芳香化酶抑制剂筛选模型的研究进展

Progress of research on the screening models of aromatase inhibitors

芳香化酶是生物体催化雄性激素转变为雌性激素的限速酶,以其为靶点筛选芳香化酶抑制剂,在雌激素受体阳性乳腺癌患者的治疗中具有重要地位。本文综述了芳香化酶抑制剂筛选模型的研究进展,讨论后发现,现有的各筛选模型优劣共存,通过深入研究,可建立新型的高通量筛选模型,发展前景广阔。

OBJECTIVE Aromatase,a cytochrome P450 enzyme,catalyzed the rate-limiting aromatization step for the conversion of androgens to estrogen.It＇s an effective target for inhibition of estrogen biosynthesis in treatment of hormone-sensitive breast cancer.In this review,the advances of screening models of aromatase inhibitors were comprehensively introduced.In the discussion,it was discovered that both advantages and disadvantages were existed in each screening model of aromatase inhibitors,with continued in-depth study,there will be more broad prospects of development.