Associated Papers
Design, Synthesis, and Biological Evaluation of the First Novel Macrocycle-Based FGFR Inhibitors That Overcome Clinically Acquired Resistance.
Xiang S et al.
Journal of Medicinal Chemistry, 2026
Harnessing genomic profiling for improved urothelial cancer outcomes.
Yu EM et al.
Expert Review of Anticancer Therapy, 2026
Saturation mutagenesis identifies activating and resistance-inducing FGFR kinase domain mutations.
Tangermann C et al.
Nature Genetics, 2026
Discriminating activating, deactivating and resistance variants in protein kinases.
Singh G et al.
Genome Medicine, 2025
Dabogratinib (TYRA-300), an FGFR3 isoform-selective inhibitor: preclinical and initial clinical evidence of anti-tumor activity.
Starrett JH et al.
Molecular Cancer Therapeutics, 2025
Rational Design and Identification of ISM7594 as a Tissue-Agnostic FGFR2/3 Inhibitor.
Wang Y et al.
Journal of Medicinal Chemistry, 2025
Discovery of Potent FGFR2/3 Inhibitors to Overcome Mutation Resistance and Treat Achondroplasia.
Fu D et al.
Acs Medicinal Chemistry Letters, 2025
Prevalence and biological impact of clinically relevant gene fusions in head and neck cancers.
Hoskins EL et al.
Npj Precision Oncology, 2025
Chromothripsis-Mediated Small Cell Lung Carcinoma.
Rekhtman N et al.
Cancer Discovery, 2025
Discovery of TYRA-300: First Oral Selective FGFR3 Inhibitor for the Treatment of Urothelial Cancers and Achondroplasia.
Hudkins RL et al.
Journal of Medicinal Chemistry, 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
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
A Tetravalent Bispecific Antibody Selectively Inhibits Diverse FGFR3 Oncogenic Variants.
Yang Y et al.
Cancer Research, 2024
The Irreversible FGFR Inhibitor KIN-3248 Overcomes FGFR2 Kinase Domain Mutations.
Balasooriya ER et al.
Clinical Cancer Research : an Official Journal of the American Association for Cancer Research, 2024
A Phase I Study of KIN-3248, an Irreversible Small-molecule Pan-FGFR Inhibitor, in Patients with Advanced FGFR2/3-driven Solid Tumors.
Garmezy B et al.
Cancer Research Communications, 2024
Pemigatinib for metastatic or surgically unresectable urothelial carcinoma with FGF/FGFR genomic alterations: final results from FIGHT-201.
Necchi A et al.
Annals of Oncology : Official Journal of the European Society for Medical Oncology, 2024
Structural basis and selectivity of sulfatinib binding to FGFR and CSF-1R.
Lin Q et al.
Communications Chemistry, 2024
FGFR families: biological functions and therapeutic interventions in tumors.
Liu Q et al.
Medcomm, 2023
Resistance to Selective FGFR Inhibitors in FGFR-Driven Urothelial Cancer.
Facchinetti F et al.
Cancer Discovery, 2023
Elucidating the potential effects of point mutations on FGFR3 inhibitor resistance via combined molecular dynamics simulation and community network analysis.
Liu B et al.
Journal of Computer-aided Molecular Design, 2023
Significance of the FGFR3 mutation in Chinese patients with bladder cancer.
Hao L et al.
Translational Andrology and Urology, 2023
Role of FGFR3 in bladder cancer: Treatment landscape and future challenges.
Ascione CM et al.
Cancer Treatment Reviews, 2023
Discovery of 2-Amino-7-sulfonyl-7H-pyrrolo[2,3-d]pyrimidine Derivatives as Potent Reversible FGFR Inhibitors with Gatekeeper Mutation Tolerance: Design, Synthesis, and Biological Evaluation.
Xie W et al.
Journal of Medicinal Chemistry, 2022
Targeting Gatekeeper Mutations for Kinase Drug Discovery.
Zhou Y et al.
Journal of Medicinal Chemistry, 2022
Characterization of the cholangiocarcinoma drug pemigatinib against FGFR gatekeeper mutants.
Lin Q et al.
Communications Chemistry, 2022
Molecularly Targeted Therapy towards Genetic Alterations in Advanced Bladder Cancer.
Thomas J et al.
Cancers, 2022
Targeted therapies: Expanding the role of FGFR3 inhibition in urothelial carcinoma.
Zengin ZB et al.
Urologic Oncology, 2022
Fibroblast Growth Factor Receptor 1-4 Genetic Aberrations as Clinically Relevant Biomarkers in Squamous Cell Lung Cancer.
Moes-Sosnowska J et al.
Frontiers in Oncology, 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
Intrinsic relative preference profile of pan-kinase inhibitor drug staurosporine towards the clinically occurring gatekeeper mutations in Protein Tyrosine Kinases.
Ren Z et al.
Computational Biology and Chemistry, 2021
Neuroblastoma Risk Assessment and Treatment Stratification with Hybrid Capture-Based Panel Sequencing.
Szymansky A et al.
Journal of Personalized Medicine, 2021
Insights of fibroblast growth factor receptor 3 aberrations in pan-cancer and their roles in potential clinical treatment.
Li J et al.
Aging, 2021
Identifying therapeutic drug targets using bidirectional effect genes.
Estrada K et al.
Nature Communications, 2021
Fibroblast growth factor receptors in cancer: genetic alterations, diagnostics, therapeutic targets and mechanisms of resistance.
Krook MA et al.
British Journal of Cancer, 2021
Ultradeep targeted sequencing of circulating tumor DNA in plasma of early and advanced breast cancer.
Chin YM et al.
Cancer Science, 2021
Therapeutics potentiating microglial p21-Nrf2 axis can rescue neurodegeneration caused by neuroinflammation.
Nakano-Kobayashi A et al.
Science Advances, 2020
Identification of pathogenic missense mutations using protein stability predictors.
Gerasimavicius L et al.
Scientific Reports, 2020
Detection of circulating tumor DNA in patients of operative colorectal and gastric cancers.
Suzuki T et al.
Oncotarget, 2020
A Novel FGFR3 Splice Variant Preferentially Expressed in African American Prostate Cancer Drives Aggressive Phenotypes and Docetaxel Resistance.
Olender J et al.
Molecular Cancer Research : Mcr, 2019
Germline susceptibility variants impact clinical outcome and therapeutic strategies for stage III colorectal cancer.
Lin PC et al.
Scientific Reports, 2019
Ensemble-Based Replica Exchange Alchemical Free Energy Methods: The Effect of Protein Mutations on Inhibitor Binding.
Bhati AP et al.
Journal of Chemical Theory and Computation, 2019