Pharmacological characterization of type II glucocorticoid binding sites in AtT20 pituitary cell culture.
Recent evidence indicates that at least two functional glucocorticoid receptors (Type I and Type II) are present in many tissues. It has also become increasingly recognized that, as in other systems, stimulus-response relationships for steroid hormones are often nonlinear. Thus, precise pharmacological parameters are required to establish a functional relationship(s) between binding site and response characteristics. We therefore pharmacologically characterized a glucocorticoid binding site present in AtT20 mouse pituitary cells, a cell line extensively used in studying Type II glucocorticoid receptor function. By several different criteria, glucocorticoids were shown to bind to a single class of binding sites, which, in comparison to available literature, correspond to classical Type II glucocorticoid receptors. No evidence for Type I adrenal steroid binding sites was observed, under the experimental conditions used. Unambiguous Kb values for both glucocorticoid agonists and antagonists were therefore calculated. These parameters should prove of use in elucidating the relationships between glucocorticoid receptor activation and different responses in both AtT20 cells and other glucocorticoid responsive tissues.
Gannon
M N
MN
Department of Neuroendocrinology, Rockefeller University, New York, NY 10021.
Spencer
R L
RL
Lundblad
J R
JR
McEwen
B S
BS
Roberts
J L
JL
D000818:Animals; D001667:Binding, Competitive; D002460:Cell Line; D003600:Cytosol / Q000187:drug effects / Q000378:metabolism; D003907:Dexamethasone / Q000494:pharmacology; D005938:Glucocorticoids / Q000378:metabolism*; D051379:Mice; D010902:Pituitary Gland / Q000187:drug effects / Q000378:metabolism*; D011965:Receptors, Glucocorticoid / Q000378:metabolism*
D005938:Glucocorticoids; D011965:Receptors, Glucocorticoid; D003907:Dexamethasone