Trim Steven A, Trim Carol M
Venomtech Ltd, Kent Enterprise Hub, University of Kent, Canterbury, UK.
Br J Pain. 2013 Nov;7(4):179-88. doi: 10.1177/2049463713502005.
Adequate pain control is still a significant challenge and largely unmet medical need in the 21st century. With many small molecules failing to reach required levels of potency and selectivity, drug discovery is once again turning to nature to replenish pain therapeutic pipelines. Venomous animals are frequently stereotyped as inflictors of pain and distress and have historically been vilified by mankind. Yet, ironically, the very venoms that cause pain when directly injected by the host animal may actually turn out to contain the next generation of analgesics when injected by the clinician. The last 12 months have seen dramatic discoveries of analgesic tools within venoms. Spiders, snakes and even centipedes are yielding peptides with immense therapeutic potential. Significant advances are also taking place in delivery methods that can improve bioavailability and pharmacokinetics of these exciting natural resources. Turning proteinaceous venom into pharmaceutical liquid gold is the goal of venomics and the focus of this article.
在21世纪，充分的疼痛控制仍然是一项重大挑战，也是尚未得到满足的主要医疗需求。由于许多小分子无法达到所需的效力和选择性水平，药物研发再次将目光投向自然界，以充实疼痛治疗药物的研发渠道。有毒动物常常被刻板地视为疼痛和痛苦的施加者，历史上一直遭到人类的诋毁。然而，具有讽刺意味的是，宿主动物直接注射时会引起疼痛的毒液，当由临床医生注射时，实际上可能含有下一代镇痛药。在过去12个月里，人们在毒液中发现了具有显著镇痛作用的物质。蜘蛛、蛇甚至蜈蚣都能产生具有巨大治疗潜力的肽。在改善这些令人兴奋的天然资源的生物利用度和药代动力学的给药方法方面也取得了重大进展。将蛋白质类毒液转化为药用“液体黄金”是毒液组学的目标，也是本文的重点。
