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PDBsum entry 2qr7
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References listed in PDB file
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Key reference
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Title
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Structural basis for activation of the autoinhibitory c-Terminal kinase domain of p90 rsk2.
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Authors
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M.Malakhova,
V.Tereshko,
S.Y.Lee,
K.Yao,
Y.Y.Cho,
A.Bode,
Z.Dong.
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Ref.
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Nat Struct Mol Biol, 2008,
15,
112-113.
[DOI no: ]
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PubMed id
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Abstract
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The X-ray structure at 2.0-A resolution of the p90 ribosomal S6 kinase 2
C-terminal kinase domain revealed a C-terminal autoinhibitory alphaL-helix that
was embedded in the kinase scaffold and determines the inactive kinase
conformation. We suggest a mechanism of activation through displacement of the
alphaL-helix and rearrangement of the conserved residue Glu500, as well as the
reorganization of the T-loop into the active conformation.
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Figure 1.
The autoinhibitory C-terminal  L-helix
is shown in yellow. (a) The folding diagram. Disordered residues
715–740 are indicated in gray. (b) The 'cradle' position of
the L-helix
on the potential surface (positive in blue, negative in red).
See Supplementary Methods and Supplementary Table 1 online for
details of the structure determination and crystallographic
statistics, respectively. The sequence alignment is shown in
Supplementary Figure 4 online.
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Figure 2.
(a) The CTD superimposed on active PKA (chain A from PDB
1CDK) illustrates the different positions of the D-helix.
Boxed region corresponds to boxed region in c. The ligand
(inhibitory peptide, purple ribbon) and an ATP analog (AMP-PNP;
blue van der Waals surface representation) bound to PKA are
included. (b) The CTD RSK2 superimposed on the autoinhibited
Ca^2+/calmodulin-dependent protein kinase I (PDB 1A06). (c) A
comparison of the active sites of CTD and PKA. Selected RSK2 CTD
residues are shown. Only residue Glu127 (analogous to Glu500 in
the CTD structure), which differs in the two structures, is
shown for PKA. The ATP analog and Mg^2+ ions (balls) are shown
in blue.
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The above figures are
reprinted
by permission from Macmillan Publishers Ltd:
Nat Struct Mol Biol
(2008,
15,
112-113)
copyright 2008.
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