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Proceedings of the National Academy of Sciences, ISSN 0027-8424, 11/2014, Volume 111, Issue 45, pp. E4869 - E4877
The human FGF receptors (FGFRs) play critical roles in various human cancers, and several FGFR inhibitors are currently under clinical investigation.... 
Structure-based drug design | Drug discovery | Cancer drug resistance | Kinase inhibitor | structure-based drug design | WILD-TYPE | MULTIDISCIPLINARY SCIENCES | BCR-ABL | GROWTH-FACTOR RECEPTORS | DRUG-RESISTANCE | kinase inhibitor | LUNG-CANCER | GENE FUSIONS | cancer drug resistance | SELECTIVE INHIBITOR | drug discovery | THERAPEUTIC TARGET | FACTOR RECEPTOR 4 | REGULATES PROLIFERATION | Receptor, Fibroblast Growth Factor, Type 4 - chemistry | Receptor, Epidermal Growth Factor - genetics | Receptor, Fibroblast Growth Factor, Type 4 - metabolism | Receptor, Fibroblast Growth Factor, Type 2 - chemistry | Receptor, Fibroblast Growth Factor, Type 2 - metabolism | Humans | Receptor, Fibroblast Growth Factor, Type 1 - metabolism | Crystallography, X-Ray | Structure-Activity Relationship | Mutation, Missense | Receptor, Fibroblast Growth Factor, Type 1 - genetics | Protein Kinase Inhibitors - chemistry | Receptor, Epidermal Growth Factor - metabolism | Neoplasms - genetics | Receptor, Fibroblast Growth Factor, Type 2 - antagonists & inhibitors | Antineoplastic Agents - pharmacology | Receptor, Fibroblast Growth Factor, Type 4 - genetics | Binding Sites | Neoplasms - enzymology | Antineoplastic Agents - chemistry | Receptor, Fibroblast Growth Factor, Type 1 - antagonists & inhibitors | Receptor, Epidermal Growth Factor - chemistry | Neoplasms - drug therapy | Drug Resistance, Neoplasm - genetics | Cell Line, Tumor | Receptor, Epidermal Growth Factor - antagonists & inhibitors | Protein Kinase Inhibitors - pharmacology | Receptor, Fibroblast Growth Factor, Type 1 - chemistry | Neoplasms - pathology | Receptor, Fibroblast Growth Factor, Type 4 - antagonists & inhibitors | Receptor, Fibroblast Growth Factor, Type 2 - genetics | Amino Acid Substitution | Drug Resistance, Neoplasm - drug effects | Amino acids | T cell receptors | Mutation | Kinases | Binding sites | Adenosine triphosphatase | Index Medicus | Biological Sciences | PNAS Plus
Journal Article
Science, ISSN 0036-8075, 9/2012, Volume 337, Issue 6099, pp. 1231 - 1235
The brain tumor glioblastoma multiforme (GBM) is among the most lethal forms of human cancer. Here, we report that a small subset of GBMs (3.1%; 3 of 97 tumors... 
