Cargando…
Structure-Activity Relationships of Baicalein and its Analogs as Novel TSLP Inhibitors
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 TSL...
| Autores principales: | , , , , , , , , , , , , , , , , , , , , , , , , |
|---|---|
| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
Nature Publishing Group UK
2019
|
| Materias: | |
| Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6584507/ https://www.ncbi.nlm.nih.gov/pubmed/31217492 http://dx.doi.org/10.1038/s41598-019-44853-5 |
| _version_ | 1783428523069800448 |
|---|---|
| author | Park, Bernie Byunghoon Choi, Jae Wan Park, Dawon Choi, Doyoung Paek, Jiwon Kim, Hyun Jung Son, Se-Young Mushtaq, Ameeq Ul Shin, Hyeji Kim, Sang Hoon Zhou, Yuanyuan Lim, Taehyeong Park, Ji Young Baek, Ji-Young Kim, Kyul Kwon, Hongmok Son, Sang-Hyun Chung, Ka Young Jeong, Hyun-Ja Kim, Hyung-Min Jung, Yong Woo Lee, Kiho Lee, Ki Yong Byun, Youngjoo Jeon, Young Ho |
| author_facet | Park, Bernie Byunghoon Choi, Jae Wan Park, Dawon Choi, Doyoung Paek, Jiwon Kim, Hyun Jung Son, Se-Young Mushtaq, Ameeq Ul Shin, Hyeji Kim, Sang Hoon Zhou, Yuanyuan Lim, Taehyeong Park, Ji Young Baek, Ji-Young Kim, Kyul Kwon, Hongmok Son, Sang-Hyun Chung, Ka Young Jeong, Hyun-Ja Kim, Hyung-Min Jung, Yong Woo Lee, Kiho Lee, Ki Yong Byun, Youngjoo Jeon, Young Ho |
| author_sort | Park, Bernie Byunghoon |
| collection | PubMed |
| description | 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. |
| format | Online Article Text |
| id | pubmed-6584507 |
| institution | National Center for Biotechnology Information |
| language | English |
| publishDate | 2019 |
| publisher | Nature Publishing Group UK |
| record_format | MEDLINE/PubMed |
| spelling | pubmed-65845072019-06-26 Structure-Activity Relationships of Baicalein and its Analogs as Novel TSLP Inhibitors Park, Bernie Byunghoon Choi, Jae Wan Park, Dawon Choi, Doyoung Paek, Jiwon Kim, Hyun Jung Son, Se-Young Mushtaq, Ameeq Ul Shin, Hyeji Kim, Sang Hoon Zhou, Yuanyuan Lim, Taehyeong Park, Ji Young Baek, Ji-Young Kim, Kyul Kwon, Hongmok Son, Sang-Hyun Chung, Ka Young Jeong, Hyun-Ja Kim, Hyung-Min Jung, Yong Woo Lee, Kiho Lee, Ki Yong Byun, Youngjoo Jeon, Young Ho Sci Rep Article 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. Nature Publishing Group UK 2019-06-19 /pmc/articles/PMC6584507/ /pubmed/31217492 http://dx.doi.org/10.1038/s41598-019-44853-5 Text en © The Author(s) 2019 Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons license and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/. |
| spellingShingle | Article Park, Bernie Byunghoon Choi, Jae Wan Park, Dawon Choi, Doyoung Paek, Jiwon Kim, Hyun Jung Son, Se-Young Mushtaq, Ameeq Ul Shin, Hyeji Kim, Sang Hoon Zhou, Yuanyuan Lim, Taehyeong Park, Ji Young Baek, Ji-Young Kim, Kyul Kwon, Hongmok Son, Sang-Hyun Chung, Ka Young Jeong, Hyun-Ja Kim, Hyung-Min Jung, Yong Woo Lee, Kiho Lee, Ki Yong Byun, Youngjoo Jeon, Young Ho Structure-Activity Relationships of Baicalein and its Analogs as Novel TSLP Inhibitors |
| title | Structure-Activity Relationships of Baicalein and its Analogs as Novel TSLP Inhibitors |
| title_full | Structure-Activity Relationships of Baicalein and its Analogs as Novel TSLP Inhibitors |
| title_fullStr | Structure-Activity Relationships of Baicalein and its Analogs as Novel TSLP Inhibitors |
| title_full_unstemmed | Structure-Activity Relationships of Baicalein and its Analogs as Novel TSLP Inhibitors |
| title_short | Structure-Activity Relationships of Baicalein and its Analogs as Novel TSLP Inhibitors |
| title_sort | structure-activity relationships of baicalein and its analogs as novel tslp inhibitors |
| topic | Article |
| url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6584507/ https://www.ncbi.nlm.nih.gov/pubmed/31217492 http://dx.doi.org/10.1038/s41598-019-44853-5 |
| work_keys_str_mv | AT parkberniebyunghoon structureactivityrelationshipsofbaicaleinanditsanalogsasnoveltslpinhibitors AT choijaewan structureactivityrelationshipsofbaicaleinanditsanalogsasnoveltslpinhibitors AT parkdawon structureactivityrelationshipsofbaicaleinanditsanalogsasnoveltslpinhibitors AT choidoyoung structureactivityrelationshipsofbaicaleinanditsanalogsasnoveltslpinhibitors AT paekjiwon structureactivityrelationshipsofbaicaleinanditsanalogsasnoveltslpinhibitors AT kimhyunjung structureactivityrelationshipsofbaicaleinanditsanalogsasnoveltslpinhibitors AT sonseyoung structureactivityrelationshipsofbaicaleinanditsanalogsasnoveltslpinhibitors AT mushtaqameequl structureactivityrelationshipsofbaicaleinanditsanalogsasnoveltslpinhibitors AT shinhyeji structureactivityrelationshipsofbaicaleinanditsanalogsasnoveltslpinhibitors AT kimsanghoon structureactivityrelationshipsofbaicaleinanditsanalogsasnoveltslpinhibitors AT zhouyuanyuan structureactivityrelationshipsofbaicaleinanditsanalogsasnoveltslpinhibitors AT limtaehyeong structureactivityrelationshipsofbaicaleinanditsanalogsasnoveltslpinhibitors AT parkjiyoung structureactivityrelationshipsofbaicaleinanditsanalogsasnoveltslpinhibitors AT baekjiyoung structureactivityrelationshipsofbaicaleinanditsanalogsasnoveltslpinhibitors AT kimkyul structureactivityrelationshipsofbaicaleinanditsanalogsasnoveltslpinhibitors AT kwonhongmok structureactivityrelationshipsofbaicaleinanditsanalogsasnoveltslpinhibitors AT sonsanghyun structureactivityrelationshipsofbaicaleinanditsanalogsasnoveltslpinhibitors AT chungkayoung structureactivityrelationshipsofbaicaleinanditsanalogsasnoveltslpinhibitors AT jeonghyunja structureactivityrelationshipsofbaicaleinanditsanalogsasnoveltslpinhibitors AT kimhyungmin structureactivityrelationshipsofbaicaleinanditsanalogsasnoveltslpinhibitors AT jungyongwoo structureactivityrelationshipsofbaicaleinanditsanalogsasnoveltslpinhibitors AT leekiho structureactivityrelationshipsofbaicaleinanditsanalogsasnoveltslpinhibitors AT leekiyong structureactivityrelationshipsofbaicaleinanditsanalogsasnoveltslpinhibitors AT byunyoungjoo structureactivityrelationshipsofbaicaleinanditsanalogsasnoveltslpinhibitors AT jeonyoungho structureactivityrelationshipsofbaicaleinanditsanalogsasnoveltslpinhibitors |