Schechter Naomi R, Yang David J, Azhdarinia Ali, Chanda Mithu
Department of Radiation Oncology, The University of California San Francisco, San Francisco, California, USA.
Recent Pat Anticancer Drug Discov. 2007 Nov;2(3):251-8. doi: 10.2174/157489207782497253.
Improvement of scintigraphic tumor imaging is extensively determined by the development of more tumor specific radiopharmaceuticals. Thus, to improve the differential diagnosis, prognosis, planning and monitoring of cancer treatment, several functional pharmaceuticals have been developed. The application of molecular targets for cancer imaging, therapy and prevention using generator-produced isotopes is the major focus of many ongoing research projects. Radionuclide imaging modalities (single photon emission computed tomography, SPECT; positron emission tomography, PET) are diagnostic cross-sectional imaging techniques that map the location and concentration of radionuclide-labeled radiotracers. Generator produced isotopes, such as 99mTc and 68Ga, are readily available and affordable. 99mTc (t1/2=6 hr; 140 keV) is used for SPECT and 68Ga (t1/2=68 min; 511 keV, 89%) is used for PET. 99mTc- and 68Ga-labeled agents using various chelators have been synthesized and their potential uses to assess tumor targets have been evaluated. Molecular targets labeled with 99mTc and 68Ga can be utilized for the prediction of therapeutic response, monitoring tumor response to treatment and aiding in the differential diagnosis of tumor versus non-tumor tissue. Molecular targets for oncological research in (1) cell apoptosis, (2) gene and nucleic acid-based approach, (3) angiogenesis (4) tumor hypoxia, and (5) metabolic imaging are discussed. Numerous imaging ligands in these categories have been developed and evaluated in animals and humans. Molecular targets were imaged and their potential to redirect optimal cancer diagnosis and therapeutics was demonstrated.
闪烁肿瘤成像的改善在很大程度上取决于更多肿瘤特异性放射性药物的研发。因此,为了改善癌症治疗的鉴别诊断、预后评估、治疗规划和监测,已经开发了几种功能性药物。利用发生器产生的同位素进行癌症成像、治疗和预防的分子靶点应用是许多正在进行的研究项目的主要重点。放射性核素成像模态(单光子发射计算机断层扫描,SPECT;正电子发射断层扫描,PET)是诊断性断层成像技术,可绘制放射性核素标记的放射性示踪剂的位置和浓度。发生器产生的同位素,如99mTc和68Ga,容易获得且价格低廉。99mTc(半衰期=6小时;140keV)用于SPECT,68Ga(半衰期=68分钟;511keV,89%)用于PET。已经合成了使用各种螯合剂的99mTc和68Ga标记的试剂,并评估了它们评估肿瘤靶点的潜在用途。用99mTc和68Ga标记的分子靶点可用于预测治疗反应、监测肿瘤对治疗的反应以及辅助鉴别肿瘤组织与非肿瘤组织。讨论了肿瘤学研究在(1)细胞凋亡、(2)基于基因和核酸的方法、(3)血管生成、(4)肿瘤缺氧和(5)代谢成像方面的分子靶点。已经在动物和人类中开发并评估了这些类别中的许多成像配体。对分子靶点进行了成像,并证明了它们在优化癌症诊断和治疗方面的潜力。