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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | Sheppard, J. R. |
| Abstract | Identification and characterization of hormone receptors on the cell surface is an effective tool for studying the plasma membrane. Using the direct binding of a radiolabeled antagonist, (-)[3H]alprenolol, to crude membrane preparations, and a physiological response (cellular cyclic AMP levels), I demonstrated a catecholamine (beta-adrenergic) hormone receptor site coupled to a catecholamine responsive adenylate cyclase [ATP pyrophosphate-lyase (cyclizing), EC 4.6.1.1] on 3T3 and simian virus 40 (SV40)-transformed 3T3 cells. At a concentration of 1 muM, epinephrine and isoproterenol elevate cellular cyclic AMP levels 8- and 12-fold, respectively, in both cell lines. Norepinephrine was also a potent agonist on 3T3 cells (8-fold stimulation), but SV3T3 cells showed a lesser (2-fold) response to this hormone. The specificity of the physiological response (as well as the direct binding studies using the alprenolol radiolabel) is indicated by the increased effectiveness of (-) compared to (+) stereoisomers, rapid and reversible kinetics (steady state within 2 min), high affinity (Kd approximately 30 nM) and saturability (indicating a finite number of hormone receptors). These hormone receptor studies indicate the 3T3 cells have a beta1 adrenergic receptor while the SV3T3 cells have a receptor with beta2 qualities. In addition, the number of beta-adrenergic hormone receptors appear to be increased in the normal 3T3 cells by approximately 2-fold over the SV3T3 cells (300 versus versus 120 femtomol/mg of protein). |
| ISSN | 00278424 |
| e-ISSN | 10916490 |
| Journal | Proceedings of the National Academy of Sciences of the United States of America |
| Issue Number | 3 |
| Volume Number | 74 |
| Language | English |
| Publisher | National Academy of Sciences |
| Publisher Date | 1977-05-01 |
| Publisher Place | United States |
| Access Restriction | Open |
| Subject Keyword | Adenylate Cyclase Metabolism Cell Transformation, Neoplastic Receptors, Adrenergic, Beta Receptors, Adrenergic Adrenergic Beta-Agonists Pharmacology Alprenolol Cell Line Cell Membrane Kinetics Simian Virus 40 Stereoisomerism Research Support, U.S. Gov't, P.H.S. Multidisciplinary |
| Content Type | Text |
| Resource Type | Article |
| Subject | Multidisciplinary |
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