Department of Psychiatry, University of Toronto, Toronto, ON, Canada.
Molecules. 2010 Nov 15;15(11):8260-78. doi: 10.3390/molecules15118260.
Imaging protein kinase expression with radiolabeled small molecule inhibitors has been actively pursued to monitor the clinical potential of targeted therapeutics and treatments as well as to determine kinase receptor density changes related to disease progression. The goal of the present review is to provide an overview of the breadth of radiolabeled small molecules that have been synthesized to target intracellular protein kinases, not only for imaging in oncology, but also for other areas of interest, particularly the central nervous system. Considerable radiotracer development has focused on imaging receptor tyrosine kinases of growth factors, protein kinases A, B and C, and glycogen synthase kinase-3ß. Design considerations, structural attributes and relevant biological results are summarized.
用放射性标记的小分子抑制剂来成像蛋白激酶的表达一直受到积极的研究，以监测靶向治疗和治疗的临床潜力，以及确定与疾病进展相关的激酶受体密度变化。本综述的目的是提供一个广泛的综述，介绍了为靶向细胞内蛋白激酶而合成的放射性标记小分子，不仅用于肿瘤学成像，还用于其他感兴趣的领域，特别是中枢神经系统。大量的放射性示踪剂开发集中在成像生长因子的受体酪氨酸激酶、蛋白激酶 A、B 和 C 以及糖原合酶激酶-3β。总结了设计考虑因素、结构属性和相关的生物学结果。
