Structure and allostery of the PKA RIIbeta tetrameric holoenzyme
Zhang, P., Smith-Nguyen, E.V., Keshwani, M.M., Deal, M.S., Kornev, A.P., Taylor, S.S.(2012) Science 335: 712-716
- PubMed: 22323819 
- DOI: https://doi.org/10.1126/science.1213979
- Primary Citation of Related Structures:  
3TNP, 3TNQ - PubMed Abstract: 
In its physiological state, cyclic adenosine monophosphate (cAMP)-dependent protein kinase (PKA) is a tetramer that contains a regulatory (R) subunit dimer and two catalytic (C) subunits. We describe here the 2.3 angstrom structure of full-length tetrameric RII¦Â(2):C(2) holoenzyme. This structure showing a dimer of dimers provides a mechanistic understanding of allosteric activation by cAMP. The heterodimers are anchored together by an interface created by the ¦Â4-¦Â5 loop in the RII¦Â subunit, which docks onto the carboxyl-terminal tail of the adjacent C subunit, thereby forcing the C subunit into a fully closed conformation in the absence of nucleotide. Diffusion of magnesium adenosine triphosphate (ATP) into these crystals trapped not ATP, but the reaction products, adenosine diphosphate and the phosphorylated RII¦Â subunit. This complex has implications for the dissociation-reassociation cycling of PKA. The quaternary structure of the RII¦Â tetramer differs appreciably from our model of the RI¦Á tetramer, confirming the small-angle x-ray scattering prediction that the structures of each PKA tetramer are different.
Organizational Affiliation: 
Howard Hughes Medical Institute, University of California, San Diego, La Jolla, CA 92093-0654, USA.