1h5u: Difference between revisions
New page: left|200px<br /> <applet load="1h5u" size="450" color="white" frame="true" align="right" spinBox="true" caption="1h5u, resolution 1.76Å" /> '''THE 1.76 A RESOLUTI... |
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==About this Structure== | ==About this Structure== | ||
1H5U is a [[http://en.wikipedia.org/wiki/Single_protein Single protein]] structure of sequence from [[http://en.wikipedia.org/wiki/Oryctolagus_cuniculus Oryctolagus cuniculus]] with GLC, CHI and PLP as [[http://en.wikipedia.org/wiki/ligands ligands]]. Active as [[http://en.wikipedia.org/wiki/ ]], with EC number [[http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.4.1.1 2.4.1.1]]. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1H5U OCA]]. | 1H5U is a [[http://en.wikipedia.org/wiki/Single_protein Single protein]] structure of sequence from [[http://en.wikipedia.org/wiki/Oryctolagus_cuniculus Oryctolagus cuniculus]] with GLC, CHI and PLP as [[http://en.wikipedia.org/wiki/ligands ligands]]. Active as [[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]]. Structure known Active Sites: CHI, GLC and PLP. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1H5U OCA]]. | ||
==Reference== | ==Reference== | ||
The 1.76 A resolution crystal structure of glycogen phosphorylase B complexed with glucose, and CP320626, a potential antidiabetic drug., Oikonomakos NG, Zographos SE, Skamnaki VT, Archontis G, Bioorg Med Chem. 2002 May;10(5):1313-9. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=11886794 11886794] | The 1.76 A resolution crystal structure of glycogen phosphorylase B complexed with glucose, and CP320626, a potential antidiabetic drug., Oikonomakos NG, Zographos SE, Skamnaki VT, Archontis G, Bioorg Med Chem. 2002 May;10(5):1313-9. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=11886794 11886794] | ||
[[Category: Oryctolagus cuniculus]] | [[Category: Oryctolagus cuniculus]] | ||
[[Category: Phosphorylase]] | |||
[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Archontis, G.]] | [[Category: Archontis, G.]] | ||
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[[Category: transferase]] | [[Category: transferase]] | ||
''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 11:35:20 2007'' | ||
Revision as of 12:30, 30 October 2007
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THE 1.76 A RESOLUTION CRYSTAL STRUCTURE OF GLYCOGEN PHOSPHORYLASE B COMPLEXED WITH GLUCOSE AND CP320626, A POTENTIAL ANTIDIABETIC DRUG
OverviewOverview
CP320626, a potential antidiabetic drug, inhibits glycogen phosphorylase, in synergism with glucose. To elucidate the structural basis of, synergistic inhibition, we determined the structure of muscle glycogen, phosphorylase b (MGPb) complexed with both glucose and CP320626 at 1.76 A, resolution, and refined to a crystallographic R value of 0.211, (R(free)=0.235). CP320626 binds at a novel allosteric site, which is some, 33 A from the catalytic site, where glucose binds. The high resolution, structure allows unambiguous definition of the conformation of the, 1-acetyl-4-hydroxy-piperidine ring supported by theoretical energy, calculations. Both CP320626 and glucose promote the less active T-state, thereby explaining their synergistic inhibition. Structural comparison of, ... [(full description)]
About this StructureAbout this Structure
1H5U is a [Single protein] structure of sequence from [Oryctolagus cuniculus] with GLC, CHI and PLP as [ligands]. Active as [Phosphorylase], with EC number [2.4.1.1]. Structure known Active Sites: CHI, GLC and PLP. Full crystallographic information is available from [OCA].
ReferenceReference
The 1.76 A resolution crystal structure of glycogen phosphorylase B complexed with glucose, and CP320626, a potential antidiabetic drug., Oikonomakos NG, Zographos SE, Skamnaki VT, Archontis G, Bioorg Med Chem. 2002 May;10(5):1313-9. PMID:11886794
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