Bauer David, Visca Hannah, Weerakkody Anuradha, Carter Lukas M, Samuels Zachary, Kaminsky Spencer, Andreev Oleg A, Reshetnyak Yana K, Lewis Jason S
Department of Radiology and the Molecular Pharmacology Program, Memorial Sloan Kettering Cancer Center, New York, NY, United States.
Department of Physics, University of Rhode Island, Kingston, RI, United States.
Front Oncol. 2022 May 19;12:882541. doi: 10.3389/fonc.2022.882541. eCollection 2022.
Acidosis of the tumor microenvironment is a hallmark of tumor progression and has emerged as an essential biomarker for cancer diagnosis, prognosis, and evaluation of treatment response. A tool for quantitatively visualizing the acidic tumor environment could significantly advance our understanding of the behavior of aggressive tumors, improving patient management and outcomes. Zr-labeled pH-low insertion peptides (pHLIP) are a class of radiopharmaceutical imaging probes for the analysis of acidic tumor microenvironments positron emission tomography (PET). Their unique structure allows them to sense and target acidic cancer cells. In contrast to traditional molecular imaging agents, pHLIP's mechanism of action is pH-dependent and does not rely on the presence of tumor-specific molecular markers. In this study, one promising acidity-imaging PET probe ([Zr]Zr-DFO-Cys-Var3) was identified as a candidate for clinical translation.
肿瘤微环境的酸中毒是肿瘤进展的一个标志，并且已成为癌症诊断、预后以及治疗反应评估的重要生物标志物。一种用于定量可视化酸性肿瘤环境的工具能够显著推进我们对侵袭性肿瘤行为的理解，改善患者管理和治疗结果。锆标记的pH-低插入肽（pHLIP）是一类用于正电子发射断层扫描（PET）分析酸性肿瘤微环境的放射性药物成像探针。它们独特的结构使其能够感知并靶向酸性癌细胞。与传统分子成像剂不同，pHLIP的作用机制是pH依赖性的，并不依赖于肿瘤特异性分子标志物的存在。在本研究中，一种有前景的酸度成像PET探针（[Zr]Zr-DFO-Cys-Var3）被确定为临床转化的候选物。
