Associated Papers
Novel molecular mechanisms of FLT3 deregulation: from the acute myeloid leukemia experience to therapeutic insights in acute lymphoblastic leukemia.
Lo Schiavo F et al.
Molecular 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
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
Single-cell DNA and surface protein characterization of high hyperdiploid acute lymphoblastic leukemia at diagnosis and during treatment.
Aertgeerts M et al.
Hemasphere, 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
Suppression of Glioblastoma Stem Cell Potency and Tumor Growth via LRRK2 Inhibition.
Park S et al.
International Journal of Stem Cells, 2024
Alkynyl nicotinamides show antileukemic activity in drug-resistant acute myeloid leukemia.
Ramdas B et al.
The Journal of Clinical Investigation, 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
Current knowledge about FLT3 gene mutations, exploring the isoforms, and protein importance in AML.
Macečková D et al.
Molecular Biology Reports, 2024
Landscape of FLT3 Variations Associated with Structural and Functional Impact on Acute Myeloid Leukemia: A Computational Study.
Mirza Z et al.
International Journal of Molecular Sciences, 2024
Characterisation of FLT3 alterations in childhood acute lymphoblastic leukaemia.
Gutierrez-Camino A et al.
British Journal of Cancer, 2024
TP-0184 inhibits FLT3/ACVR1 to overcome FLT3 inhibitor resistance and hinder AML growth synergistically with venetoclax.
Tyagi A et al.
Leukemia, 2024
A Review of FLT3 Kinase Inhibitors in AML.
Negotei C et al.
Journal of Clinical Medicine, 2023
Indole-based FLT3 inhibitors and related scaffolds as potential therapeutic agents for acute myeloid leukemia.
Ezelarab HAA et al.
Bmc 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
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
Luxeptinib (CG-806) Targets FLT3 and Clusters of Kinases Operative in Acute Myeloid Leukemia.
Rice WG et al.
Molecular Cancer Therapeutics, 2022
Detection of oncogenic and clinically actionable mutations in cancer genomes critically depends on variant calling tools.
Garcia-Prieto CA et al.
Bioinformatics (oxford, England), 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
Developments and challenges of FLT3 inhibitors in acute myeloid leukemia.
Ge SS et al.
Frontiers in Oncology, 2022
Genomic Abnormalities as Biomarkers and Therapeutic Targets in Acute Myeloid Leukemia.
Ribeiro S et al.
Cancers, 2021
Deletions in FLT-3 juxtamembrane domain define a new class of pathogenic mutations: case report and systematic analysis.
Young DJ et al.
Blood Advances, 2021
Selectively targeting FLT3-ITD mutants over FLT3-wt by a novel inhibitor for acute myeloid leukemia.
Wang A et al.
Haematologica, 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
Targeting AML-associated FLT3 mutations with a type I kinase inhibitor.
Jones LM et al.
The Journal of Clinical Investigation, 2020
Exploiting loss of heterozygosity for allele-selective colorectal cancer chemotherapy.
Rendo V et al.
Nature Communications, 2020
A highly selective inhibitor of interleukin-1 receptor-associated kinases 1/4 (IRAK-1/4) delineates the distinct signaling roles of IRAK-1/4 and the TAK1 kinase.
Scarneo SA et al.
The Journal of Biological Chemistry, 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
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