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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
European Journal of Organic Chemistry, ISSN 1434-193X, 08/2014, Volume 2014, Issue 23, pp. 5063 - 5070
Journal Article
Journal of Biological Chemistry, ISSN 0021-9258, 03/2009, Volume 284, Issue 12, pp. 8023 - 8032
Journal Article
European Journal of Organic Chemistry, ISSN 1434-193X, 08/2014, Volume 2014, Issue 23, pp. 5063 - 5070
Journal Article
Nature, ISSN 0028-0836, 01/2010, Volume 463, Issue 7280, pp. 501 - 506
In an effort to find new pharmacological modalities to overcome resistance to ATP-binding-site inhibitors of Bcr-Abl, we recently reported the discovery of... 
CELL LUNG-CANCER | KINASE-INHIBITOR | SELECTIVE INHIBITOR | C-ABL | TYROSINE KINASE | MULTIDISCIPLINARY SCIENCES | DYNAMICS | MUTATIONS | LYMPHOBLASTIC-LEUKEMIA | IMATINIB RESISTANCE | CHRONIC MYELOID-LEUKEMIA | Humans | Leukemia, Myelogenous, Chronic, BCR-ABL Positive - drug therapy | Male | Transplantation, Heterologous | Piperazines - chemistry | Pyrimidines - chemistry | Pyrimidines - metabolism | Antineoplastic Agents - metabolism | Mass Spectrometry | Bone Marrow Transplantation | Inhibitory Concentration 50 | Female | Antineoplastic Agents - pharmacology | Binding Sites | Disease Models, Animal | Fusion Proteins, bcr-abl - chemistry | Leukemia, Myelogenous, Chronic, BCR-ABL Positive - enzymology | Protein Structure, Tertiary | Crystallization | Antineoplastic Combined Chemotherapy Protocols | Models, Molecular | Pyrimidines - pharmacology | Antineoplastic Agents - chemistry | Mutation - genetics | Imatinib Mesylate | Piperazines - pharmacology | Fusion Proteins, bcr-abl - genetics | Animals | Cell Line, Tumor | Leukemia, Myelogenous, Chronic, BCR-ABL Positive - metabolism | Mice | Benzamides | Fusion Proteins, bcr-abl - metabolism | Drug Resistance, Neoplasm - drug effects | Nilotinib | Dasatinib | Drug resistance in microorganisms | Usage | Nuclear magnetic resonance spectroscopy | Research | Chronic myeloid leukemia | X-ray crystallography | Chromosome abnormalities | Gene mutations | Analysis | Genetic aspects | Diagnosis | Binding proteins | Drug therapy | Health aspects | Proteins | Studies | Competition | Enzymes | E coli | Kinases | Drug resistance | Crystal structure | Index Medicus
Journal Article
Nature chemical biology, ISSN 1552-4450, 12/2014, Volume 10, Issue 12, pp. 1006 - 1012
Her3 (also known as ErbB3) belongs to the epidermal growth factor receptor tyrosine kinases and is well credentialed as an anti-cancer target but is thought to... 
ADJUVANT CHEMOTHERAPY | LUNG-CANCER | DOMAIN | PROTEIN | MET AMPLIFICATION | TYROSINE KINASE | BIOCHEMISTRY & MOLECULAR BIOLOGY | SELECTIVE INHIBITORS | EXTENDED 5-SUBSTITUENT | OVARIAN-CANCER | HER2-POSITIVE BREAST-CANCER | Proto-Oncogene Proteins c-met - metabolism | Adenine - chemical synthesis | Receptor, ErbB-2 - genetics | Antineoplastic Agents - chemical synthesis | Humans | Protein Multimerization | Receptor, ErbB-2 - chemistry | Gene Expression Regulation, Neoplastic | Receptor, ErbB-2 - metabolism | Molecular Targeted Therapy | Receptor, ErbB-3 - chemistry | Proteolysis | Adenosine Triphosphate - metabolism | Antineoplastic Agents - pharmacology | Acrylamides - pharmacology | Protein Kinase Inhibitors - chemical synthesis | Catalytic Domain | Adenine - analogs & derivatives | Signal Transduction | Receptor, ErbB-3 - antagonists & inhibitors | Adenine - pharmacology | Cysteine - chemistry | Receptor, ErbB-3 - genetics | Proto-Oncogene Proteins c-met - genetics | Cell Line, Tumor | Hydrophobic and Hydrophilic Interactions | Cell Proliferation - drug effects | Molecular Docking Simulation | Protein Kinase Inhibitors - pharmacology | Adamantane - chemistry | Proto-Oncogene Proteins c-met - chemistry | Adenosine Triphosphate - chemistry | Acrylamides - chemical synthesis | Signal transduction | Cell growth | Phosphorylation | Pharmacology | Epidermal growth factor | Kinases | Index Medicus
Journal Article
European Journal of Organic Chemistry, ISSN 1434-193X, 06/2015, Volume 2015, Issue 18, pp. 3963 - 3970
A highly stereoselective, concise (14 steps longest linear sequence and 20 steps overall), and efficient (15 % overall yield) synthesis of militarinone D has... 
Synthetic methods | Asymmetric synthesis | Nitrogen heterocycles | Natural products | PYRIDONE ALKALOIDS | METABOLITES | ASYMMETRIC-SYNTHESIS | TENELLIN | CHEMISTRY, ORGANIC | Enzymes | Synthesis | Aldehydes | Isomerization | Organic compounds | Owner operator
Journal Article
Clinical Cancer Research, ISSN 1078-0432, 01/2017, Volume 23, Issue 1, pp. 204 - 213
Purpose: Efforts to discover drugs that overcome resistance to targeted therapies in patients with rare oncogenic alterations, such as NTRK1 and ROS1... 
CABOZANTINIB | ONCOGENE | CRIZOTINIB RESISTANCE | ONCOLOGY | INHIBITOR | Drugs | Lung cancer | Extracellular signal-regulated kinase | Insulin-like growth factors | Tumor cell lines | Drug resistance | Drug development | Patients | Mutants | Metastases | AACR | Inhibitors | Experimental design | Inhibition | Aberration | Drug discovery | Target acquisition | Cancer | Index Medicus | drug screening
Journal Article