Katzenellenbogen J A
Department of Chemistry, University of Illinois, Urbana 61801, USA.
J Nucl Med. 1995 Jun;36(6 Suppl):8S-13S.
Imaging of breast or prostate cancers based on their content of steroid receptors poses a major challenge in the design of radiotracers. Receptors for steroid hormones are proteins that interact at specific sites in chromatin. Several analogs of estrogens, progestins and androgens have been radiolabeled and evaluated both in vitro and in vivo for receptor binding affinity and selectivity. Breast tumors in patients have been imaged with [18F]fluoroestradiol. Scintigraphic images with radiolabeled progestin analogs may be useful for monitoring the efficacy of tamoxifen treatment in breast cancer patients. Tissue distribution and imaging studies in animals with fluorine-substituted androgens indicate that it may be possible to develop a steroid receptor-based radiotracer for staging prostate cancer. Radiochemists are reporting some progress in labeling steroid receptor ligands with 99mTc. By using the techniques of molecular nuclear medicine, new imaging procedures could be developed that might provide more precise information to help characterize disease and effect treatment decisions in patients with breast or prostate cancers.
基于乳腺癌或前列腺癌的类固醇受体含量进行成像,在放射性示踪剂的设计中是一项重大挑战。类固醇激素受体是在染色质特定部位相互作用的蛋白质。几种雌激素、孕激素和雄激素的类似物已被放射性标记,并在体外和体内对受体结合亲和力和选择性进行了评估。已用[18F]氟雌二醇对患者的乳腺肿瘤进行成像。用放射性标记的孕激素类似物进行的闪烁成像可能有助于监测乳腺癌患者他莫昔芬治疗的疗效。对用氟取代的雄激素进行的动物组织分布和成像研究表明,有可能开发出一种基于类固醇受体的放射性示踪剂用于前列腺癌分期。放射化学家在用99mTc标记类固醇受体配体方面报告了一些进展。通过使用分子核医学技术,有可能开发出新的成像程序,从而提供更精确的信息,以帮助对乳腺癌或前列腺癌患者的疾病进行特征描述并做出治疗决策。