Translocator protein (TSPO)-Targeted agents for photodynamic therapy of cancer.

Xie Q

Xie Q(1), Su M(1), Liu Y(1), Zhang D(2), Li Z(3), Bai M(4).
Author information:
(1)Vanderbilt University Institute of Imaging Sciences, Vanderbilt University Medical Center, 1161 21st Avenue South, Nashville, TN, 37232, USA.
(2)Vanderbilt University Institute of Imaging Sciences, Vanderbilt University Medical Center, 1161 21st Avenue South, Nashville, TN, 37232, USA; Department of Hepatobiliary Surgery, The Second Affiliated Hospital of Guangzhou Medical University, No. 250 East Changgang Road, Guangzhou, 510260, PR China.
(3)Vanderbilt University Institute of Imaging Sciences, Vanderbilt University Medical Center, 1161 21st Avenue South, Nashville, TN, 37232, USA; Department of General Surgery, The Fourth Affiliated Hospital of China Medical University, No. 4 Chongshan East Road, Huanggu District, Shenyang, 110032, PR China.
(4)Vanderbilt University Institute of Imaging Sciences, Vanderbilt University Medical Center, 1161 21st Avenue South, Nashville, TN, 37232, USA; Department of Radiology and Radiological Sciences, Vanderbilt University Medical Center, Nashville, TN, 37232, USA; Vanderbilt Ingram Cancer Center, Vanderbilt University Medical Center, Nashville, TN, 37232, USA. Electronic address: [Email]

https://dx.doi.org/10.1016/j.pdpdt.2021.102209

Photodynamic therapy (PDT) is a clinically approved therapeutic strategy that combines a specific wavelength of light and light-activated photosensitizers (PSs). The usage of PDT for cancer treatment is often hampered by the lack of tumor selectivity of PSs, which may cause photodamage to surrounding normal tissues. Recently, translocator protein (TSPO) has attracted great interest as a tumor biomarker, whose expression correlates with tumor aggressiveness. In this study, we report the development of a series of novel TSPO-PSs based on quinazoline, pyrazolopyrimidine, and tetrahydrocarbazole structures. These TSPO-PSs bind to TSPO with nanomolar affinities and demonstrated efficient and target-specific PDT effect upon light irradiation. Therefore, they may have great potential in the treatment of tumors associated with high-TSPO expression.