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

Authors
Park, Bernie ByunghoonChoi, Jae WanPark, DawonChoi, DoyoungPaek, JiwonKim, Hyun JungSon, Se-YoungUl Mushtaq, AmeeqShin, HyejiKim, Sang HoonZhou, YuanyuanLim, TaehyeongPark, Ji YoungBaek, Ji-YoungKim, KyulKwon, HongmokSon, Sang-HyunChung, Ka YoungJeong, Hyun-JaKim, Hyung-MinJung, Yong WooLee, KihoLee, Ki YongByun, YoungjooJeon, Young Ho
Issue Date
19-Jun-2019
Publisher
NATURE PUBLISHING GROUP
Citation
SCIENTIFIC REPORTS, v.9
Indexed
SCIE
SCOPUS
Journal Title
SCIENTIFIC REPORTS
Volume
9
URI
https://scholar.korea.ac.kr/handle/2021.sw.korea/64748
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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