Associated Papers
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
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
DNA damage response and repair gene mutations predict clinical outcomes in biliary tract cancer.
Tan S et al.
Cancer, 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
Analytic validation of an FGFR -focused cell-free DNA liquid biopsy assay (FGFR-Dx).
Reeser JW et al.
Medrxiv : the Preprint Server for Health Sciences, 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
Therapeutic advances of targeting receptor tyrosine kinases in cancer.
Tomuleasa C et al.
Signal Transduction and Targeted Therapy, 2024
Computational biophysical characterization of the effect of gatekeeper mutations on the binding of ponatinib to the FGFR kinase.
Mahapatra S et al.
Archives of Biochemistry and Biophysics, 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
Targeted next-generation sequencing of 491 lung cancers in clinical practice: Implications for future detection strategy and targeted therapy.
Liu XD et al.
Heliyon, 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
Preclinical characterization of CPL304110 as a potent and selective inhibitor of fibroblast growth factor receptors 1, 2, and 3 for gastric, bladder, and squamous cell lung cancer.
Popiel D et al.
Frontiers in Oncology, 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
A new ALK inhibitor overcomes resistance to first- and second-generation inhibitors in NSCLC.
Lu Y et al.
Embo Molecular Medicine, 2022
Case Report: Targeted Therapy with Anlotinib for a Rare Case of Spinal Cord Glioblastoma with FGFR3 Mutation.
Liu R et al.
Oncotargets and Therapy, 2022
Mutation profile and immunoscore signature in thymic carcinomas: An exploratory study and review of the literature.
Asselta R et al.
Thoracic Cancer, 2021
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
Exploiting loss of heterozygosity for allele-selective colorectal cancer chemotherapy.
Rendo V et al.
Nature Communications, 2020
dbCPM: a manually curated database for exploring the cancer passenger mutations.
Yue Z et al.
Briefings in Bioinformatics, 2020
Development and validation of a targeted gene sequencing panel for application to disparate cancers.
McCabe MJ et al.
Scientific Reports, 2019
Discovery of 2-(4-Chloro-3-(trifluoromethyl)phenyl)-N-(4-((6,7-dimethoxyquinolin-4-yl)oxy)phenyl)acetamide (CHMFL-KIT-64) as a Novel Orally Available Potent Inhibitor against Broad-Spectrum Mutants of c-KIT Kinase for Gastrointestinal Stromal Tumors.
Wu Y et al.
Journal of Medicinal Chemistry, 2019
Discovery of ( E)- N1-(3-Fluorophenyl)- N3-(3-(2-(pyridin-2-yl)vinyl)-1 H-indazol-6-yl)malonamide (CHMFL-KIT-033) as a Novel c-KIT T670I Mutant Selective Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs).
Liu X et al.
Journal of Medicinal Chemistry, 2019
Discovery of potent SOS1 inhibitors that block RAS activation via disruption of the RAS-SOS1 interaction.
Hillig RC et al.
Proceedings of the National Academy of Sciences of the United States of America, 2019
Targeted mutation detection in breast cancer using MammaSeq™.
Smith NG et al.
Breast Cancer Research : Bcr, 2019
Validation and Clinical Applications of a Comprehensive Next Generation Sequencing System for Molecular Characterization of Solid Cancer Tissues.
Dehghani M et al.
Frontiers in Molecular Biosciences, 2019
Expression of myeloid Src-family kinases is associated with poor prognosis in AML and influences Flt3-ITD kinase inhibitor acquired resistance.
Patel RK et al.
Plos One, 2019
Structure, activation and dysregulation of fibroblast growth factor receptor kinases: perspectives for clinical targeting.
Farrell B et al.
Biochemical Society Transactions, 2018
A therapeutic approach to pantothenate kinase associated neurodegeneration.
Sharma LK et al.
Nature Communications, 2018
The potent and selective cyclin-dependent kinases 4 and 6 inhibitor ribociclib (LEE011) is a versatile combination partner in preclinical cancer models.
Kim S et al.
Oncotarget, 2018
Validation of the Oncomine™ focus panel for next-generation sequencing of clinical tumour samples.
Williams HL et al.
Virchows Archiv : an International Journal of Pathology, 2018