I Mezô, J Seprôdi, B Vincze, I Pályi, G Kéri, Z Vadász, G Tóth, M Kovács, M Koppán, J E Horváth, A Kálnay, I Teplán
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引用次数: 0
摘要
已经合成了新的鸡I型GnRH激动剂和拮抗剂，并对其生物活性进行了测试。这些类似物的共同特征是分子在6号位置插入了- l -天冬氨酸残基。与垂体结合的激动剂仍具有较低的内分泌活性。另一方面，在体外实验中显示出直接的抗肿瘤作用。拮抗剂的内分泌活性较低;然而，它显示出有效的、直接的抗肿瘤活性。这些观察结果可能导致具有选择性抗肿瘤作用的新的GnRH类似物的发展。
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.
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