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| [[Image:2oh0.gif|left|200px]] | | {{Seed}} |
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| {{STRUCTURE_2oh0| PDB=2oh0 | SCENE= }} | | {{STRUCTURE_2oh0| PDB=2oh0 | SCENE= }} |
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| '''Crystal structure of Protein Kinase A in complex with Pyridine-Pyrazolopyridine Based Inhibitors'''
| | ===Crystal structure of Protein Kinase A in complex with Pyridine-Pyrazolopyridine Based Inhibitors=== |
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| ==Overview==
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| Thr-211 is one of three different amino acid residues in the kinase domain of protein kinase B/Akt as compared to protein kinase A (PKA), a closely related analog in the same AGC family. In an attempt to improve the potency and selectivity of our indazole-pyridine series of Akt inhibitors over PKA, efforts have focused on the incorporation of a chemical functionality to interact with the hydroxy group of Thr-211. Several substituents including an oxygen anion, amino, and nitro groups have been introduced at the C-6 position of the indazole scaffold, leading to a significant drop in Akt potency. Incorporation of a nitrogen atom into the phenyl ring at the same position (i.e., 9f) maintained the Akt activity and, in some cases, improved the selectivity over PKA. The structure-activity relationships of the new pyridine-pyrazolopyridine series of Akt inhibitors and their structural features when bound to PKA are also discussed.
| | The line below this paragraph, {{ABSTRACT_PUBMED_17258463}}, adds the Publication Abstract to the page |
| | (as it appears on PubMed at http://www.pubmed.gov), where 17258463 is the PubMed ID number. |
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| | {{ABSTRACT_PUBMED_17258463}} |
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| ==About this Structure== | | ==About this Structure== |
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| [[Category: Akt]] | | [[Category: Akt]] |
| [[Category: Protein kinase some]] | | [[Category: Protein kinase some]] |
| ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 10:53:54 2008'' | | |
| | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 05:28:36 2008'' |