Owen Caroline P
Department of Pharmacy, School of Pharmacy and Chemistry, Kingston University, Penrhyn Road, Kingston upon Thames, Surrey KT12EE, UK.
Anticancer Agents Med Chem. 2009 Jul;9(6):613-26. doi: 10.2174/187152009788680046.
Prostate cancer is an age-related disease and a major cause of death in Western countries. A large proportion of prostate cancers have been found to be dependent on androgens for growth and various therapeutic approaches have aimed at either decreasing androgen levels or blocking their action. One method of decreasing androgen levels is through inhibition of enzymes involved in the biosynthetic pathway, for example, the P450 enzyme complex 17alpha-hydroxylase/C17,20-lyase (P450(17alpha)), which catalyses the conversion of pregnenolone and progesterone into the androgen precursors dehydroepiandrosterone and androstenedione respectively. A number of researchers have targeted this enzyme and have produced potent steroidal and non-steroidal inhibitors. This review looks at the various inhibitors that have been developed, focussing mainly on more recent inhibitors reported over the last ten years. Some mention is also given to structural requirements suggested to be important for potent activity.
前列腺癌是一种与年龄相关的疾病，也是西方国家主要的死亡原因之一。已发现很大一部分前列腺癌依赖雄激素生长，各种治疗方法旨在降低雄激素水平或阻断其作用。降低雄激素水平的一种方法是抑制参与生物合成途径的酶，例如，细胞色素P450酶复合物17α-羟化酶/C17,20-裂解酶（P450(17α)），它催化孕烯醇酮和孕酮分别转化为雄激素前体脱氢表雄酮和雄烯二酮。许多研究人员已将这种酶作为靶点，并开发出了强效的甾体和非甾体抑制剂。本综述探讨了已开发的各种抑制剂，主要关注过去十年报道的最新抑制剂。还提及了对强效活性很重要的结构要求。
