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PDBsum entry 4ykn
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Transferase/transferase inhibitor
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PDB id
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4ykn
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References listed in PDB file
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Key reference
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Title
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Discovery of a potent class of pi3kα inhibitors with unique binding mode via encoded library technology (elt).
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Authors
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H.Yang,
P.F.Medeiros,
K.Raha,
P.Elkins,
K.E.Lind,
R.Lehr,
N.D.Adams,
J.L.Burgess,
S.J.Schmidt,
S.D.Knight,
K.R.Auger,
M.D.Schaber,
G.J.Franklin,
Y.Ding,
J.L.Delorey,
P.A.Centrella,
S.Mataruse,
S.R.Skinner,
M.A.Clark,
J.W.Cuozzo,
G.Evindar.
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Ref.
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Acs Med Chem Lett, 2015,
6,
531-536.
[DOI no: ]
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PubMed id
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Abstract
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In the search of PI3K p110α wild type and H1047R mutant selective small
molecule leads, an encoded library technology (ELT) campaign against the desired
target proteins was performed which led to the discovery of a selective
chemotype for PI3K isoforms from a three-cycle DNA encoded library. An X-ray
crystal structure of a representative inhibitor from this chemotype demonstrated
a unique binding mode in the p110α protein.
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Secondary reference #1
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Title
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Baculovirus production of fully-Active phosphoinositide 3-Kinase alpha as a p85alpha-P110alpha fusion for X-Ray crystallographic analysis with ATP competitive enzyme inhibitors.
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Authors
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R.H.Sinnamon,
P.Mcdevitt,
B.L.Pietrak,
V.R.Leydon,
Y.Xue,
R.Lehr,
H.Qi,
M.Burns,
P.Elkins,
P.Ward,
G.Vincentini,
D.Fisher,
M.Grimes,
M.Brandt,
K.R.Auger,
T.Ho,
K.Johanson,
C.S.Jones,
B.Schwartz,
T.D.Sweitzer,
R.B.Kirkpatrick.
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Ref.
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Protein Expr Purif, 2010,
73,
167-176.
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PubMed id
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