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PDBsum entry 2onc
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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 alogliptin: a potent, Selective, Bioavailable, And efficacious inhibitor of dipeptidyl peptidase iv.
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Authors
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J.Feng,
Z.Zhang,
M.B.Wallace,
J.A.Stafford,
S.W.Kaldor,
D.B.Kassel,
M.Navre,
L.Shi,
R.J.Skene,
T.Asakawa,
K.Takeuchi,
R.Xu,
D.R.Webb,
S.L.Gwaltney.
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Ref.
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J Med Chem, 2007,
50,
2297-2300.
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PubMed id
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Note In the PDB file this reference is
annotated as "TO BE PUBLISHED".
The citation details given above were identified by an automated
search of PubMed on title and author
names, giving a
percentage match of
94%.
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Abstract
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Alogliptin is a potent, selective inhibitor of the serine protease dipeptidyl
peptidase IV (DPP-4). Herein, we describe the structure-based design and
optimization of alogliptin and related quinazolinone-based DPP-4 inhibitors.
Following an oral dose, these noncovalent inhibitors provide sustained reduction
of plasma DPP-4 activity and a lowering of blood glucose in animal models of
diabetes. Alogliptin is currently undergoing phase III trials in patients with
type 2 diabetes.
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