ArticleExperimental & molecular medicine2022
BMS794833 inhibits macrophage efferocytosis by directly binding to MERTK and inhibiting its activity.
Article in Experimental & molecular medicine, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 21 papers.
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21 citing papers in PubMed, 24 citations in OpenAlex.
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- Dynamic remodeling of the pancreas immune landscape in obesity.Nature communications · 2026Article
- FADS1-mediated Efferocytosis in Tumor-Associated Macrophages Shapes an Immunosuppressive Microenvironment in Gastric Cancer.Cellular and molecular life sciences : CMLS · 2026Article
- Targeting programmed cell death in male infertility: pathogenic mechanisms and therapeutic strategies.Molecular biology reports · 2026Review
- Mitochondria Clearance Enables Macrophage-Driven Maturation of iPSC-Derived Cardiomyocyte Metabolism.Cellular and molecular bioengineering · 2026Article
- Targeted proteomic analyses during combined angiotensin-converting enzyme inhibitor and mineralocorticoid receptor antagonist administration (CARDALIS®) in healthy dogs.Journal of veterinary internal medicine · 2026Article
- Stalling the Enemy: Targeting Nsp13 for Next-Generation SARS-CoV-2 Antivirals.International journal of molecular sciences · 2026Article
- Advancements in nanomedicine for the therapeutic regulation of efferocytosis: opportunities and challenges.Theranostics · 2026Review
- Lnc-CHRM4-2:1 Inhibits M2 Polarization and Efferocytosis of Macrophages by Downregulating MerTK and SLC2A1 in Rheumatoid Arthritis.Journal of immunology research · 2026Article
- Article
- Interrogating mediators of single-cell transcriptional changes in the acute damaged cerebral cortex: Insights into endothelial-astrocyte interactions.Molecular and cellular neurosciences · 2025Article
- USP22 enhances atherosclerotic plaque stability and macrophage efferocytosis by stabilizing PPARγ.Communications biology · 2025Article
- Targeting MERTK tyrosine kinase: Virtual screening and molecular dynamics insights for anti-cancer drug development.PloS one · 2025Article
- Discovery of Dual MER/AXL Kinase Inhibitors as Bifunctional Small Molecules for Inhibiting Tumor Growth and Enhancing Tumor Immune Microenvironment.Journal of medicinal chemistry · 2024Article
- The Role of Macrophage Efferocytosis in the Pathogenesis of Apical Periodontitis.International journal of molecular sciences · 2024Article
- SOX2 Expression Does Not Guarantee Cancer Stem Cell-like Characteristics in Lung Adenocarcinoma.Cells · 2024Article
- Targeting Macrophages for Tumor Therapy.The AAPS journal · 2023Review
- Glucose Deprivation Induces Cancer Cell Death through Failure of ROS Regulation.International journal of molecular sciences · 2023Article
Corrections and comments
- Erratum issued
Authors and funding
6 authors at 4 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Myeloid epithelial reproductive proto-oncogene tyrosine kinase (MERTK) plays an essential role in modulating cancer immune tolerance by regulating macrophage efferocytosis. Studies are underway to develop small-molecule chemicals that inhibit MERTK as cancer immunotherapeutic agents, but these efforts are in their early stages. This study identified BMS794833, whose primary targets are MET and VEGFR2, as a potent MERTK inhibitor and developed a real-time efferocytosis monitoring system. The X-ray cocrystal structure revealed that BMS794833 was in contact with the ATP-binding pocket and the allosteric back pocket, rendering MERTK inactive. Homogeneous time-resolved fluorescence kinetic and Western blotting analyses showed that BMS794833 competitively inhibited MERTK activity in vitro and inhibited the autophosphorylation of MERTK in macrophages. We developed a system to monitor MERTK-dependent efferocytosis in real time, and using this system, we confirmed that BMS794833 significantly inhibited the efferocytosis of differentiated macrophages. Finally, BMS794833 significantly inhibited efferocytosis in vivo in a mouse model. These data show that BMS794833 is a type II MERTK inhibitor that regulates macrophage efferocytosis. In addition, the real-time efferocytosis monitoring technology developed in this study has great potential for future applications.
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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.