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PDBsum entry 3krx
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Protein binding
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PDB id
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3krx
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Contents |
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618 a.a.
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338 a.a.
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61 a.a.
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References listed in PDB file
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Key reference
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Title
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Structure of human g protein-Coupled receptor kinase 2 in complex with the kinase inhibitor balanol.
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Authors
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J.J.Tesmer,
V.M.Tesmer,
D.T.Lodowski,
H.Steinhagen,
J.Huber.
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Ref.
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J Med Chem, 2010,
53,
1867-1870.
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PubMed id
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Abstract
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G protein-coupled receptor kinase 2 (GRK2) is a pharmaceutical target for the
treatment of cardiovascular diseases such as congestive heart failure,
myocardial infarction, and hypertension. To better understand how nanomolar
inhibition and selectivity for GRK2 might be achieved, we have determined
crystal structures of human GRK2 in complex with Gbetagamma in the presence and
absence of the AGC kinase inhibitor balanol. The selectivity of balanol among
human GRKs is assessed.
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