ArticleJournal of thrombosis and haemostasis : JTH2018
The small-molecule MERTK inhibitor UNC2025 decreases platelet activation and prevents thrombosis.
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Article in Journal of thrombosis and haemostasis : JTH, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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23citing papers in PubMed
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Who cites it
23 citing papers in PubMed, 30 citations in OpenAlex.
- Endothelial MerTK impairment promotes cardiac dysfunction in the condition of high fat diet.Redox biology · 2026Article
- Enhancing Chemosensitivity With Quercetin: Mechanistic Insights Into MerTK and Associated Signaling Pathways.Cancer reports (Hoboken, N.J.) · 2025Review
- iMer, a naturally occurring MERTK splice variant, binds to GAS6 to decrease platelet activation and thrombus formation.Blood vessels, thrombosis & hemostasis · 2025Article
- Recent advances in TAM mechanisms in lung diseases.Journal of translational medicine · 2025Review
- UNC9426, a Potent and Orally Bioavailable TYRO3-Specific Inhibitor.Journal of medicinal chemistry · 2025Article
- MERTK Inhibition as a Targeted Novel Cancer Therapy.International journal of molecular sciences · 2024Review
- Design, Synthesis, and Biological Evaluation of 2-Substituted Aniline Pyrimidine Derivatives as Potent Dual Mer/c-Met Inhibitors.Molecules (Basel, Switzerland) · 2024Article
- Regulation of brain endothelial cell physiology by the TAM receptor tyrosine kinase Mer.Communications biology · 2023Article
- Targeted Phagocytosis Induction for Cancer Immunotherapy via Bispecific MerTK-Engaging Antibodies.International journal of molecular sciences · 2022Article
- Apolipoprotein A-I, elevated in trauma patients, inhibits platelet activation and decreases clot strength.Platelets · 2022Article
- Immunothrombosis and the Role of Platelets in Venous Thromboembolic Diseases.International journal of molecular sciences · 2022Review
- Rodent models of pulmonary embolism and chronic thromboembolic pulmonary hypertension.Heliyon · 2022Review
- Vitamin K Effects on Gas6 and Soluble Axl Receptors in Intensive Care Patients: An Observational Screening Study.Nutrients · 2021Observational
- Targeting MERTK and AXL inCancers · 2021Review
- Multi-omics data integration and network-based analysis drives a multiplex drug repurposing approach to a shortlist of candidate drugs against COVID-19.Briefings in bioinformatics · 2021Article
- MERTK Inhibition: Potential as a Treatment Strategy in EGFR Tyrosine Kinase Inhibitor-Resistant Non-Small Cell Lung Cancer.Pharmaceuticals (Basel, Switzerland) · 2021Review
- MERTK in cancer therapy: Targeting the receptor tyrosine kinase in tumor cells and the immune system.Pharmacology & therapeutics · 2020Review
- Pulmonary Artery Thrombosis: A Diagnosis That Strives for Its Independence.International journal of molecular sciences · 2020Review
- Mouse laser injury models: variations on a theme.Platelets · 2020Review
- TAM-ing T cells in the tumor microenvironment: implications for TAM receptor targeting.Cancer immunology, immunotherapy : CII · 2020Review
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Authors and funding
21 authors at 6 institutions in 1 country.
B R BranchfordDepartment of Pediatrics, Section of Hematology/Oncology, University of Colorado School of Medicine, Aurora, CO, USA.ORCID 0000-0002-4076-270X
T J StalkerDepartment of Medicine, University of Pennsylvania, Philadelphia, PA, USA.
L LawDepartment of Pediatrics, Section of Hematology/Oncology, University of Colorado School of Medicine, Aurora, CO, USA.
G AcevedoDepartment of Pediatrics, Section of Hematology/Oncology, University of Colorado School of Medicine, Aurora, CO, USA.
S SatherDepartment of Pediatrics, Section of Hematology/Oncology, University of Colorado School of Medicine, Aurora, CO, USA.
C BrzezinskiDepartment of Pediatrics, Section of Hematology/Oncology, University of Colorado School of Medicine, Aurora, CO, USA.
K M WilsonCarver College of Medicine, University of Iowa, Iowa City, IA, USA.
K MinsonAflac Cancer and Blood Disorders Center of Children's Healthcare of Atlanta, Atlanta, GA, USA.
A B Lee-SherickDepartment of Pediatrics, Section of Hematology/Oncology, University of Colorado School of Medicine, Aurora, CO, USA.
P Davizon-CastilloDepartment of Pediatrics, Section of Hematology/Oncology, University of Colorado School of Medicine, Aurora, CO, USA.
C NgDepartment of Pediatrics, Section of Hematology/Oncology, University of Colorado School of Medicine, Aurora, CO, USA.
