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

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.

SUBMITTER: Tesmer JJ

PROVIDER: S-EPMC3073382 | biostudies-literature | 2010 Feb

REPOSITORIES: biostudies-literature

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

Tesmer John J G JJ Tesmer Valerie M VM Lodowski David T DT Steinhagen Henning H Huber Jochen J

Journal of medicinal chemistry 20100201 4

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. ...[more]

PMID: 20128603

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