A5084633055- Click Chemistry and Applications
- Viral Infections and Vectors
- Peptidase Inhibition and Analysis
- Natural Compounds in Disease Treatment
- interferon and immune responses
- Macrophage Migration Inhibitory Factor
- Chemical Synthesis and Analysis
- Myeloproliferative Neoplasms: Diagnosis and Treatment
- Ubiquitin and proteasome pathways
Chinese Academy of Medical Sciences & Peking Union Medical College
2021-2022
Peking Union Medical College Hospital
2021
Xinjiang Institute of Materia Medica
2021
Celastrol (CEL), a pentacyclic triterpene compound, has been proven to have definite antipulmonary fibrosis effect. However, its direct targets for remain unknown. In this study, we designed and synthesized series of celastrol-based probes identify the in human pulmonary fibroblasts using an activity-based protein profiling strategy. Among many fished targets, identified key protein, cullin-associated neddylation-dissociated 1 (CAND1), which was involved fibroblast–myofibroblast...
Since triple angiokinase inhibitor could not fully explain the anti-pulmonary fibrosis activity of nintedanib (NDNB), chemoproteomic strategy was performed to identify TANK-binding kinase 1 (TBK1) as key target NDNB in human pulmonary fibroblasts (HPFs). Functionally, exerts anti-fibrosis through impairing p-TBK1-mediated Yes-associated protein (YAP)/transcriptional cofactor with PDZ-binding motif (TAZ) nuclear translocation.
We identified tripeptidyl-peptidase 1 (TPP1) as one of the direct targets nintedanib (NDNB) employing clickable photoaffinity probes, which provides insights into functional meaning well-known IPF therapeutic drug.