Ward Stephen G, Finan Peter
Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath BA2 7AY, UK.
Curr Opin Pharmacol. 2003 Aug;3(4):426-34. doi: 10.1016/s1471-4892(03)00078-x.
The phosphoinositide 3-kinase (PI3K) family of enzymes consists of several closely related isoforms that are thought to have distinct biological roles. Until now, researchers have been frustrated by poor selectivity of the available pharmacological inhibitors, which are unable to distinguish adequately the activities of different PI3K isoforms. Recently published patent specifications describe new PI3K inhibitors, including several that are selective for the PI3Kdelta isoform. There is now cautious optimism that isoform-selective PI3K inhibitors will provide new avenues for therapeutic applications in a range of diseases.
磷酸肌醇3激酶（PI3K）家族的酶由几种密切相关的亚型组成，这些亚型被认为具有不同的生物学作用。到目前为止，研究人员一直因现有药理抑制剂的选择性不佳而感到沮丧，这些抑制剂无法充分区分不同PI3K亚型的活性。最近公布的专利说明书描述了新的PI3K抑制剂，包括几种对PI3Kδ亚型具有选择性的抑制剂。目前人们持谨慎乐观态度，认为亚型选择性PI3K抑制剂将为一系列疾病的治疗应用提供新途径。