Exons | Neurons | Genes | REPORTS | Stem cells | Aneuploidy | Chromosomes | Cells | Tumors | Daughter cells | Cancer | ANEUPLOIDY | SELECTIVE INHIBITOR | POTENT | MULTIDISCIPLINARY SCIENCES | CANCER | RECEPTOR TYROSINE KINASE | DISCOVERY | CHROMOSOMAL INSTABILITY | FAMILY | Microtubule-Associated Proteins - chemistry | Neoplasm Transplantation | Translocation, Genetic | Oncogene Proteins, Fusion - metabolism | Receptor, Fibroblast Growth Factor, Type 3 - chemistry | Microtubule-Associated Proteins - genetics | Microtubule-Associated Proteins - metabolism | Mitosis | Humans | Receptor, Fibroblast Growth Factor, Type 1 - metabolism | Receptor, Fibroblast Growth Factor, Type 3 - antagonists & inhibitors | Fetal Proteins - metabolism | Receptor, Fibroblast Growth Factor, Type 1 - genetics | Receptor, Fibroblast Growth Factor, Type 3 - metabolism | Brain Neoplasms - metabolism | Oncogene Proteins, Fusion - chemistry | Spindle Apparatus - metabolism | Glioblastoma - genetics | Oncogene Fusion | Glioblastoma - metabolism | Antineoplastic Agents - pharmacology | Benzamides - pharmacology | Nuclear Proteins - genetics | Chromosomal Instability | Pyrazoles - pharmacology | Protein Structure, Tertiary | Receptor, Fibroblast Growth Factor, Type 3 - genetics | Enzyme Inhibitors - pharmacology | Brain Neoplasms - genetics | Nuclear Proteins - metabolism | Pyrimidines - pharmacology | Nuclear Proteins - chemistry | Piperazines - pharmacology | Receptor, Fibroblast Growth Factor, Type 1 - antagonists & inhibitors | Xenograft Model Antitumor Assays | Animals | Cell Transformation, Neoplastic | Oncogene Proteins, Fusion - genetics | Fetal Proteins - genetics | Mice | Receptor, Fibroblast Growth Factor, Type 1 - chemistry | Fetal Proteins - chemistry | Physiological aspects | Development and progression | Fibroblast growth factors | Genetic aspects | Research | Health aspects | Glioblastoma multiforme | Proteins | Kinases | Brain cancer | Genomics | Pharmaceutical sciences | Index Medicus
Journal Article
Cancer Discovery, ISSN 2159-8274, 12/2012, Volume 2, Issue 12, pp. 1118 - 1133
Journal Article
Clinical Cancer Research, ISSN 1078-0432, 07/2013, Volume 19, Issue 13, pp. 3693 - 3702
Journal Article
Oncogene, ISSN 0950-9232, 06/2013, Volume 32, Issue 25, pp. 3059 - 3070
Fibroblast growth factor receptors (FGFRs) can act as driving oncoproteins in certain cancers, making them attractive drug targets. Here we have characterized... 
tyrosine kinase inhibitors | ERK1/2 | FGFR | PKB | acquired resistance | MULTIPLE-MYELOMA | BLADDER-CANCER | PHOSPHORYLATION | PROTEIN-KINASE | BIOCHEMISTRY & MOLECULAR BIOLOGY | STOMACH-CANCER | LINES | CELL BIOLOGY | C/EBP-ALPHA | AMPLIFICATION | GENE | ONCOLOGY | GASTRIC-CANCER | GENETICS & HEREDITY | Receptor, Fibroblast Growth Factor, Type 2 - metabolism | Humans | Receptor, Fibroblast Growth Factor, Type 1 - metabolism | Receptor, Fibroblast Growth Factor, Type 3 - antagonists & inhibitors | Multiple Myeloma - drug therapy | Receptor Protein-Tyrosine Kinases - antagonists & inhibitors | Female | Receptor, Fibroblast Growth Factor, Type 2 - antagonists & inhibitors | Antineoplastic Agents - pharmacology | Benzamides - pharmacology | Pyrazoles - pharmacology | Receptor, Fibroblast Growth Factor, Type 3 - genetics | Receptors, Fibroblast Growth Factor - antagonists & inhibitors | Pyrimidines - pharmacology | Stomach Neoplasms - drug therapy | Urinary Bladder Neoplasms - drug therapy | Receptor Protein-Tyrosine Kinases - drug effects | Breast Neoplasms - drug therapy | Piperazines - pharmacology | Receptor, Fibroblast Growth Factor, Type 1 - antagonists & inhibitors | Neoplasms - drug therapy | Drug Resistance, Neoplasm - genetics | Signal Transduction - drug effects | Receptors, Fibroblast Growth Factor - metabolism | Cell Line, Tumor | Mutation | Multiple Myeloma - genetics | Gene mutations | Analysis | Physiological aspects | Genetic aspects | Fibroblast growth factors | Research | Health aspects | Fibroblast growth factor receptors | Proteins | Signal transduction | Inhibitor drugs | Gene expression | Cancer | Index Medicus
Journal Article
Journal Article
Gut, ISSN 0017-5749, 03/2017, Volume 66, Issue 3, pp. 530 - 540
ObjectiveSorafenib is effective in hepatocellular carcinoma (HCC), but patients ultimately present disease progression. Molecular mechanisms underlying... 
