Molecular mechanism for inhibition of g protein-coupled receptor kinase 2 by a selective RNA aptamer.

@article{Tesmer2012MolecularMF,
  title={Molecular mechanism for inhibition of g protein-coupled receptor kinase 2 by a selective RNA aptamer.},
  author={Valerie M. Tesmer and Sabine Lennarz and G{\"u}nter Mayer and John J G Tesmer},
  journal={Structure},
  year={2012},
  volume={20 8},
  pages={
          1300-9
        }
}
Cardiovascular homeostasis is maintained in part by the rapid desensitization of activated heptahelical receptors that have been phosphorylated by G protein-coupled receptor kinase 2 (GRK2). However, during chronic heart failure GRK2 is upregulated and believed to contribute to disease progression. We have determined crystallographic structures of GRK2 bound to an RNA aptamer that potently and selectively inhibits kinase activity. Key to the mechanism of inhibition is the positioning of an… CONTINUE READING
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