科研之友
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摘要
Topoisomerase I (TOPI) is a nuclear enzyme found in all eukaryotic cells that is responsible for coiling and uncoiling DNA to allow transcription and replication. Because cancer cells have an increased rate of transcription, translation and replication, they are susceptible to TOPI inhibition. Camptothecin (CPT) was the first TOPI inhibitor to be identified, but poor solubility and toxicity limited its use. Topotecan and irinotecan are FDA-approved CPT analogues that are used in the treatment of colon, cervical, ovarian and small cell lung cancers. A number of new CPT and non-CPT TOPI inhibitors are being developed to decrease side effects, increase target specificity and ultimately, increase efficacy. In this review, we will discuss new CPT and non-CPT TOPI-inhibiting analogues, as well as nanotechnology-based modifications to TOPI inhibitors intended to improve drug delivery.
- 出版日期2016-12
