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

黄芩素及其类似物作为新型 TSLP 抑制剂的构效关系

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作者:Bernie Byunghoon Park, Jae Wan Choi, Dawon Park, Doyoung Choi, Jiwon Paek, Hyun Jung Kim, Se-Young Son, Ameeq Ul Mushtaq, Hyeji Shin, Sang Hoon Kim, Yuanyuan Zhou, Taehyeong Lim, Ji Young Park, Ji-Young Baek, Kyul Kim, Hongmok Kwon, Sang-Hyun Son, Ka Young Chung, Hyun-Ja Jeong, Hyung-Min Kim, Yong W

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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