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Overview This group represents closely related cell-surface and intracellular tyrosine kinases, most of which mediate growth factor signaling pathways implicated in cancer, angiogenesis, and developmental processes. They are validated targets for a variety of kinase inhibitors, with extensive roles in oncological and vascular diseases. The provided list should be considered a "kinase inhibition profile" rather than a single molecular target. Structured curation should capture each as its own canonical entry for any structured data system.
Other names CD331 EC 2.7.10.1 CD333 KDR CD309 Kinase insert domain receptor FLK1 CD140a CD140b CD135 CD117 KIT Stem cell factor receptor FLT4 SRC avian sarcoma viral (v-src) oncogene homolog CD350 02
Mechanism of action ATP-competitive inhibition of kinase domains. Inhibition of downstream signaling leading to anti-proliferative, anti-angiogenic, and pro-apoptotic effects.
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Biological functions Signal transduction Cell proliferation Differentiation Angiogenesis Skeletal development Vascular permeability Wound healing Embryonic development Fibrogenesis Hematopoiesis Stem cell maintenance Melanogenesis Lymphangiogenesis Cell adhesion/motility Neural crest development
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Disease associations Cancer Glioblastoma Breast cancer Skeletal disorders Bladder cancer Multiple myeloma Skeletal dysplasia Wet age-related macular degeneration Diabetic retinopathy Glioma Sarcoma Fibrosis Cardiovascular disease Acute myeloid leukemia (AML) Hematological malignancies Gastrointestinal stromal tumors (GIST) Melanoma Lymphedema Metastatic spread Inflammatory disease Osteoporosis Thyroid cancer (medullary thyroid carcinoma) Multiple endocrine neoplasia
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Safety considerations Hyperphosphatemia Mucositis Off-target effects (cardiotoxicity, ocular toxicity) Skeletal defects (with germline targeting) On-target adverse effects Hypertension Thromboembolism Hemorrhage Proteinuria Myelosuppression Edema Cardiovascular effects Cardiotoxicity Blood dyscrasias QT prolongation Infections Cytopenias Skin pigmentation changes Hypersensitivity Lymphedema Vascular leakage Bleeding Retinopathy Acquired drug resistance Class effects: hematologic toxicity Class effects: hand-foot skin reaction
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Interacting drugs Dovitinib
17 more in the full profile.
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Biomarkers FGFR1 amplification/mutation FGFR3 mutation/fusion VEGFR2 expression/phosphorylation Circulating VEGF levels PDGFRA amplification/mutation PDGFRB amplification/mutation FLT3 internal tandem duplication (ITD) D835 mutations c-Kit expression KIT mutation (e.g., exon 11) VEGFR3 expression Lymphatic vessel density SRC activity Phosphorylation status RET mutation RET rearrangement Gene fusions (e.g., FGFR-TACC) Activating mutations Protein overexpression (e.g., c-Kit/CD117, PDGFRα amplification)
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