Cloning, sequencing, and expression of human gonadotropin releasing hormone (GnRH) receptor.
Gonadotropin releasing hormone is a hypothalamic decapeptide that stimulates the release of gonadotropic hormones from the anterior pituitary gland. Therapeutically, the human pituitary GnRH receptor is the target of agonists used in the suppression of prostate cancer. Here we report the isolation of a cDNA representing this receptor. It encodes a protein with a transmembrane topology similar with that of other G protein-coupled, 7-transmembrane receptors. Binding studies of the cloned receptor demonstrate high affinity and pharmacological properties similar with the native human pituitary GnRH receptor. Northern blot and reverse transcriptase/PCR analysis revealed that its mRNA is expressed in pituitary, ovary, testis, breast, and prostate but not in liver and spleen. Availability of a human GnRH receptor cDNA should permit the design of improved analogs for therapeutic applications.
Kakar
S S
SS
Department of Physiology and Biophysics, University of Alabama, Birmingham 35294.
Musgrove
L C
LC
Devor
D C
DC
Sellers
J C
JC
Neill
J D
JD
D000595:Amino Acid Sequence; D000818:Animals; D001483:Base Sequence; D002118:Calcium / Q000378:metabolism; D002460:Cell Line; D002462:Cell Membrane / Q000378:metabolism; D003001:Cloning, Molecular / Q000379:methods; D005260:Female; D015870:Gene Expression; D015723:Gene Library; D007987:Gonadotropin-Releasing Hormone / Q000031:analogs & derivatives / Q000494:pharmacology; D006801:Humans; D007700:Kinetics; D008297:Male; D008969:Molecular Sequence Data; D009928:Organ Specificity; D010903:Pituitary Gland, Anterior / Q000378:metabolism*; D016133:Polymerase Chain Reaction / Q000379:methods; D011487:Protein Conformation; D012333:RNA, Messenger / Q000378:metabolism*; D011966:Receptors, LHRH / Q000235:genetics* / Q000378:metabolism*; D011994:Recombinant Proteins / Q000378:metabolism; D014162:Transfection; D017329:Triptorelin Pamoate / Q000031:analogs & derivatives*
D012333:RNA, Messenger; D011966:Receptors, LHRH; D011994:Recombinant Proteins; D017329:Triptorelin Pamoate; D007987:Gonadotropin-Releasing Hormone; C019176:Tryptal; D002118:Calcium