Harnessing affinity-based protein profiling to reveal a novel target of nintedanib

Chen, Xiong; Li, Menglin; Li, Manru; Wang, Dongmei; Zhang, Jinlan

doi:10.1039/d1cc00354b

Cited by 2 publications

(2 citation statements)

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“…In addition to the three target proteins mentioned above, a diverse of different studies have shown that chemical proteomics is an excellent and powerful technique for discovering direct protein-ligand interactions [2]. Validation revealed that tripeptidase 1 (TPP1) is one of the direct targets that may be responsible for the multiple actions of nintedanib.…”

Section: Tpp1mentioning

confidence: 99%

“…Nintedanib was approved by the EMA in 2014 for the treatment of adult patients with advanced, metastatic and locally recurrent NSCLC. Chen's team [2] used an affinity-based protein profiling (AfBPP)-based chemical proteomic strategy for the target identification of nintedanib and identified TPP1 as one of its direct targets. Patients with systemic sclerosis-associated ILD can use nintedanib to slow down the decline in lung function.…”

Section: Introductionmentioning

confidence: 99%

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Synthesis and efficacy analysis of multi-target TKI drug nintedanib

2023

Second International Conference on Biological Engineering and Medical Science (ICBioMed 2022)

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In the medical field, nintedanib (BIBF1120) belongs to a very potent small molecular buccal tyrosine kinase inhibitor (TKI), which plays an important role in the treatment of different diseases. For example, it can be used to treat idiopathic pulmonary fibrosis (IPF), lung cancer, and other interstitial lung diseases (ILD). Tripeptidase 1 (TPP1) was discovered to be a direct target for nintedanib using affinity-based protein profiling (AfBPP) technology, which might be a novel tyrosine kinase inhibition and nintedanib vary. After thorough clinical testing, the drug can be used to treat patients with a range of solid tumors and the crippling lung condition IPF. Although this drug is effective in treatment, it is very expensive. Therefore, it is necessary to study the synthesis route of nintedanib to reduce its price and make more patients able to buy the drug. Different synthetic routes for the nintedanib have been developed and greatly increased the yield of the nintedanib. As a result, the three ways that nintedanib is synthesized are analyzed in this article. The first is created via decarboxylated cyclization and acidic hydrogenation. The third employs the synthetic Eschen Moser coupling reaction path, whereas the second refines the first route. After comparing the three approaches, it can derive the best synthetic route of a drug and use it for the synthesis of the target drug. And the therapeutic effect of the target drug on the disease should not be further analyzed.

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Section: Tpp1mentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%