2qcs

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{{STRUCTURE_2qcs| PDB=2qcs | SCENE= }}
{{STRUCTURE_2qcs| PDB=2qcs | SCENE= }}
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'''A complex structure between the Catalytic and Regulatory subunit of Protein Kinase A that represents the inhibited state'''
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===A complex structure between the Catalytic and Regulatory subunit of Protein Kinase A that represents the inhibited state===
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==Overview==
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Protein kinase A (PKA) holoenzyme is one of the major receptors for cyclic adenosine monophosphate (cAMP), where an extracellular stimulus is translated into a signaling response. We report here the structure of a complex between the PKA catalytic subunit and a mutant RI regulatory subunit, RIalpha(91-379:R333K), containing both cAMP-binding domains. Upon binding to the catalytic subunit, RI undergoes a dramatic conformational change in which the two cAMP-binding domains uncouple and wrap around the large lobe of the catalytic subunit. This large conformational reorganization reveals the concerted mechanism required to bind and inhibit the catalytic subunit. The structure also reveals a holoenzyme-specific salt bridge between two conserved residues, Glu261 and Arg366, that tethers the two adenine capping residues far from their cAMP-binding sites. Mutagenesis of these residues demonstrates their importance for PKA activation. Our structural insights, combined with the mutagenesis results, provide a molecular mechanism for the ordered and cooperative activation of PKA by cAMP.
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The line below this paragraph, {{ABSTRACT_PUBMED_17889648}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 17889648 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17889648}}
==About this Structure==
==About this Structure==
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[[Category: Protein-protein interaction]]
[[Category: Protein-protein interaction]]
[[Category: Transferase/transferase inhibitor complex]]
[[Category: Transferase/transferase inhibitor complex]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 14:44:38 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 11:31:40 2008''

Revision as of 08:31, 28 July 2008

Image:2qcs.png

Template:STRUCTURE 2qcs

A complex structure between the Catalytic and Regulatory subunit of Protein Kinase A that represents the inhibited state

Template:ABSTRACT PUBMED 17889648

About this Structure

2QCS is a Protein complex structure of sequences from Bos taurus and Mus musculus. Full crystallographic information is available from OCA.

Reference

PKA-I holoenzyme structure reveals a mechanism for cAMP-dependent activation., Kim C, Cheng CY, Saldanha SA, Taylor SS, Cell. 2007 Sep 21;130(6):1032-43. PMID:17889648

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