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J. Biol. Chem., Vol. 264, Issue 12, 6707-6710, Apr, 1989
JL Benovic, WC Stone, MG Caron and RJ Lefkowitz
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. Inositol
hexasulfate, with an IC50 of 13 microM is approximately 270-fold more
potent than inositol hexaphosphate implicating the sulfate group as a major
determinant of the inhibition. The inhibition by heparin is competitive
with substrate and of mixed type with respect to ATP. Polycations also
inhibit receptor phosphorylation by beta-adrenergic receptor kinase.
Polylysine is more effective with an IC50 of 69 microM, while spermine (990
microM) and spermidine (2570 microM) are less potent. Polylysine, spermine,
and spermidine are also able to block effectively the inhibition by
heparin. The identification of compounds which specifically inhibit
beta-adrenergic receptor kinase should prove useful in further defining the
biological role of this enzyme.
Inhibition of the beta-adrenergic receptor kinase by polyanions
Department of Medicine, Howard Hughes Medical Institute, Duke University Medical Center, Durham, North Carolina 27710.
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