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2o5k
From Proteopedia
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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.]] | ||
| Line 28: | Line 28: | ||
[[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 16:14, 21 February 2008
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Crystal Structure of GSK3beta in complex with a benzoimidazol inhibitor
Overview
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
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.
Reference
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]]
Page seeded by OCA on Thu Feb 21 18:14:40 2008
Categories: Homo sapiens | Single protein | Cho, J M. | Cho, Y S. | Heo, Y S. | Hyun, Y L. | Kim, Y E. | Lee, S C. | Lee, Y S. | Ro, S. | Shin, D. | HBM | Benzoimidazol inhibitor | Gsk3beta | Transferase
