Associated Papers
Autoregulation of the MET receptor tyrosine kinase by its intracellular juxtamembrane domain.
Linossi EM et al.
The Biochemical Journal, 2025
Discovery of a MET -driven monogenic cause of steatotic liver disease.
Pinto E Vairo F et al.
Hepatology (baltimore, Md.), 2025
Discriminating activating, deactivating and resistance variants in protein kinases.
Singh G et al.
Genome Medicine, 2025
On-target toxicity limits the efficacy of CDK11 inhibition against cancers with 1p36 deletions.
Julian L et al.
Biorxiv : the Preprint Server for Biology, 2025
STX-721, a Covalent EGFR/HER2 Exon 20 Inhibitor, Utilizes Exon 20-Mutant Dynamic Protein States and Achieves Unique Mutant Selectivity Across Human Cancer Models.
Pagliarini RA et al.
Clinical Cancer Research : an Official Journal of the American Association for Cancer Research, 2025
Challenges and resistance mechanisms to EGFR targeted therapies in head and neck cancers and breast cancer: Insights into RTK dependent and independent mechanisms.
Shyamsunder S et al.
Oncotarget, 2025
Dual Disruption of DNA Repair by a Novel CHK2 Inhibitor, ART-446, and Olaparib is a Promising Strategy for Triple-Negative Breast Cancer Therapy.
Kang HJ et al.
Biomolecules & Therapeutics, 2025
Targeting c-MET Alterations in Cancer: A Review of Genetic Drivers and Therapeutic Implications.
Ji M et al.
Cancers, 2025
Image-Based Phenotypic Profiling Enables Rapid and Accurate Assessment of EGFR-Activating Mutations in Tissues from Lung Cancer Patients.
Lei Q et al.
Journal of the American Chemical Society, 2025
Discovery of a Novel Mutant-Selective Epidermal Growth Factor Receptor Inhibitor Using an In Silico Enabled Drug Discovery Platform.
Igawa H et al.
Journal of Medicinal Chemistry, 2024
A first-in-class Wiskott-Aldrich syndrome protein activator with antitumor activity in hematologic cancers.
Spriano F et al.
Haematologica, 2024
GLI1 confers resistance to PARP inhibitors by activating the DNA damage repair pathway.
Ikeuchi H et al.
Oncogene, 2024
Conserved regulatory motifs in the juxtamembrane domain and kinase N-lobe revealed through deep mutational scanning of the MET receptor tyrosine kinase domain.
Estevam GO et al.
Elife, 2024
Whole-Exome Sequencing Reveals Novel Candidate Driver Mutations and Potential Druggable Mutations in Patients with High-Risk Neuroblastoma.
Nokchan N et al.
Journal of Personalized Medicine, 2024
Strain-release alkylation of Asp12 enables mutant selective targeting of K-Ras-G12D.
Zheng Q et al.
Nature Chemical Biology, 2024
Suppression of Glioblastoma Stem Cell Potency and Tumor Growth via LRRK2 Inhibition.
Park S et al.
International Journal of Stem Cells, 2024
An ALK2 inhibitor, BLU-782, prevents heterotopic ossification in a mouse model of fibrodysplasia ossificans progressiva.
Davis AJ et al.
Science Translational Medicine, 2024
Discovery and Preclinical Characterization of BIIB129, a Covalent, Selective, and Brain-Penetrant BTK Inhibitor for the Treatment of Multiple Sclerosis.
Himmelbauer MK et al.
Journal of Medicinal Chemistry, 2024
Conserved regulatory motifs in the juxtamembrane domain and kinase N-lobe revealed through deep mutational scanning of the MET receptor tyrosine kinase domain.
Estevam GO et al.
Biorxiv : the Preprint Server for Biology, 2024
Recording and classifying MET receptor mutations in cancers.
Guérin C et al.
Elife, 2024
Biophysical and structural characterization of the impacts of MET phosphorylation on tepotinib binding.
