Inhibition of the beta-adrenergic receptor kinase by polyanions.

  title={Inhibition of the beta-adrenergic receptor kinase by polyanions.},
  author={Jeffrey L. Benovic and William C. Stone and Marc G. Caron and Robert J Lefkowitz},
  journal={The Journal of biological chemistry},
  volume={264 12},
The beta-adrenergic receptor kinase, which specifically phosphorylates the agonist-occupied beta-adrenergic receptor, is strongly inhibited by polyanions. Heparin and dextran sulfate inhibit the enzyme with an IC50 of approximately 0.15 microM. De-N-sulfated heparin is approximately 8-fold less potent. Other acid mucopolysaccharides such as heparan sulfate and chondroitin sulfates B and C are also less effective. Polyaspartic and polyglutamic acid also inhibit with IC50 values of 1.3-2 microM… CONTINUE READING