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분자활성 촉매반응 연구단
분자활성 촉매반응 연구단
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HS-1371, a novel kinase inhibitor of RIP3-mediated necroptosis

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Title
HS-1371, a novel kinase inhibitor of RIP3-mediated necroptosis
Author(s)
Han-Hee Park; Se-Yeon Park; Shinmee Mah; Jung-Hee Park; Soon-Sun Hong; Sungwoo Hong; You-Sun Kim
Publication Date
2018-09
Journal
EXPERIMENTAL AND MOLECULAR MEDICINE, v.50, no.9, pp.125 -
Publisher
NATURE PUBLISHING GROUP
Abstract
Necroptosis is a type of programmed cell death that usually occurs under apoptosis-deficient conditions. Receptor-interacting protein kinase-3 (RIP3, or RIPK3) is a central player in necroptosis, and its kinase activity is essential for downstream necroptotic signaling events. Since RIP3 kinase activity has been associated with various diseases, the development of specific RIP3 inhibitors is an attractive strategy for therapeutic application. In this study, we identified a potent RIP3 inhibitor, HS-1371, by the extensive screening of chemical libraries focused on kinases. HS-1371 directly binds to RIP3 in an ATP-competitive and time-independent manner, providing a mechanism of action. Moreover, the compound inhibited TNF-induced necroptosis but did not inhibit TNF-induced apoptosis, indicating that this novel inhibitor has a specific inhibitory effect on RIP3-mediated necroptosis via the suppression of RIP3 kinase activity. Our results suggest that HS-1371 could serve as a potential preventive or therapeutic agent for diseases involving RIP3 hyperactivation © The Author(s) 2018
URI
https://pr.ibs.re.kr/handle/8788114/5203
ISSN
1226-3613
Appears in Collections:
Center for Catalytic Hydrocarbon Functionalizations(분자활성 촉매반응 연구단) > Journal Papers (저널논문)
Files in This Item:
H_s12276-018-0152-8(HS-1371).pdfDownload

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