ArticleInternational journal of molecular sciences2020
Activity-Based Protein Profiling Reveals Potential Dasatinib Targets in Gastric Cancer.
Article in International journal of molecular sciences, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
17 citing papers in PubMed, 20 citations in OpenAlex.
- Quantification of Binding of Small Molecules to Native Kinases by Flow Cytometry Reveals Divergence from Biochemical Affinities.Journal of the American Chemical Society · 2026Article
- Molecular and Biochemical Evidence of Edaravone's Impact on Dasatinib-induced AGS Cell Senescence: A Promising Strategy for Gastric Cancer Therapy.Current medicinal chemistry · 2026Article
- Single cell analysis reveals cancer associated fibroblast subtypes as prognostic markers and therapeutic targets in gastric cancer.Discover oncology · 2025Article
- Development and verification of lymphangiogenesis score for prediction of prognosis and immune landscape in gastric cancer.Frontiers in immunology · 2025Article
- MAPK-targeted therapies in non-gastrointestinal stromal tumor soft tissue sarcomas: current landscape and future directions.Frontiers in oncology · 2025Review
- Integrating transcriptomic data and digital pathology for NRG-based prediction of prognosis and therapy response in gastric cancer.Annals of medicine · 2024Article
- Osteosarcoma: A comprehensive review of model systems and experimental therapies.Medical research archives · 2024Article
- Therapeutic targeting of senescent cells in the CNS.Nature reviews. Drug discovery · 2024Review
- Activity-based protein profiling and global proteome analysis reveal MASTL as a potential therapeutic target in gastric cancer.Cell communication and signaling : CCS · 2024Article
- Advances in targeted therapy for human epidermal growth factor receptor 2 positive in advanced gastric cancer.World journal of gastrointestinal oncology · 2024Review
- Characterization of gastric cancer-stimulated signaling pathways and function of CTGF in cancer-associated fibroblasts.Cell communication and signaling : CCS · 2024Article
- CSF3R T618I Collaborates With RUNX1-RUNX1T1 to Expand Hematopoietic Progenitors and Sensitizes to GLI Inhibition.HemaSphere · 2023Article
- Molecular Target and Action Mechanism of Anti-Cancer Agents.International journal of molecular sciences · 2023Article
- Study on the role and pharmacology of cuproptosis in gastric cancer.Frontiers in oncology · 2023Article
- Drugging the undruggable: activity-based protein profiling offers opportunities for targeting the KLK activome.Cancer biology & therapy · 2022Article
- Overexpression of Laminin 5Journal of oncology · 2022Article
- Identification of Nucleolin as a Novel AEG-1-Interacting Protein in Breast Cancer via Interactome Profiling.Cancers · 2021Article
Corrections and comments
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Authors and funding
12 authors at 3 institutions in 1 country.
Funding
Abstract
Dasatinib is a multi-target kinase inhibitor, whose targets include BCR-ABL, SRC family kinases, and various cancer kinases. The elevated SRC activity in gastric cancer (GC) has prompted the need for the therapeutic application of dasatinib in GC. We observed that the efficacy of dasatinib varied with the GC cell lines. The differential effect of dasatinib was not correlated with the basal SRC activity of each cell line. Moreover, the GC cell lines showing the strong antitumor effects of dasatinib were refractory to other SRC inhibitors, i.e., bosutinib and saracatinib, suggesting that unexpected dasatinib's targets could exist. To profile the targets of dasatinib in GC, we performed activity-based protein profiling (ABPP) via mass spectrometry using a desthiobiotin-ATP probe. We identified 29 and 18 kinases as potential targets in dasatinib-sensitive (SNU-216, MKN-1) and -resistant (SNU-484, SNU-601) cell lines, respectively. The protein-protein interaction mapping of the differential drug targets in dasatinib-sensitive and -resistant GC using the STRING database suggested that dasatinib could target cellular energy homeostasis in the drug-sensitive GC. RNAi screening for identified targets indicated p90RSK could be a novel dasatinib target, which is important for maintaining the viability and motility of GC cells. Further functional validation of dasatinib off-target actions will provide more effective therapeutic options for GC.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.