Covalent linking of photoreactive gonadotropin-releasing hormone to gonadotropes produces a prolonged signal.
A bioactive, photoreactive derivative of gonadotropin-releasing hormone (GnRH; gonadoliberin), [azidobenzoyl-D-Lys6]GnRH, was shown to bind covalently to dispersed pituitary cells after irradiation. Approximately 7% of the total cell-associated radioactivity was covalently bound to the receptors. Photolysis of cultured pituitary cells in the presence of the photoreactive derivative resulted in persistent activation of luteinizing hormone (LH; lutropin) release. This persistent response was time dependent and concentration dependent. No increase in the basal rate of LH release was observed with cells incubated in the presence of photoreactive GnRH analog and maintained in the dark or with hormone derivatives that lack the photoreactive azido group. These results suggest that only the covalently bound cell surface receptors account for the persistent activation of LH release after photolysis.
D000345:Affinity Labels; D000818:Animals; D004305:Dose-Response Relationship, Drug; D005260:Female; D007987:Gonadotropin-Releasing Hormone / Q000031:analogs & derivatives*; D006728:Hormones; D007700:Kinetics; D007986:Luteinizing Hormone / Q000378:metabolism; D010782:Photolysis; D010902:Pituitary Gland / Q000378:metabolism*; D051381:Rats; D011956:Receptors, Cell Surface / Q000378:metabolism*; D011966:Receptors, LHRH
D000345:Affinity Labels; D006728:Hormones; D011956:Receptors, Cell Surface; D011966:Receptors, LHRH; D007987:Gonadotropin-Releasing Hormone; D007986:Luteinizing Hormone