Heparin-mediated inactivation and transformation of mammary cytoplasmic glucocorticoid receptor.

Glucocorticoid receptor of lactating mouse mammary gland cytosol was exposed to heparin when the receptor was either steroid-free or steroid-bound. Heparin caused a dose-dependent and time-dependent loss of steroid binding activity (inactivation) of the steroid-free receptor; this heparin-induced inactivation was inhibited by molybdate. In contrast, steroid-bound receptor maintained its steroid binding capacity in the presence of heparin but the heparin caused transformation of receptor as detected by increased binding to DNA-cellulose and ATP-Sepharose. Heparin also converted steroid-bound receptor from the 7-8S form to the 4S form. Molybdate inhibited both the heparin-induced transformation and associated conversion to the 4S form.