10.1021/acs.molpharmaceut.8b00325.s001 Weichao Li Weichao Li Yiqing Zhou Yiqing Zhou Guanghui Tang Guanghui Tang Nai-Kei Wong Nai-Kei Wong Mengquan Yang Mengquan Yang Dan Tan Dan Tan Youli Xiao Youli Xiao Chemoproteomics Reveals the Antiproliferative Potential of Parkinson’s Disease Kinase Inhibitor LRRK2-IN‑1 by Targeting PCNA Protein American Chemical Society 2018 cancer cells cancer cell death LRRK 2-IN cell cycle arrest Targeting PCNA Protein LRRK 2-IN 2018-07-11 00:00:00 Journal contribution https://acs.figshare.com/articles/journal_contribution/Chemoproteomics_Reveals_the_Antiproliferative_Potential_of_Parkinson_s_Disease_Kinase_Inhibitor_LRRK2-IN_1_by_Targeting_PCNA_Protein/6854807 LRRK2-IN-1, one of the first selective inhibitors of leucine-rich repeat kinase 2 (LRRK2), was serendipitously found to exhibit potent antiproliferative activity in several types of human cancer cells. In this study, we employed a chemoproteomic strategy utilizing a photoaffinity probe to identify the cellular target(s) of LRRK2-IN-1 underlying its anticancer activity. LRRK2-IN-1 was found to induce cell cycle arrest as well as cancer cell death by specifically binding to human proliferating cell nuclear antigen (PCNA) in cancer cells. Our current findings suggest the potential of LRRK2-IN-1 as a novel pharmacological molecule for scrutinizing cell physiology and furnish a logical foundation for the future development of therapeutic reagents for cancer.