Research Group SynBioC, Department of Green Chemistry and Technology, Faculty of Bioscience Engineering, Universiteit Gent, Coupure Links 653, 9000 Gent, Belgium.
Cancer Research Institute Ghent (CRIG), Corneel Heymanslaan 10, 9000 Gent, Belgium.
J Med Chem. 2021 Jun 10;64(11):7179-7188. doi: 10.1021/acs.jmedchem.1c00294. Epub 2021 May 20.
Over the past decades, therapeutics based on biological macromolecules and cells have successfully entered the clinical arena and progressively occupied an increasing share of what once was almost exclusively small molecule territory. This perspective explores the opportunities for chemists at the interface between biologics and small molecule-based products. It provides concrete examples by zooming in on the area of post-translational protein modification. The conclusion is that, rather than diminishing the relevance of chemistry in the pharmaceutical enterprise, the advent of the biologics has provided an additional playing field for synthetic and medicinal chemists, where they can contribute to the efficacy and scope of applicability of biological entities in a collaborative effort to transformatively address unmet medical needs.
在过去几十年中，基于生物大分子和细胞的治疗方法已经成功进入临床领域，并逐渐占据了曾经几乎完全由小分子占据的市场份额。本文探讨了处于生物制品和基于小分子产品交叉点的化学家的机会。通过聚焦于翻译后蛋白质修饰领域，提供了具体的例子。结论是，生物制品的出现并没有降低化学在制药企业中的相关性，而是为合成和药物化学家提供了一个额外的领域，他们可以在合作中为生物实体的疗效和适用范围做出贡献，从而改变解决未满足的医疗需求。
