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- W4283751946 abstract "Molecular targeting of tumor-overexpressed oncoproteins can improve the selectivity and tolerability of anticancer therapies. The immunoinhibitory membrane protein programmed death ligand 1 (PD-L1) is highly expressed on certain tumor types, which masks malignant cells from T cell recognition and creates an optimal environment for the cancer to thrive and spread. We report here a ligand-tetrazine conjugate (LTzC) armed with a PD-L1 small molecule inhibitor to selectively target PD-L1-expressing cancer cells and inhibit PD-L1 function and conjugated to a tetrazine module and a lipoyl group to incorporate bioorthogonal reactivities and an oxidative stress enhancer into the construct. By pairing LTzC with an imaging probe, we have established a track-&-tag system for selective labeling of PD-L1 both on and in living cells using click chemistry. We have further shown the specificity and versatility of LTzC by click-to-release activation of prodrugs and selective killing of PD-L1-expressing breast cancer cells, offering a new multimodal approach to track-&-treat malignant cells that are capable of evading the immune system." @default.
- W4283751946 created "2022-07-02" @default.
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- W4283751946 date "2022-07-01" @default.
- W4283751946 modified "2023-10-13" @default.
- W4283751946 title "Targeted Molecular Construct for Bioorthogonal Theranostics of PD-L1-Expressing Cancer Cells" @default.
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- W4283751946 doi "https://doi.org/10.1021/jacsau.2c00328" @default.
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