AUTHOR=Bauer David , Visca Hannah , Weerakkody Anuradha , Carter Lukas M. , Samuels Zachary , Kaminsky Spencer , Andreev Oleg A. , Reshetnyak Yana K. , Lewis Jason S. 

TITLE=PET Imaging of Acidic Tumor Environment With 89Zr-labeled pHLIP Probes

JOURNAL=Frontiers in Oncology

VOLUME=12

YEAR=2022

URL=https://www.frontiersin.org/journals/oncology/articles/10.3389/fonc.2022.882541

DOI=10.3389/fonc.2022.882541

ISSN=2234-943X

ABSTRACT=<p>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. <sup>89</sup>Zr-labeled pH-low insertion peptides (pHLIP) are a class of radiopharmaceutical imaging probes for the <italic>in vivo</italic> analysis of acidic tumor microenvironments <italic>via</italic> 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 ([<sup>89</sup>Zr]Zr-DFO-Cys-Var3) was identified as a candidate for clinical translation.</p>