Ciba-Geigy award for outstanding research. Regulation of adrenergic receptor function by phosphorylation.

ABSTRACT

The various subtypes of adrenergic receptors represent distinct structural entities which are coupled in different ways to two major transmembrane signalling systems, the adenylate cyclase and phosphatidyl-inositol pathways. Recent evidence suggests that the functional linkage of both beta and alpha 1-adrenergic receptors to their respective effector systems is regulated by covalent modification of the receptors by phosphorylation-dephosphorylation reactions. Receptor phosphorylation appears to lead to desensitization of the biological response to receptor stimulation. Several kinases including protein kinase A, protein kinase C and a cAMP independent kinase appear to participate in these reactions.