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G‐Protein–coupled receptor kinase expression in hypertension
Author(s) -
Gros Robert,
Tan Christopher M.,
Chorazyczewski Jozef,
Kelvin David J.,
Benovic Jeffrey L.,
Feldman Ross D.
Publication year - 1999
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1016/s0009-9236(99)70074-3
Subject(s) - pharmacology , chemistry , medicine
In human hypertension we have recently identified an increase in lymphocyte G‐protein receptor kinase‐2 (GRK‐2) protein expression, the key protein regulating the interaction between G‐protein–coupled receptors and activation of adenylyl cyclase. However, it was not known whether this increase in GRK‐2 protein expression was attributable to regulation at the level of translation. Furthermore, the relationship between extent of GRK‐2 expression, receptor activation of adenylyl cyclase, and blood pressure was unclear. We therefore studied lymphocytes from 7 young subjects with borderline hypertension and 14 young normotensive subjects. Immunodetectable GRK‐2 protein expression in lymphocytes from subjects with hypertension was increased (155% ± 7% of normotensive subjects; P < .05). In addition, GRK‐2 protein expression was positively correlated with blood pressure ( r = 0.53; P = .013) and inversely correlated with β‐adrenergic–mediated adenylyl cyclase activity ( r = −0.54, P = .012). However, lymphocyte GRK‐2 messenger ribonucleic acid (mRNA) content was not altered (110% ± 13% of that observed in normotensive control subjects). Increased GRK‐2 protein expression may be an important factor in the impairment of β‐adrenergic–mediated vasodilation, characteristic of the hypertensive state. Clinical Pharmacology & Therapeutics (1999) 65 , 545–551; doi: