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@ARTICLE{Li:280468,
author = {Li, Jinyu and Flick, Franziska and Verheugd, Patricia and
Carloni, Paolo and Lüscher, Bernhard and Rossetti, Giulia},
title = {{I}nsight into the {M}echanism of {I}ntramolecular
{I}nhibition of the {C}atalytic {A}ctivity of {S}irtuin 2
({SIRT}2)},
journal = {PLoS one},
volume = {10},
number = {9},
issn = {1932-6203},
address = {Lawrence, Kan.},
publisher = {PLoS},
reportid = {FZJ-2016-00242},
pages = {e0139095 -},
year = {2015},
abstract = {Sirtuin 2 (SIRT2) is a NAD+-dependent deacetylase that has
been associated with neurodegeneration and cancer. SIRT2 is
composed of a central catalytic domain, the structure of
which has been solved, and N- and C-terminal extensions that
are thought to control SIRT2 function. However structural
information of these N- and C-terminal regions is missing.
Here, we provide the first full-length molecular models of
SIRT2 in the absence and presence of NAD+. We also predict
the structural alterations associated with phosphorylation
of SIRT2 at S331, a modification that inhibits catalytic
activity. Bioinformatics tools and molecular dynamics
simulations, complemented by in vitro deacetylation assays,
provide a consistent picture based on which the C-terminal
region of SIRT2 is suggested to function as an
autoinhibitory region. This has the capacity to partially
occlude the NAD+ binding pocket or stabilize the NAD+ in a
non-productive state. Furthermore, our simulations suggest
that the phosphorylation at S331 causes large conformational
changes in the C-terminal region that enhance the
autoinhibitory activity, consistent with our previous
findings that phosphorylation of S331 by cyclin-dependent
kinases inhibits SIRT2 catalytic activity. The molecular
insight into the role of the C-terminal region in
controlling SIRT2 function described in this study may be
useful for future design of selective inhibitors targeting
SIRT2 for therapeutic applications.},
cin = {IAS-5 / JSC / INM-9},
ddc = {500},
cid = {I:(DE-Juel1)IAS-5-20120330 / I:(DE-Juel1)JSC-20090406 /
I:(DE-Juel1)INM-9-20140121},
pnm = {511 - Computational Science and Mathematical Methods
(POF3-511) / 571 - Connectivity and Activity (POF3-571)},
pid = {G:(DE-HGF)POF3-511 / G:(DE-HGF)POF3-571},
typ = {PUB:(DE-HGF)16},
UT = {WOS:000361800700166},
pubmed = {pmid:26407304},
doi = {10.1371/journal.pone.0139095},
url = {https://juser.fz-juelich.de/record/280468},
}