Department of Biophysics, Faculty of Basic Science, Tarbiat Modares University, Tehran, Iran.
Biopolymers. 2010;94(3):292-7. doi: 10.1002/bip.21335.
Gonadotropin releasing hormone (GnRH) has a pivotal role in the biology of reproduction processes. In extrapituitary compartments GnRH and its receptor act as a part of the autocrin regulatory system of cell proliferation, resulting in its anticancer activity. Here the anticancer activity of a new analogue of GnRH has been investigated. Results indicate that proliferation of human breast and ovarian cancer cell lines is dose-dependently inhibited. The inhibitory efficiency of this new analogue is proved to be higher than the original triptorelin. In addition to its antimitogenic activity, evidence was found for the involvement of the apoptotic mechanism in the action of the new analogue. Furthermore the presence of chemical groups in the peptide sequence is thought to increase the protease stability of the new analogue in comparison with triptorelin. Consequently our new analogue can be considered as a good pharmaceutical candidate.
促性腺激素释放激素（GnRH）在生殖过程的生物学中起着关键作用。在外分泌隔室中，GnRH 和其受体作为细胞增殖的自分泌调节系统的一部分起作用，从而具有抗癌活性。本文研究了 GnRH 的一种新类似物的抗癌活性。结果表明，人乳腺癌和卵巢癌细胞系的增殖呈剂量依赖性抑制。该新类似物的抑制效率被证明高于原始的曲普瑞林。除了抗有丝分裂活性外，还发现新类似物的作用涉及凋亡机制。此外，肽序列中的化学基团被认为增加了新类似物与曲普瑞林相比的蛋白酶稳定性。因此，我们的新类似物可以被认为是一种很好的药物候选物。