molecular genetics | stem cells | Hepatocellular carcinoma | molecular mechanisms | drug resistance | GROWTH-FACTOR RECEPTOR | CLASSIFICATION | ACTIVATION | INHIBITION | GASTROENTEROLOGY & HEPATOLOGY | MUTATION | Niacinamide - analogs & derivatives | Humans | Receptor, Fibroblast Growth Factor, Type 1 - metabolism | Fibroblast Growth Factors - genetics | Drug Resistance, Neoplasm | Male | Antineoplastic Agents - therapeutic use | Gene Expression Profiling | Fibroblast Growth Factors - metabolism | Carcinoma, Hepatocellular - drug therapy | Somatomedins - antagonists & inhibitors | Female | Liver Neoplasms - pathology | Spheroids, Cellular | Somatomedins - metabolism | Gene Expression | Signal Transduction | Liver Neoplasms - drug therapy | Niacinamide - therapeutic use | Phenylurea Compounds - therapeutic use | Survival Rate | Receptor, Fibroblast Growth Factor, Type 1 - antagonists & inhibitors | Disease Progression | Xenograft Model Antitumor Assays | Animals | Receptors, Somatomedin - metabolism | Somatomedins - genetics | Carcinoma, Hepatocellular - pathology | Liver Neoplasms - metabolism | Cell Line, Tumor | Aged | Mice | Mice, Inbred BALB C | Fibroblast Growth Factors - antagonists & inhibitors | Receptors, Somatomedin - antagonists & inhibitors | Carcinoma, Hepatocellular - metabolism | Fibroblast growth factors | Hepatoma | Research | Insulin-like growth factor 1 | Index Medicus | Abridged Index Medicus | Liver cancer | Càncer de fetge | Antineoplastic agents | Medicaments antineoplàstics
Journal Article
Clinical Cancer Research, ISSN 1078-0432, 10/2017, Volume 23, Issue 20, pp. 6138 - 6151
Purpose: FGFR1 amplification occurs in approximately 15% of estrogen receptor-positive (ER+) human breast cancers. Weinvestigated mechanisms by which FGFR1... 
AMPLIFICATION | PROTEIN | ONCOLOGY | THERAPEUTIC TARGET | GENES | ENDOCRINE THERAPY | FACTOR RECEPTOR-1 | FIBROBLAST-GROWTH-FACTOR | SIGNALING MODULE | EXPRESSION | NUCLEAR TRANSLOCATION | Humans | Gene Expression Regulation, Neoplastic | Receptor, Fibroblast Growth Factor, Type 1 - metabolism | Fibroblast Growth Factors - genetics | Molecular Targeted Therapy | Receptor, Fibroblast Growth Factor, Type 1 - genetics | Breast Neoplasms - metabolism | Fibroblast Growth Factors - metabolism | Estrogen Receptor alpha - metabolism | Female | Transcription, Genetic | Disease Models, Animal | Estrogen Receptor alpha - antagonists & inhibitors | Breast Neoplasms - drug therapy | Receptor, Fibroblast Growth Factor, Type 1 - antagonists & inhibitors | Estrogen Receptor Modulators - pharmacology | Protein Transport | Drug Resistance, Neoplasm - genetics | Animals | Breast Neoplasms - genetics | Estrogen Receptor alpha - genetics | Gene Amplification | Signal Transduction - drug effects | Breast Neoplasms - pathology | Cell Line, Tumor | Mice | Protein Kinase Inhibitors - pharmacology | Neoplasm Staging | Cell proliferation | Fibroblast growth factor | Transcription | Genes | Estrogens | Estrogen | Estrogen receptors | Antagonists | Kinases | Nuclei | Fulvestrant | Gene sequencing | E2F protein | Surgery | Xenografts | Inhibition | Fibroblast growth factor receptor 1 | Protein-tyrosine kinase | Deoxyribonucleic acid--DNA | Binding | Tyrosine | Deprivation | Breast cancer | siRNA | Gene expression | Patients | Polymerase chain reaction | Amplification | Ribonucleic acids | Experimental design | Breast | Ligands | Nuclei (cytology) | Tumors | Cancer | Fibroblast growth factor receptors | Index Medicus | breast cancer | drug resistance | fulvestrant | FGFR1
Journal Article
Journal Article
European Journal of Medicinal Chemistry, ISSN 0223-5234, 07/2017, Volume 135, pp. 531 - 543
A series of 2-oxo-3, 4-dihydropyrimido[4,5- ]-pyrimidinyl derivatives were designed and synthesized as new irreversible inhibitors of the FGFR family. One of... 
