Affinity-based Protein Profiling Reveals Cellular Targets of Photoreactive Anticancer Inhibitors

Title
Affinity-based Protein Profiling Reveals Cellular Targets of Photoreactive Anticancer Inhibitors
Authors
이준석Nan MaZhi-Min ZhangKe ChengLegen LinDong-Mei ZhangPiliang HaoKe DingWen-Cai YeZhengqiu Li
Keywords
affinity profiling; drug; photo-crosslinking
Issue Date
2019-12
Publisher
ACS Chemical Biology
Citation
VOL 14, NO 12-2552
Abstract
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.
URI
http://pubs.kist.re.kr/handle/201004/70661
ISSN
1554-8929
Appears in Collections:
KIST Publication > Article
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