2c1a: Difference between revisions
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==Overview== | ==Overview== | ||
Structure-based drug design of novel isoquinoline-5-sulfonamide inhibitors | 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 Structure== | ==About this Structure== | ||
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[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Protein complex]] | [[Category: Protein complex]] | ||
[[Category: Transferred entry: 2 | [[Category: Transferred entry: 2 7.11 1]] | ||
[[Category: Aherne, G | [[Category: Aherne, G W.]] | ||
[[Category: Bavetsias, V.]] | [[Category: Bavetsias, V.]] | ||
[[Category: Berdini, V.]] | [[Category: Berdini, V.]] | ||
[[Category: Caldwell, J.]] | [[Category: Caldwell, J.]] | ||
[[Category: Collins, I.]] | [[Category: Collins, I.]] | ||
[[Category: Davies, T | [[Category: Davies, T G.]] | ||
[[Category: Donald, A.]] | [[Category: Donald, A.]] | ||
[[Category: Fonseca, T.]] | [[Category: Fonseca, T.]] | ||
[[Category: Garrett, M | [[Category: Garrett, M D.]] | ||
[[Category: Hunter, L | [[Category: Hunter, L J.]] | ||
[[Category: Mcdonald, E.]] | [[Category: Mcdonald, E.]] | ||
[[Category: Rowlands, M | [[Category: Rowlands, M G.]] | ||
[[Category: Seavers, L | [[Category: Seavers, L C.A.]] | ||
[[Category: Woodhead, S.]] | [[Category: Woodhead, S.]] | ||
[[Category: Workman, P.]] | [[Category: Workman, P.]] | ||
[[Category: Wyatt, P | [[Category: Wyatt, P G.]] | ||
[[Category: I5S]] | [[Category: I5S]] | ||
[[Category: atp-binding]] | [[Category: atp-binding]] | ||
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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 16:43:48 2008'' | ||
