Harnessing affinity-based protein profiling to reveal a novel target of nintedanib. Issue 25 (26th February 2021)

• Record Type: Journal Article
• Authors: Chen, Xiong; Li, Menglin; Li, Manru; Wang, Dongmei; Zhang, Jinlan
• Is Part Of: Chemical communications. Volume 57:Issue 25(2021)
• Page Start: 3139
• Page End: 3142
• Publication Date: 2021-02-26
• Subjects: Chemistry -- Periodicals; 540
• DOI: 10.1039/d1cc00354b
• Languages: English
• ISSNs: 1359-7345

Abstract

Abstract : We identified tripeptidyl-peptidase 1 (TPP1) as one of the direct targets of nintedanib (NDNB) employing clickable photoaffinity probes, which provides insights into the functional meaning of the well-known IPF therapeutic drug. Abstract : Nintedanib (BIBF1120), a triple angiokinase inhibitor, was first approved for idiopathic pulmonary fibrosis (IPF) therapy and is also efficacious for lung carcinoma, and interstitial lung diseases, far beyond its inhibition of VEGFR/PDGFR/FGFR. We identified tripeptidyl-peptidase 1 (TPP1) as one of the direct targets of nintedanib employing the affinity-based protein profiling (A f BPP) technique. This may be a new mechanism for nintedanib's role different from tyrosine kinase inhibition.