Londhe Priya, Gutwillig Megan, London Cheryl
Tufts University School of Medicine, Boston, MA 02111, USA.
Sackler School of Graduate Biomedical Sciences, Tufts University, Boston, MA 02111, USA.
Vet Clin North Am Small Anim Pract. 2019 Sep;49(5):917-931. doi: 10.1016/j.cvsm.2019.04.005. Epub 2019 Jun 8.
Advances in molecular biology have permitted a much more detailed understanding of cellular dysfunction at the molecular and genetic levels in cancer cells. This has resulted in the identification of novel targets for therapeutic intervention, including proteins that regulate signal transduction, gene expression, and protein turnover. In many instances, small molecules are used to disrupt the function of these targets, often through competitive inhibition of ATP binding or the prevention of necessary protein-protein interactions. More than 40 small molecule inhibitors are now approved to treat a variety of human cancers, substantially impacting patient outcomes.
分子生物学的进展使人们能够在分子和基因水平上更详细地了解癌细胞中的细胞功能障碍。这导致了新型治疗干预靶点的发现，包括调节信号转导、基因表达和蛋白质周转的蛋白质。在许多情况下，小分子被用于破坏这些靶点的功能，通常是通过竞争性抑制ATP结合或阻止必要的蛋白质-蛋白质相互作用。目前已有40多种小分子抑制剂被批准用于治疗多种人类癌症，对患者的治疗结果产生了重大影响。
