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
Discovery of MDI-114215: A Potent and Selective LIMK Inhibitor To Treat Fragile X Syndrome.
Baldwin AG et al.
Journal of Medicinal Chemistry, 2025
Importance of driver gene mutation assessment and targeted therapy for patients with early‑stage non‑small cell lung cancer and non‑R0 resection.
Shen PY et al.
Oncology Letters, 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
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
The role of APOBEC3B in lung tumor evolution and targeted cancer therapy resistance.
Caswell DR et al.
Nature Genetics, 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
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
Genetic and pharmacological interrogation of cancer vulnerability using a multiplexed cell line screening platform.
Xia Y et al.
Communications Biology, 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
Heterogeneous Response to First-Generation Tyrosine Kinase Inhibitors in Non-Small-Cell Lung Cancers with Different EGFR Exon 19 Mutations.
Xu H et al.
Targeted Oncology, 2020
Mutation and drug-specific intracellular accumulation of EGFR predict clinical responses to tyrosine kinase inhibitors.
de Wit M et al.
Ebiomedicine, 2020
Exploiting loss of heterozygosity for allele-selective colorectal cancer chemotherapy.
Rendo V et al.
Nature Communications, 2020
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
Frequency and significance of epidermal growth factor receptor mutations detected by PCR methods in patients with non-small cell lung cancer.
Nakajima E et al.
Oncology Letters, 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
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
Combined effect of cabozantinib and gefitinib in crizotinib-resistant lung tumors harboring ROS1 fusions.
Kato Y et al.
Cancer Science, 2018
Discovery of a highly selective KIT kinase primary V559D mutant inhibitor for gastrointestinal stromal tumors (GISTs).
Yu K et al.
Oncotarget, 2017
Design of Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitors Using a Crystallographic Surrogate Derived from Checkpoint Kinase 1 (CHK1).
Williamson DS et al.
Journal of Medicinal Chemistry, 2017
Brain metastases in patients with non-small cell lung cancer: the role of mutated-EGFRs with an exon 19 deletion or L858R point mutation in cancer cell dissemination.
Hsiao SH et al.
Oncotarget, 2017
Analytic and Clinical Validation of an Ultrasensitive, Quantitative Polymerase Chain Reaction Assay for EGFR Mutation Analysis With Circulating Tumor DNA.
Wang X et al.
Archives of Pathology & Laboratory Medicine, 2017
Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode.
Wang A et al.
Journal of Medicinal Chemistry, 2017
Epidermal growth factor receptor mutations in adenocarcinoma in situ and minimally invasive adenocarcinoma detected using mutation-specific monoclonal antibodies.
Nakamura H et al.
Lung Cancer (amsterdam, Netherlands), 2016
Optimization of a Novel Series of Ataxia-Telangiectasia Mutated Kinase Inhibitors as Potential Radiosensitizing Agents.
Min J et al.
Journal of Medicinal Chemistry, 2016
Genotyping of EGFR Mutations from Bronchial Cytological Specimens in Slovakian Lung Cancer Patients.
Baluchova K et al.
Advances in Experimental Medicine and Biology, 2016
Characterization of DDR2 Inhibitors for the Treatment of DDR2 Mutated Nonsmall Cell Lung Cancer.
Terai H et al.
Acs Chemical Biology, 2015
Molecular profiling of lung adenosquamous carcinoma: hybrid or genuine type?
Vassella E et al.
Oncotarget, 2015
Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor.
Henderson JL et al.
Journal of Medicinal Chemistry, 2015