Marton L J, Pegg A E
Department of Pathology, University of Wisconsin Medical School, Madison 53706, USA.
Annu Rev Pharmacol Toxicol. 1995;35:55-91. doi: 10.1146/annurev.pa.35.040195.000415.
Polyamines are ubiquitous cell components essential for normal growth. Compounds interfering with polyamine biosynthesis or function have considerable potential for use as therapeutic agents. Inhibitors of ornithine decarboxylase have been shown to be valuable for the treatment of diseases caused by parasitic protozoa, most notably African sleeping sickness. They may also be useful chemopreventive and antineoplastic agents. Inhibitors of S-adenosylmethionine decarboxylase also have potential as treatments of these diseases. Protocols minimizing uptake of exogenous polyamines via the polyamine-transport system will probably be needed for the full potential of the inhibitors to be realized. Polyamine analogues, notably those with ethyl or benzyl groups on the terminal nitrogen atoms, have potent antiproliferative activity and are promising agents for the treatment of cancer. These analogues are transported by the polyamine-transport system, and their therapeutic effects are less likely to be blocked by the availability of the exogenous polyamines.
多胺是正常生长所必需的普遍存在的细胞成分。干扰多胺生物合成或功能的化合物具有作为治疗剂的巨大潜力。鸟氨酸脱羧酶抑制剂已被证明对治疗由寄生原生动物引起的疾病有价值，最显著的是非洲昏睡病。它们也可能是有用的化学预防剂和抗肿瘤剂。S-腺苷甲硫氨酸脱羧酶抑制剂也有作为这些疾病治疗方法的潜力。为了充分发挥抑制剂的潜力，可能需要尽量减少通过多胺转运系统摄取外源性多胺的方案。多胺类似物，特别是那些在末端氮原子上带有乙基或苄基的类似物，具有强大的抗增殖活性，是治疗癌症的有前景的药物。这些类似物通过多胺转运系统运输，其治疗效果不太可能被外源性多胺的可用性所阻断。
