2o5k: Difference between revisions
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==Overview== | ==Overview== | ||
A hydroxy functional group was introduced as the hydrogen bond donor and | A hydroxy functional group was introduced as the hydrogen bond donor and acceptor at the hinge region of protein kinase in order to develop novel ATP-competitive inhibitors. Several derivatives of 7-hydroxyl-1H-benzoimidazole were designed as inhibitors of glycogen synthase kinase-3beta with the help of ab initio calculations and a docking study. Enzymatic assay and an X-ray complex study showed that these designed compounds were highly potent ATP-competitive inhibitors. | ||
==About this Structure== | ==About this Structure== | ||
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[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: [Tau protein] kinase]] | [[Category: [Tau protein] kinase]] | ||
[[Category: Cho, J | [[Category: Cho, J M.]] | ||
[[Category: Cho, Y | [[Category: Cho, Y S.]] | ||
[[Category: Heo, Y | [[Category: Heo, Y S.]] | ||
[[Category: Hyun, Y | [[Category: Hyun, Y L.]] | ||
[[Category: Kim, Y | [[Category: Kim, Y E.]] | ||
[[Category: Lee, S | [[Category: Lee, S C.]] | ||
[[Category: Lee, Y | [[Category: Lee, Y S.]] | ||
[[Category: Ro, S.]] | [[Category: Ro, S.]] | ||
[[Category: Shin, D.]] | [[Category: Shin, D.]] | ||
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[[Category: transferase]] | [[Category: transferase]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:14:40 2008'' | ||
Revision as of 19:14, 21 February 2008
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Crystal Structure of GSK3beta in complex with a benzoimidazol inhibitor
OverviewOverview
A hydroxy functional group was introduced as the hydrogen bond donor and acceptor at the hinge region of protein kinase in order to develop novel ATP-competitive inhibitors. Several derivatives of 7-hydroxyl-1H-benzoimidazole were designed as inhibitors of glycogen synthase kinase-3beta with the help of ab initio calculations and a docking study. Enzymatic assay and an X-ray complex study showed that these designed compounds were highly potent ATP-competitive inhibitors.
About this StructureAbout this Structure
2O5K is a Single protein structure of sequence from Homo sapiens with as ligand. Active as [Tau_protein_kinase [Tau protein] kinase], with EC number 2.7.11.26 Full crystallographic information is available from OCA.
ReferenceReference
Design and synthesis of 7-hydroxy-1H-benzoimidazole derivatives as novel inhibitors of glycogen synthase kinase-3beta., Shin D, Lee SC, Heo YS, Lee WY, Cho YS, Kim YE, Hyun YL, Cho JM, Lee YS, Ro S, Bioorg Med Chem Lett. 2007 Oct 15;17(20):5686-9. Epub 2007 Aug 19. PMID:17764934 [[Category: [Tau protein] kinase]]
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