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PDBsum entry 4wms
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References listed in PDB file
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Key reference
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Title
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A maltose-Binding protein fusion construct yields a robust crystallography platform for mcl1.
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Authors
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M.C.Clifton,
D.M.Dranow,
A.Leed,
B.Fulroth,
J.W.Fairman,
J.Abendroth,
K.A.Atkins,
E.Wallace,
D.Fan,
G.Xu,
Z.J.Ni,
D.Daniels,
J.Van drie,
G.Wei,
A.B.Burgin,
T.R.Golub,
B.K.Hubbard,
M.H.Serrano-Wu.
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Ref.
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Plos One, 2015,
10,
e0125010.
[DOI no: ]
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PubMed id
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Abstract
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Crystallization of a maltose-binding protein MCL1 fusion has yielded a robust
crystallography platform that generated the first apo MCL1 crystal structure, as
well as five ligand-bound structures. The ability to obtain fragment-bound
structures advances structure-based drug design efforts that, despite
considerable effort, had previously been intractable by crystallography. In the
ligand-independent crystal form we identify inhibitor binding modes not observed
in earlier crystallographic systems. This MBP-MCL1 construct dramatically
improves the structural understanding of well-validated MCL1 ligands, and will
likely catalyze the structure-based optimization of high affinity MCL1
inhibitors.
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