regorafenib and Leukemia--Myeloid--Acute

regorafenib has been researched along with Leukemia--Myeloid--Acute* in 2 studies

Other Studies

2 other study(ies) available for regorafenib and Leukemia--Myeloid--Acute

Article	Year
Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. Journal of medicinal chemistry, 2019, 12-26, Volume: 62, Issue:24 Gastrointestinal stromal tumors (GISTs) are prototypes of stem cell factor receptor (c-KIT)-driven cancer. Two receptor tyrosine kinases, c-KIT and fms-tyrosine kinase (FLT3), are frequently mutated in acute myeloid leukemia (AML) patients, and these mutations are associated with poor prognosis. In this study, we discovered a multitargeted tyrosine kinase inhibitor, compound Topics: Animals; Antineoplastic Agents; Apoptosis; Cell Proliferation; Female; fms-Like Tyrosine Kinase 3; Gastrointestinal Neoplasms; Gastrointestinal Stromal Tumors; Humans; Leukemia, Myeloid, Acute; Male; Mice; Mice, Inbred ICR; Mice, Inbred NOD; Mice, Nude; Mice, SCID; Mutation; Phosphorylation; Protein Kinase Inhibitors; Proto-Oncogene Proteins c-kit; Pyrimidines; Rats, Sprague-Dawley; Tumor Cells, Cultured; Xenograft Model Antitumor Assays	2019
The target landscape of clinical kinase drugs. Science (New York, N.Y.), 2017, 12-01, Volume: 358, Issue:6367 Kinase inhibitors are important cancer therapeutics. Polypharmacology is commonly observed, requiring thorough target deconvolution to understand drug mechanism of action. Using chemical proteomics, we analyzed the target spectrum of 243 clinically evaluated kinase drugs. The data revealed previously unknown targets for established drugs, offered a perspective on the "druggable" kinome, highlighted (non)kinase off-targets, and suggested potential therapeutic applications. Integration of phosphoproteomic data refined drug-affected pathways, identified response markers, and strengthened rationale for combination treatments. We exemplify translational value by discovering SIK2 (salt-inducible kinase 2) inhibitors that modulate cytokine production in primary cells, by identifying drugs against the lung cancer survival marker MELK (maternal embryonic leucine zipper kinase), and by repurposing cabozantinib to treat FLT3-ITD-positive acute myeloid leukemia. This resource, available via the ProteomicsDB database, should facilitate basic, clinical, and drug discovery research and aid clinical decision-making. Topics: Animals; Antineoplastic Agents; Cell Line, Tumor; Cytokines; Drug Discovery; fms-Like Tyrosine Kinase 3; Humans; Leukemia, Myeloid, Acute; Lung Neoplasms; Mice; Molecular Targeted Therapy; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proteomics; Xenograft Model Antitumor Assays	2017

Article

Year

Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia.

Journal of medicinal chemistry, 2019, 12-26, Volume: 62, Issue:24

Gastrointestinal stromal tumors (GISTs) are prototypes of stem cell factor receptor (c-KIT)-driven cancer. Two receptor tyrosine kinases, c-KIT and fms-tyrosine kinase (FLT3), are frequently mutated in acute myeloid leukemia (AML) patients, and these mutations are associated with poor prognosis. In this study, we discovered a multitargeted tyrosine kinase inhibitor, compound

Topics: Animals; Antineoplastic Agents; Apoptosis; Cell Proliferation; Female; fms-Like Tyrosine Kinase 3; Gastrointestinal Neoplasms; Gastrointestinal Stromal Tumors; Humans; Leukemia, Myeloid, Acute; Male; Mice; Mice, Inbred ICR; Mice, Inbred NOD; Mice, Nude; Mice, SCID; Mutation; Phosphorylation; Protein Kinase Inhibitors; Proto-Oncogene Proteins c-kit; Pyrimidines; Rats, Sprague-Dawley; Tumor Cells, Cultured; Xenograft Model Antitumor Assays

2019

The target landscape of clinical kinase drugs.

Science (New York, N.Y.), 2017, 12-01, Volume: 358, Issue:6367

Kinase inhibitors are important cancer therapeutics. Polypharmacology is commonly observed, requiring thorough target deconvolution to understand drug mechanism of action. Using chemical proteomics, we analyzed the target spectrum of 243 clinically evaluated kinase drugs. The data revealed previously unknown targets for established drugs, offered a perspective on the "druggable" kinome, highlighted (non)kinase off-targets, and suggested potential therapeutic applications. Integration of phosphoproteomic data refined drug-affected pathways, identified response markers, and strengthened rationale for combination treatments. We exemplify translational value by discovering SIK2 (salt-inducible kinase 2) inhibitors that modulate cytokine production in primary cells, by identifying drugs against the lung cancer survival marker MELK (maternal embryonic leucine zipper kinase), and by repurposing cabozantinib to treat FLT3-ITD-positive acute myeloid leukemia. This resource, available via the ProteomicsDB database, should facilitate basic, clinical, and drug discovery research and aid clinical decision-making.

Topics: Animals; Antineoplastic Agents; Cell Line, Tumor; Cytokines; Drug Discovery; fms-Like Tyrosine Kinase 3; Humans; Leukemia, Myeloid, Acute; Lung Neoplasms; Mice; Molecular Targeted Therapy; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proteomics; Xenograft Model Antitumor Assays

2017