FGFR | Irreversible inhibitor | 2-Oxo-3,4-dihydropyrimido[4, 5-d]pyrimidinyl derivatives | CHEMISTRY, MEDICINAL | DISCOVERY | FAMILY | AZD4547 | 2-Oxo-3,4-dihydropyrimido[4,5-d]pyrimidinyl derivatives | SELECTIVE INHIBITOR | POTENT | PATHWAY | REACTIVATION | RESISTANCE | TYROSINE KINASE INHIBITOR | TARGETING FGFR | Cell Line | Protein Kinase Inhibitors - chemical synthesis | Receptor, Fibroblast Growth Factor, Type 4 - metabolism | Receptor, Fibroblast Growth Factor, Type 2 - metabolism | Pyrimidines - chemical synthesis | Antineoplastic Agents - chemical synthesis | Humans | Receptor, Fibroblast Growth Factor, Type 1 - metabolism | Receptor, Fibroblast Growth Factor, Type 3 - antagonists & inhibitors | Structure-Activity Relationship | Pyrimidines - pharmacology | Antineoplastic Agents - chemistry | Receptor, Fibroblast Growth Factor, Type 1 - antagonists & inhibitors | Receptor, Fibroblast Growth Factor, Type 3 - metabolism | Pyrimidines - chemistry | Dose-Response Relationship, Drug | Protein Kinase Inhibitors - chemistry | Receptor, Fibroblast Growth Factor, Type 2 - antagonists & inhibitors | Antineoplastic Agents - pharmacology | Cell Proliferation - drug effects | Molecular Structure | Protein Kinase Inhibitors - pharmacology | Receptor, Fibroblast Growth Factor, Type 4 - antagonists & inhibitors | Drug Screening Assays, Antitumor | Fibroblast growth factors | Enzyme inhibitors | Drug discovery | Lung cancer, Non-small cell | Derivatives (Financial instruments) | Resveratrol | Index Medicus
Journal Article
PLoS ONE, ISSN 1932-6203, 2011, Volume 6, Issue 6, pp. e20351 - e20351
Background: Squamous cell lung carcinomas account for approximately 25% of new lung carcinoma cases and 40,000 deaths per year in the United States. Although... 
MULTIPLE-MYELOMA | GEFITINIB | GENE | TRASTUZUMAB | MULTIDISCIPLINARY SCIENCES | THERAPEUTIC TARGET | RESISTANCE | CARCINOMAS | RECEPTOR | OVARIAN-CANCER | ACTIVATING MUTATIONS | Carcinoma, Non-Small-Cell Lung - pathology | Lung Neoplasms - genetics | Cell Survival - drug effects | Lung Neoplasms - enzymology | Carcinoma, Non-Small-Cell Lung - genetics | Humans | Genetic Loci - genetics | Receptor, Fibroblast Growth Factor, Type 1 - metabolism | 3' Untranslated Regions - genetics | Lung Neoplasms - pathology | Open Reading Frames - genetics | Receptor, Fibroblast Growth Factor, Type 1 - antagonists & inhibitors | Gene Knockdown Techniques | Gene Amplification - drug effects | Cell Line, Tumor | Cell Proliferation - drug effects | Protein Kinase Inhibitors - pharmacology | Carcinoma, Non-Small-Cell Lung - enzymology | RNA, Small Interfering - metabolism | Care and treatment | Analysis | Oncology, Experimental | Lung cancer, Small cell | Research | Lung cancer, Non-small cell | Health aspects | Cancer | Adenocarcinoma | Lung cancer | Oncology | Single-nucleotide polymorphism | Kinases | Medical schools | Clinical outcomes | Ovarian cancer | Rodents | Fibroblasts | Fibroblast growth factor receptor 1 | Growth factors | Squamous cell carcinoma | Small cell lung carcinoma | Non-small cell lung carcinoma | Lung carcinoma | Bladder cancer | Patients | Esophagus | Amplification | Chromosome 8 | Mutation | Fibroblast growth factor receptors | Tumors | Index Medicus
Journal Article