2c1a: Difference between revisions
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==About this Structure== | ==About this Structure== | ||
2C1A is a | 2C1A is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Bos_taurus Bos taurus] and [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with I5S as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Transferred_entry:_2.7.11.1 Transferred entry: 2.7.11.1], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.37 2.7.1.37] Structure known Active Site: AC1. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2C1A OCA]. | ||
==Reference== | ==Reference== | ||
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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 Mon Nov 5 15:18:38 2007'' | ||
Revision as of 16:13, 5 November 2007
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STRUCTURE OF CAMP-DEPENDENT PROTEIN KINASE COMPLEXED WITH ISOQUINOLINE-5-SULFONIC ACID (2-(2-(4-CHLOROBENZYLOXY) ETHYLAMINO)ETHYL)AMIDE
OverviewOverview
Structure-based drug design of novel isoquinoline-5-sulfonamide inhibitors, of PKB as potential antitumour agents was investigated. Constrained, pyrrolidine analogues that mimicked the bound conformation of linear, prototypes were identified and investigated by co-crystal structure, determinations with the related protein PKA. Detailed variation in the, binding modes between inhibitors with similar overall conformations was, observed. Potent PKB inhibitors from this series inhibited GSK3beta, phosphorylation in cellular assays, consistent with inhibition of PKB, kinase activity in cells.
About this StructureAbout this Structure
2C1A is a Protein complex structure of sequences from Bos taurus and Homo sapiens with I5S as ligand. Active as Transferred entry: 2.7.11.1, with EC number 2.7.1.37 Structure known Active Site: AC1. Full crystallographic information is available from OCA.
ReferenceReference
Structure-based design of isoquinoline-5-sulfonamide inhibitors of protein kinase B., Collins I, Caldwell J, Fonseca T, Donald A, Bavetsias V, Hunter LJ, Garrett MD, Rowlands MG, Aherne GW, Davies TG, Berdini V, Woodhead SJ, Davis D, Seavers LC, Wyatt PG, Workman P, McDonald E, Bioorg Med Chem. 2006 Feb 15;14(4):1255-73. Epub 2005 Oct 24. PMID:16249095
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OCA- Pages with broken file links
- Bos taurus
- Homo sapiens
- Protein complex
- Transferred entry: 2.7.11.1
- Aherne, G.W.
- Bavetsias, V.
- Berdini, V.
- Caldwell, J.
- Collins, I.
- Davies, T.G.
- Donald, A.
- Fonseca, T.
- Garrett, M.D.
- Hunter, L.J.
- Mcdonald, E.
- Rowlands, M.G.
- Seavers, L.C.A.
- Woodhead, S.
- Workman, P.
- Wyatt, P.G.
- I5S
- Atp-binding
- Camp
- Complex (transferase/inhibitor)
- Phosphorylation
- Protein kinase inhibitor
- Serine/threonine-protein kinase
- Transferase