Pfizer Animal Health, Pfizer Inc, 7000 Portage Road, Kalamazoo, MI, 49009, USA.
Adv Exp Med Biol. 2010;692:1-9. doi: 10.1007/978-1-4419-6902-6_1.
Drug discovery is an iterative process with high risks and low chance of success. New genomics technologies allow veterinary medicine and agrochemical companies to validate and functionally screen new receptor-based targets, including neuropeptide G-protein coupled receptors, which were previously not amenable to high throughput screening. However this is just the first step in a long process to translate a mechanistic assay hit into a drug on the market. In addition to effectively eradicating pests on crops and parasites on their host, the molecules must also be safe, cheap to synthesise, formulatable and patentable. This is a costly process in which early attrition of unsuitable molecules is key to any successful program. Although first principle discovery is risky the ultimate benefits are considerable and future genomics resources will help to generate higher quality hits to strengthen the discovery pipeline.
药物发现是一个具有高风险和低成功率的迭代过程。新的基因组学技术使兽医和农化公司能够验证和功能筛选新的基于受体的靶标,包括以前不能进行高通量筛选的神经肽 G 蛋白偶联受体。然而,这只是将一种基于机制的测定命中物转化为市场上的药物的漫长过程的第一步。除了有效地消灭作物上的害虫和其宿主上的寄生虫外,这些分子还必须安全、廉价合成、可配方和可专利。这是一个昂贵的过程,其中不合适的分子的早期淘汰是任何成功项目的关键。虽然基于原理的发现具有风险,但最终的收益是相当可观的,未来的基因组学资源将有助于产生更高质量的命中物,以加强发现管道。