Associated Papers
Comprehensive resistance profiling of chronic myeloid leukaemia associated ABL1 variants against five tyrosine kinase inhibitors using prime editing.
Jung Y et al.
Nature Biomedical Engineering, 2025
Innovative rapid screening for complex BCR-ABL1 kinase domain mutations in TKI-treated leukaemia patients.
Lan Y et al.
British Journal of Cancer, 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
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
Current and future of targeted therapies against BCR::ABL kinases.
Jayavel S et al.
Journal of the Egyptian National Cancer Institute, 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 MDI-114215: A Potent and Selective LIMK Inhibitor To Treat Fragile X Syndrome.
Baldwin AG et al.
Journal of Medicinal Chemistry, 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
Discovery of highly potent and ALK2/ALK1 selective kinase inhibitors using DNA-encoded chemistry technology.
Jimmidi R et al.
Proceedings of the National Academy of Sciences of the United States of America, 2024
A first-in-class Wiskott-Aldrich syndrome protein activator with antitumor activity in hematologic cancers.
Spriano F et al.
Haematologica, 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
Validation of a novel NGS based BCR::ABL1 kinase domain mutation detection assay in Indian cohort.
Chaudhary P et al.
Scientific Reports, 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
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
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
Droplet digital PCR for the detection of second-generation tyrosine kinase inhibitor-resistant BCR::ABL1 kinase domain mutations in chronic myeloid leukemia.
Soverini S et al.
Leukemia, 2022
Designing Novel BCR-ABL Inhibitors for Chronic Myeloid Leukemia with Improved Cardiac Safety.
Pandrala M et al.
Journal of Medicinal Chemistry, 2022
Copy number alterations define outcome in Philadelphia chromosome-positive acute lymphoblastic leukemia.
Hohtari H et al.
Haematologica, 2022
Detection of kinase domain mutations in BCR::ABL1 leukemia by ultra-deep sequencing of genomic DNA.
Sánchez R et al.
Scientific Reports, 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
A new ALK inhibitor overcomes resistance to first- and second-generation inhibitors in NSCLC.
Lu Y et al.
Embo Molecular Medicine, 2022
A multicenter total therapy strategy for de novo adult Philadelphia chromosome positive acute lymphoblastic leukemia patients: final results of the GIMEMA LAL1509 protocol.
Chiaretti S et al.
Haematologica, 2021
The role of E255K/V-inclusive mutations in a Philadelphia-positive acute lymphoblastic leukemia with mutation evolution during sequential TKIs therapies: A case report.
Zhao M et al.
Medicine, 2021
Next-generation sequencing improves BCR-ABL1 mutation detection in Philadelphia chromosome-positive acute lymphoblastic leukaemia.
Soverini S et al.
British Journal of Haematology, 2021
Mutational spectrum and precision oncology for biliary tract carcinoma.
Lin J et al.
Theranostics, 2021
Patient specific circulating tumor DNA fingerprints to monitor treatment response across multiple tumors.
Li J et al.
Journal of Translational Medicine, 2020
Mutations in the BCR-ABL1 kinase domain in patients with chronic myeloid leukaemia treated with TKIs or at diagnosis.
Liu J et al.
Oncology Letters, 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
Ultra-accurate Duplex Sequencing for the assessment of pretreatment ABL1 kinase domain mutations in Ph+ ALL.
Short NJ et al.
Blood Cancer Journal, 2020
Exploiting loss of heterozygosity for allele-selective colorectal cancer chemotherapy.
Rendo V et al.
Nature Communications, 2020
The Immunogenic Potential of Recurrent Cancer Drug Resistance Mutations: An In Silico Study.
Punta M et al.
Frontiers in Immunology, 2020