Cyclic AMP Analog Blocks Kinase Activation by Stabilizing Inactive Conformation: Conformational Selection Highlights a New Concept in Allosteric Inhibitor Design

The regulatory (R) subunit of protein kinase A serves to modulate the activity of protein kinase A in a cAMP-dependent manner and exists in two distinct and structurally dissimilar, end point cAMP-bound “B” and C-subunit-bound “H”-conformations. Here we report mechanistic details of cAMP action as y...

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Main Authors: Badireddy, Suguna, Yunfeng, Gao, Ritchie, Mark, Akamine, Pearl, Wu, Jian, Kim, Choel W., Taylor, Susan S., Qingsong, Lin, Swaminathan, Kunchithapadam, Anand, Ganesh S.
Formato: Artigo
Idioma:Inglês
Publicado: The American Society for Biochemistry and Molecular Biology 2011
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Research
Acceso en liña:https://ncbi.nlm.nih.gov/pmc/articles/PMC3047156/
https://ncbi.nlm.nih.gov/pubmed/21081668
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1074/mcp.M110.004390
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