PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4ise ProSAT]</span></td></tr>
</table>
</table>
Line 11: Line 12:
== Function ==
== Function ==
[https://www.uniprot.org/uniprot/HXK4_HUMAN HXK4_HUMAN] Catalyzes the initial step in utilization of glucose by the beta-cell and liver at physiological glucose concentration. Glucokinase has a high Km for glucose, and so it is effective only when glucose is abundant. The role of GCK is to provide G6P for the synthesis of glycogen. Pancreatic glucokinase plays an important role in modulating insulin secretion. Hepatic glucokinase helps to facilitate the uptake and conversion of glucose by acting as an insulin-sensitive determinant of hepatic glucose usage.
[https://www.uniprot.org/uniprot/HXK4_HUMAN HXK4_HUMAN] Catalyzes the initial step in utilization of glucose by the beta-cell and liver at physiological glucose concentration. Glucokinase has a high Km for glucose, and so it is effective only when glucose is abundant. The role of GCK is to provide G6P for the synthesis of glycogen. Pancreatic glucokinase plays an important role in modulating insulin secretion. Hepatic glucokinase helps to facilitate the uptake and conversion of glucose by acting as an insulin-sensitive determinant of hepatic glucose usage.
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
Guided by co-crystal structures of compounds 15, 22 and 30, an SBDD approach led to the discovery of the 6-methyl pyridone series as a novel class of GKAs that potently activate GK in enzyme and cell assays. Anti-diabetic OGTT efficacy was demonstrated with 54 in a mouse model of type 2 diabetes.
Design, synthesis and SAR of novel glucokinase activators.,Cheruvallath ZS, Gwaltney SL 2nd, Sabat M, Tang M, Feng J, Wang H, Miura J, Guntupalli P, Jennings A, Hosfield D, Lee B, Wu Y Bioorg Med Chem Lett. 2013 Apr 1;23(7):2166-71. doi: 10.1016/j.bmcl.2013.01.093. , Epub 2013 Feb 4. PMID:23434031<ref>PMID:23434031</ref>
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
<div class="pdbe-citations 4ise" style="background-color:#fffaf0;"></div>


==See Also==
==See Also==

Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)

OCA