Grädler U et al.
The Journal of Biological Chemistry, 2023
Discovery of a Potent and Selective CDKL5/GSK3 Chemical Probe That Is Neuroprotective.
Ong HW et al.
Acs Chemical Neuroscience, 2023
Multiparameter phenotypic screening for endogenous TFEB and TFE3 translocation identifies novel chemical series modulating lysosome function.
Carling PJ et al.
Autophagy, 2023
Obscurin Rho GEF domains are phosphorylated by MST-family kinases but do not exhibit nucleotide exchange factor activity towards Rho GTPases in vitro.
Koch D et al.
Plos One, 2023
SGC-CLK-1: A chemical probe for the Cdc2-like kinases CLK1, CLK2, and CLK4.
Tiek D et al.
Current Research in Chemical Biology, 2023
The aldolase inhibitor aldometanib mimics glucose starvation to activate lysosomal AMPK.
Zhang CS et al.
Nature Metabolism, 2022
Designing Novel BCR-ABL Inhibitors for Chronic Myeloid Leukemia with Improved Cardiac Safety.
Pandrala M et al.
Journal of Medicinal Chemistry, 2022
Discovery and Characterization of a Novel Series of Chloropyrimidines as Covalent Inhibitors of the Kinase MSK1.
Hall A et al.
Acs Medicinal Chemistry Letters, 2022
Insight into Targeting Exon20 Insertion Mutations of the Epidermal Growth Factor Receptor with Wild Type-Sparing Inhibitors.
Lategahn J et al.
Journal of Medicinal Chemistry, 2022
The Occurrence of MET Ectodomain Shedding in Oral Cancer and Its Potential Impact on the Use of Targeted Therapies.
De Herdt MJ et al.
Cancers, 2022
Discovery of AS-1763: A Potent, Selective, Noncovalent, and Orally Available Inhibitor of Bruton's Tyrosine Kinase.
Kawahata W et al.
Journal of Medicinal Chemistry, 2021
Capmatinib for patients with non-small cell lung cancer with MET exon 14 skipping mutations: A review of preclinical and clinical studies.
Wu YL et al.
Cancer Treatment Reviews, 2021
MET alterations and their impact on the future of non-small cell lung cancer (NSCLC) targeted therapies.
Lee M et al.
Expert Opinion on Therapeutic Targets, 2021
A narrative review of MET inhibitors in non-small cell lung cancer with MET exon 14 skipping mutations.
Santarpia M et al.
Translational Lung Cancer Research, 2021
Clinical advantage of targeted sequencing for unbiased tumor mutational burden estimation in samples with low tumor purity.
Hong TH et al.
Journal for Immunotherapy of Cancer, 2020
Identification of pathogenic missense mutations using protein stability predictors.
Gerasimavicius L et al.
Scientific Reports, 2020
MET-dependent solid tumours - molecular diagnosis and targeted therapy.
Guo R et al.
Nature Reviews. Clinical Oncology, 2020
Discovery of Highly Selective Inhibitors of Calmodulin-Dependent Kinases That Restore Insulin Sensitivity in the Diet-Induced Obesity in Vivo Mouse Model.
Fromont C et al.
Journal of Medicinal Chemistry, 2020
Damage Incorporated: Discovery of the Potent, Highly Selective, Orally Available ATR Inhibitor BAY 1895344 with Favorable Pharmacokinetic Properties and Promising Efficacy in Monotherapy and in Combination Treatments in Preclinical Tumor Models.
Lücking U et al.
Journal of Medicinal Chemistry, 2020
Discovery of MFH290: A Potent and Highly Selective Covalent Inhibitor for Cyclin-Dependent Kinase 12/13.
Liu Y et al.
Journal of Medicinal Chemistry, 2020
Therapeutic Efficacy of ABN401, a Highly Potent and Selective MET Inhibitor, Based on Diagnostic Biomarker Test in MET-Addicted Cancer.
Kim J et al.
Cancers, 2020