Duggan Peter J, Tuck Kellie L
CSIRO Manufacturing, Bag 10, Clayton South, VIC 3169, Australia.
School of Chemical and Physical Sciences, Flinders University, Adelaide, SA 5042, Australia.
Toxins (Basel). 2015 Oct 16;7(10):4175-98. doi: 10.3390/toxins7104175.
Ziconotide (Prialt®), a synthetic version of the peptide ω-conotoxin MVIIA found in the venom of a fish-hunting marine cone snail Conus magnus, is one of very few drugs effective in the treatment of intractable chronic pain. However, its intrathecal mode of delivery and narrow therapeutic window cause complications for patients. This review will summarize progress in the development of small molecule, non-peptidic mimics of Conotoxins and a small number of other venom peptides. This will include a description of how some of the initially designed mimics have been modified to improve their drug-like properties.
齐考诺肽（普瑞巴林®）是从食鱼海洋锥螺（Conus magnus）毒液中发现的肽类ω-芋螺毒素MVIIA的合成版本，是极少数对治疗顽固性慢性疼痛有效的药物之一。然而，其鞘内给药方式和狭窄的治疗窗给患者带来了并发症。本综述将总结芋螺毒素和其他一些毒液肽的小分子非肽模拟物的开发进展。这将包括描述一些最初设计的模拟物是如何被修饰以改善其类药物性质的。
