@article{oai:repo.qst.go.jp:00080385, author = {Kuan, Hu and Xie, Lin and Hanyu, Masayuki and Zhang, Yiding and Ma, Xiaohui and Li, Lingyun and Nagatsu, Kotaro and Suzuki, Hisashi and Wang, Weizhi and Ming-Rong, Zhang and Kuan, Hu and Lin, Xie and Masayuki, Hanyu and Zhang, Yiding and Kotaro, Nagatsu and Hisashi, Suzuki and Zhang, Ming-Rong}, issue = {1}, journal = {RSC Chemical Biology}, month = {Aug}, note = {Interface peptides that mediate protein-protein interactions (PPI) are a class of important lead compounds for designing PPI inhibitors. However, Their potential as precursors for radiotracers has never been exploited. Here we reported that the interface peptides from programmed death-ligand 1 (PD-L1) can be used in positron emission tomography (PET) imaging of the programmed cell death 1 (PD-1) with high accuracy and sensitivity. Moreover, the performance differentiation between murine PD-L1 derived interface peptide (mPep-1) and human PD-L1 derived interface peptide (hPep-1) as PET tracers for PD-1 unveiled an unprecedented role of a non-critical residue in target binding, highlighting of the significance of PET imaging as a companion diagnostics in drug development. Collectively, this study not only provided a first-of-its-kind peptide-based PET tracer for PD-1 but also conveyed a unique paradigm for developing imaging agents for highly challenging protein targets, which could be used to identify other protein biomarkers involved in the PPI networks.}, pages = {214--224}, title = {Harnessing PD-L1 interface peptide for positron emission tomography imaging of the PD-1 immune checkpoint}, volume = {2020}, year = {2020} }