W ZhangCenter for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC, USA.
K B NeevesDepartment of Chemical & Biological Engineering, Colorado School of Mines, Golden, CO, USA.
S R LentzCarver College of Medicine, University of Iowa, Iowa City, IA, USA.
X WangCenter for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC, USA.
S V FryeCenter for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC, USA.
H Shelton EarpLineberger Comprehensive Cancer Center, Department of Medicine, School of Medicine, University of North Carolina, Chapel Hill, NC, USA.
D DeRyckereAflac Cancer and Blood Disorders Center of Children's Healthcare of Atlanta, Atlanta, GA, USA.
L F BrassDepartment of Medicine, University of Pennsylvania, Philadelphia, PA, USA.
D K GrahamAflac Cancer and Blood Disorders Center of Children's Healthcare of Atlanta, Atlanta, GA, USA.
J A Di PaolaDepartment of Pediatrics, Section of Hematology/Oncology, University of Colorado School of Medicine, Aurora, CO, USA.
University of Colorado Denver · USUniversity of North Carolina at Chapel Hill · USEmory University · USUniversity of Iowa · USUniversity of Pennsylvania · USColorado School of Mines · US
Funding
University of Colorado Cancer Center Support Grant - Lung Cancer Patient-Derived Xenografts with Autologous Human Immune SystemsP30CA046934 · NCI · UNIVERSITY OF COLORADO DENVER · PI James V Degregori · 1988 to 2026
$117.0MSubcellular Mechanisms pf Platelet ActivationP01HL040387 · NHLBI · UNIVERSITY OF PENNSYLVANIA · PI BENNETT, JOEL S. · 1988 to 2018
$35.5MHEMATOLOGY CLINICAL RESEARCH TRAINING PROGRAMT32HL007439 · NHLBI · UNIVERSITY OF PENNSYLVANIA · PI LAWRENCE F BRASS, PETER S KLEIN · 1985 to 2026
$17.1MThrombosis Models CoreP01HL120846 · NHLBI · UNIVERSITY OF PENNSYLVANIA · PI ABRAMS, CHARLES S. · 2014 to 2018
$12.2MTraining in Basic and Translational Child Health ResearchK12HD068372 · NICHD · UNIVERSITY OF COLORADO DENVER · PI DANIELS, STEPHEN R · 2011 to 2020
$3.7MA Systems Biology Approach to Predicting Bleeding in HemophiliaR01HL120728 · NHLBI · COLORADO SCHOOL OF MINES · PI DI PAOLA, JORGE A, FOGELSON, AARON L · 2014 to 2018
$2.7MGenetic Modifiers of von Willebrand DiseaseR01HL084086 · NHLBI · UNIVERSITY OF IOWA · PI DI PAOLA, JORGE A · 2007 to 2011
$1.7MNCI NIH HHS P30 CA046934NHLBI NIH HHS P01 HL040387NHLBI NIH HHS P01 HL120846NHLBI NIH HHS R01 HL084086NHLBI NIH HHS R01 HL120728NHLBI NIH HHS T32 HL007439NICHD NIH HHS K12 HD068372
Abstract
Essentials Signaling by Gas6 through Tyro3/Axl/Mer receptors is essential for stable platelet aggregation. UNC2025 is a small molecule inhibitor of the Mer tyrosine kinase. UNC2025 decreases platelet activation in vitro and thrombus formation in vivo. UNC2025's anti-platelet effect is synergistic with inhibition of the ADP receptor, P2Y SUMMARY: Background Growth arrest-specific protein 6 signals through the TAM (TYRO-3-AXL-MERTK) receptor family, mediating platelet activation and thrombus formation via activation of the aggregate-stabilizing α
Indexed as
AdenineAnimalsAxl Receptor Tyrosine KinaseBlood Plateletsc-Mer Tyrosine KinaseDisease Models, AnimalDrug SynergismDrug Therapy, CombinationFemaleGrowth Arrest-Specific Protein 6HumansIntercellular Signaling Peptides and ProteinsMaleMice, Inbred C57BLPhosphorylationPiperazinesAdenineAxl Receptor Tyrosine Kinasec-Mer Tyrosine KinaseGrowth Arrest-Specific Protein 6Intercellular Signaling Peptides and ProteinsMERTK protein, humanMertk protein, mousePiperazinesPlatelet Aggregation InhibitorsPlatelet Glycoprotein GPIIb-IIIa ComplexProtein Kinase InhibitorsProto-Oncogene ProteinsPurinergic P2Y Receptor AntagonistsReceptor Protein-Tyrosine KinasesTYRO3 protein, humanTyro3 protein, mouseUNC2025growth arrest-specific protein 6integrin αIIbβ3MERTKplatelet activationthrombosis
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