Ma, Nan Zhang, Zhi-Min Lee, Jun-Seok Cheng, Ke Lin, Ligen Zhang, Dong-Mei Hao, Piliang Ding, Ke Ye, Wen-Cai Li, Zhengqiu 2024-01-19T18:33:48Z 2024-01-19T18:33:48Z 2021-09-05 2019-12 1554-8929 https://pubs.kist.re.kr/handle/201004/119273 Affinity-based protein profiling has proven to be a powerful method in target identification of bioactive molecules. Here, this technology was applied in two photoreactive anticancer inhibitors, arenobufagin and HM30181. Using UV irradiation, these photoreactive reagents can covalently cross-link to target proteins, leading to a covalent binding with target proteins. Moreover, the cellular on/off targets of these two molecules, including ATP1A1, MDR1, PARP1, DDX5, NOP2, RAB6A, and ERGIC1 were first identified by affinity-based protein profiling and bioimaging approaches. The protein hit, PARP1, was further validated to be involved in the function of the anticancer effects. English AMER CHEMICAL SOC PHOTO-CROSS-LINKERS PHOTOAFFINITY PROBES TOAD VENOM CANCER BUFADIENOLIDE ARENOBUFAGIN HM30181 DESIGN Affinity-Based Protein Profiling Reveals Cellular Targets of Photoreactive Anticancer Inhibitors Article 10.1021/acschembio.9b00784 1 ACS CHEMICAL BIOLOGY, v.14, no.12, pp.2546 - 2552 ACS CHEMICAL BIOLOGY 14 12 2546 2552 scie scopus 000504806100007 2-s2.0-85076375010 Biochemistry & Molecular Biology Biochemistry & Molecular Biology Article PHOTO-CROSS-LINKERS PHOTOAFFINITY PROBES TOAD VENOM CANCER BUFADIENOLIDE ARENOBUFAGIN HM30181 DESIGN affinity profiling drug photo-crosslinking