Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 53, Issue 4, Pages 1867-1870Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm9017515
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Funding
- Michigan Economic Development Corporation
- Michigan Technology Tri-Corridor [085P1000817]
- U.S. Department of Energy, Office of Science, Office of Basic Energy Sciences [DE-AC02-06CH11357]
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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 G beta gamma in the presence and absence of the AGC kinase inhibitor balanol. The selectivity of balanol among human GRKs is assessed.
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