Synthesis of GnRH analogs having direct antitumor and low LH-releasing activity.
New chicken I GnRH agonists and antagonists have been synthesized and tested for their biological activities. The common feature of these analogs was that the molecules had a beta-L-aspartyl residue inserted in position 6. The agonist bound to the pituitary still had low endocrinological activity. On the other hand, it exhibited direct antitumor effect in in vitro assays. The endocrinological activity of the antagonist was low; however, it showed potent, direct antitumor activity. These observations might lead to the development of new GnRH analogs with selective antitumor effect.
Mezô
I
I
Semmelweis University of Medicine, 1st Department of Biochemistry, Budapest, Hungary.
Seprôdi
J
J
Vincze
B
B
Pályi
I
I
Kéri
G
G
Vadász
Z
Z
Tóth
G
G
Kovács
M
M
Koppán
M
M
Horváth
J E
JE
Kálnay
A
A
Teplán
I
I
D000818:Animals; D018931:Antineoplastic Agents, Hormonal / Q000138:chemical synthesis* / Q000494:pharmacology; D002645:Chickens; D015195:Drug Design; D005260:Female; D007987:Gonadotropin-Releasing Hormone / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology*; D006728:Hormones / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D007986:Luteinizing Hormone / Q000378:metabolism*; D008958:Models, Molecular; D010902:Pituitary Gland / Q000187:drug effects / Q000378:metabolism; D051381:Rats; D017208:Rats, Wistar; D014407:Tumor Cells, Cultured
C108847:(beta-Asp(alpha-DEA))(6),Gln(8)-GnRH; D018931:Antineoplastic Agents, Hormonal; D006728:Hormones; C100780:MI 1892; D007987:Gonadotropin-Releasing Hormone; D007986:Luteinizing Hormone