1uzu: Difference between revisions
New page: left|200px<br /> <applet load="1uzu" size="450" color="white" frame="true" align="right" spinBox="true" caption="1uzu, resolution 2.30Å" /> '''GLYCOGEN PHOSPHORYL... |
No edit summary |
||
| Line 8: | Line 8: | ||
==About this Structure== | ==About this Structure== | ||
1UZU is a [[http://en.wikipedia.org/wiki/Single_protein Single protein]] structure of sequence from [[http://en.wikipedia.org/wiki/ ]] with PLP and INR 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=1UZU OCA]]. | 1UZU 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 PLP and INR 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 Site: PLP. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1UZU OCA]]. | ||
==Reference== | ==Reference== | ||
Binding of the potential antitumour agent indirubin-5-sulphonate at the inhibitor site of rabbit muscle glycogen phosphorylase b. Comparison with ligand binding to pCDK2-cyclin A complex., Kosmopoulou MN, Leonidas DD, Chrysina ED, Bischler N, Eisenbrand G, Sakarellos CE, Pauptit R, Oikonomakos NG, Eur J Biochem. 2004 Jun;271(11):2280-90. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=15153119 15153119] | Binding of the potential antitumour agent indirubin-5-sulphonate at the inhibitor site of rabbit muscle glycogen phosphorylase b. Comparison with ligand binding to pCDK2-cyclin A complex., Kosmopoulou MN, Leonidas DD, Chrysina ED, Bischler N, Eisenbrand G, Sakarellos CE, Pauptit R, Oikonomakos NG, Eur J Biochem. 2004 Jun;271(11):2280-90. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=15153119 15153119] | ||
[[Category: Oryctolagus cuniculus]] | |||
[[Category: Phosphorylase]] | |||
[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Bischler, N.]] | [[Category: Bischler, N.]] | ||
| Line 29: | Line 31: | ||
[[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 11:21:36 2007'' | ||
Revision as of 12:16, 30 October 2007
|
GLYCOGEN PHOSPHORYLASE B IN COMPLEX WITH INDIRUBIN-5'-SULPHONATE
OverviewOverview
The binding of indirubin-5-sulphonate (E226), a potential anti-tumour, agent and a potent inhibitor (IC(50) = 35 nm) of cyclin-dependent kinase 2, (CDK2) and glycogen phosphorylase (GP) has been studied by kinetic and, crystallographic methods. Kinetic analysis revealed that E226 is a, moderate inhibitor of GPb (K(i) = 13.8 +/- 0.2 micro m) and GPa (K(i) =, 57.8 +/- 7.1 micro m) and acts synergistically with glucose. To explore, the molecular basis of E226 binding we have determined the crystal, structure of the GPb/E226 complex at 2.3 A resolution. Structure analysis, shows clearly that E226 binds at the purine inhibitor site, where caffeine, and flavopiridol also bind [Oikonomakos, N.G., Schnier, J.B., Zographos, S.E., Skamnaki, V.T., Tsitsanou, K.E. & Johnson, L.N. (2000) J. Biol., ... [(full description)]
About this StructureAbout this Structure
1UZU is a [Single protein] structure of sequence from [Oryctolagus cuniculus] with PLP and INR as [ligands]. Active as [Phosphorylase], with EC number [2.4.1.1]. Structure known Active Site: PLP. Full crystallographic information is available from [OCA].
ReferenceReference
Binding of the potential antitumour agent indirubin-5-sulphonate at the inhibitor site of rabbit muscle glycogen phosphorylase b. Comparison with ligand binding to pCDK2-cyclin A complex., Kosmopoulou MN, Leonidas DD, Chrysina ED, Bischler N, Eisenbrand G, Sakarellos CE, Pauptit R, Oikonomakos NG, Eur J Biochem. 2004 Jun;271(11):2280-90. PMID:15153119
Page seeded by OCA on Tue Oct 30 11:21:36 2007