NIBR GDC and Oncology, Novartis Pharma AG, CH4002 Basel, Switzerland.
Future Med Chem. 2009 Apr;1(1):137-55. doi: 10.4155/fmc.09.5.
Among promising targeted therapies for cancer treatment, phosphatidylinositol 3-kinase pathway inhibitors have in the last 3 years continued to retain the attention of both academic institutions and pharmaceutical companies. The large amount of published clinical and preclinical data has indeed confirmed the preponderant role of this so-called survival pathway for tumor maintenance.
Global efforts have, therefore, been deployed that have led to the genesis of a panoply of small molecule inhibitors. This review will focus on updating the reader on the current medicinal chemistry efforts targeting this pathway.
Recent discoveries important for patient stratification, quantification of target modulation in humans and combination therapies will be presented and discussed.
在癌症治疗有前景的靶向治疗中，磷脂酰肌醇 3-激酶途径抑制剂在过去 3 年中一直受到学术机构和制药公司的关注。大量已发表的临床前和临床数据确实证实了这种所谓的肿瘤维持生存途径的主导作用。
因此，全球都在努力，从而产生了一系列的小分子抑制剂。这篇综述将重点介绍针对该途径的当前药物化学研究进展。
将介绍和讨论最近对患者分层、人类目标调节量化和联合治疗有重要意义的发现。
