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PDBsum entry 3c49
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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 inhibitor specificity in human poly(ADP-Ribose) polymerase-3.
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Authors
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L.Lehtiö,
A.S.Jemth,
R.Collins,
O.Loseva,
A.Johansson,
N.Markova,
M.Hammarström,
A.Flores,
L.Holmberg-Schiavone,
J.Weigelt,
T.Helleday,
H.Schüler,
T.Karlberg.
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Ref.
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J Med Chem, 2009,
52,
3108-3111.
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PubMed id
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Abstract
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Poly(ADP-ribose) polymerases (PARPs) activate DNA repair mechanisms upon stress-
and cytotoxin-induced DNA damage, and inhibition of PARP activity is a lead in
cancer drug therapy. We present a structural and functional analysis of the PARP
domain of human PARP-3 in complex with several inhibitors. Of these, KU0058948
is the strongest inhibitor of PARP-3 activity. The presented crystal structures
highlight key features for potent inhibitor binding and suggest routes for
creating isoenzyme-specific PARP inhibitors.
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