Raab-Westphal Sabine, Marshall John F, Goodman Simon L
Translational In Vivo Pharmacology, Translational Innovation Platform Oncology, Merck KGaA, Frankfurter Str. 250, 64293 Darmstadt, Germany.
Barts Cancer Institute, Queen Mary University of London, Charterhouse Square, London EC1M 6BQ, UK.
Cancers (Basel). 2017 Aug 23;9(9):110. doi: 10.3390/cancers9090110.
Integrins are transmembrane receptors that are central to the biology of many human pathologies. Classically mediating cell-extracellular matrix and cell-cell interaction, and with an emerging role as local activators of TGFβ, they influence cancer, fibrosis, thrombosis and inflammation. Their ligand binding and some regulatory sites are extracellular and sensitive to pharmacological intervention, as proven by the clinical success of seven drugs targeting them. The six drugs on the market in 2016 generated revenues of some US$3.5 billion, mainly from inhibitors of α4-series integrins. In this review we examine the current developments in integrin therapeutics, especially in cancer, and comment on the health economic implications of these developments.
整合素是跨膜受体，在许多人类疾病生物学中起着核心作用。传统上介导细胞与细胞外基质以及细胞间的相互作用，并且作为转化生长因子β（TGFβ）的局部激活剂发挥新出现的作用，它们影响癌症、纤维化、血栓形成和炎症。其配体结合位点和一些调节位点位于细胞外，对药物干预敏感，这已被七种靶向它们的药物的临床成功所证明。2016年市场上的六种药物创造了约35亿美元的收入，主要来自α4系列整合素抑制剂。在本综述中，我们研究了整合素治疗学的当前进展，尤其是在癌症方面，并对这些进展的健康经济影响进行评论。
