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J Med Chem. 2010 Feb 25;53(4):1867-70. doi: 10.1021/jm9017515.

Structure of human G protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol.

Author information

1
Life Sciences Institute, University of Michigan, Ann Arbor, Michigan 48109-2216, USA. johntesmer@umich.edu

Abstract

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.

PMID:
20128603
PMCID:
PMC3073382
DOI:
10.1021/jm9017515
[Indexed for MEDLINE]
Free PMC Article

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