Legarza Kathleen, Yang Li-Xi
Radiobiology Laboratory, Integrated Radiation Oncology Graduate Medical Education Program, Department of Radiation Oncology, California Pacific Medical Center Research Institute, San Francisco, CA 94118, USA.
Anticancer Res. 2006 Sep-Oct;26(5A):3301-5.
Camptothecin (CPT) derivatives have emerged as a promising group of chemotherapeutic agents. The FDA has approved the CPT derivatives topotecan and irinotecan for second line treatment of ovarian cancer and metastatic colorectal cancer, respectively. These and other CPT derivatives have become part of the multi-million dollar industry that is dedicated to finding better chemotherapeutic agents with excellent tumor kill and less normal tissue toxicity. In order to reach this goal it is imperative to understand the details of the mechanisms of action and the targets of these drugs, as well as the cellular response to the drugs. Although investigations of CPT date back to the 1960's, most of the studies that have been added to our present knowledge were done in the last 10 years. The purpose of this paper is to review the latest insights into the CPT binding site, CPT-induced gene expression and CPT-induced pathways to apoptosis.
喜树碱（CPT）衍生物已成为一类很有前景的化疗药物。美国食品药品监督管理局（FDA）已分别批准CPT衍生物拓扑替康和伊立替康用于卵巢癌和转移性结直肠癌的二线治疗。这些以及其他CPT衍生物已成为价值数百万美元产业的一部分，该产业致力于寻找具有出色肿瘤杀伤效果且对正常组织毒性较小的更好化疗药物。为了实现这一目标，必须了解这些药物的作用机制细节、靶点以及细胞对药物的反应。尽管对CPT的研究可追溯到20世纪60年代，但大多数为我们当前知识所增添的研究是在过去10年完成的。本文的目的是综述对CPT结合位点、CPT诱导的基因表达以及CPT诱导的凋亡途径的最新见解。
