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Structure-Activity Relationships of Baicalein and its Analogs as Novel TSLP Inhibitors

Authors
Bernie Byunghoon ParkJae Wan ChoiDawon ParkDoyoung ChoiJiwon Paek김현정Se-Young SonAmeeq Ul MushtaqHyeji ShinSang Hoon KimYuanyuan ZhouTaehyeong LimJi Young ParkJi-Young BaekKyul KimHongmok KwonSang-Hyun SonKa Young ChungHyun-Ja JeongHyung-Min KimYong Woo JungKiho LeeKi Yong LeeYoungjoo ByunYoung Ho Jeon
Issue Date
Jun-2019
Publisher
Nature Publishing Group
Citation
Scientific Reports, v.9, no.1
Journal Title
Scientific Reports
Volume
9
Number
1
URI
http://scholarworks.bwise.kr/kbri/handle/2023.sw.kbri/687
DOI
10.1038/s41598-019-44853-5
ISSN
2045-2322
Abstract
Thymic stromal lymphopoietin (TSLP) plays an important role in the differentiation and proliferation of Th2 cells, resulting in eosinophilic inflammation and numerous allergic diseases. Baicalein (1), a major component of Scutellaria baicalensis, was found to be the first small molecule to block TSLP signaling pathways. It inhibited effectively eosinophil infiltration in house dust mite-induced and ovalbumin-challenged mouse models. Structure-activity relationship studies identified compound 11a, a biphenyl flavanone analog, as a novel human TSLP inhibitor for the discovery and development of new anti-allergic drugs.
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