A small molecule–kinase interaction map for clinical kinase inhibitors
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Summary
An efficient way to determine kinase inhibitor specificity by measuring binding of small molecules to the ATP site of kinases is described, which represents a systematic small molecule-protein interaction map for clinical compounds across a large number of related proteins.
- Type
- article
- Published
- 2005-03-01
- Cited by
- 1,905
- References
- 49
- Access
- Open access
- OpenAlex
- https://openalex.org/W2014582878
- Semantic Scholar
- https://api.semanticscholar.org/CorpusID:7780811
Keywords
Gefitinib, Small molecule, Kinase, Tyrosine kinase, Erlotinib
References
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- Induction of apoptosis and cell cycle arrest by CP-358,774, an inhibitor of epidermal growth factor receptor tyrosine kinase.
- PTK787/ZK 222584, a novel and potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases, impairs vascular endothelial growth factor-induced responses and tumor growth after oral administration.
- BCR-ABL gene mutations in relation to clinical resistance of Philadelphia-chromosome-positive leukaemia to STI571: a prospective study.
- High frequency of point mutations clustered within the adenosine triphosphate-binding region of BCR/ABL in patients with chronic myeloid leukemia or Ph-positive acute lymphoblastic leukemia who develop imatinib (STI571) resistance.
- Results of rectocele repair
- Bcr-Abl inhibition as a modality of CML therapeutics.
- Issues and progress with protein kinase inhibitors for cancer treatment
- Kinomics-structural biology and chemogenomics of kinase inhibitors and targets.
- Clinical Resistance to STI-571 Cancer Therapy Caused by BCR-ABL Gene Mutation or Amplification
- The specificities of protein kinase inhibitors: an update.
- Multiple BCR-ABL kinase domain mutations confer polyclonal resistance to the tyrosine kinase inhibitor imatinib (STI571) in chronic phase and blast crisis chronic myeloid leukemia.
- Effects of a selective inhibitor of the Abl tyrosine kinase on the growth of Bcr–Abl positive cells
- A highly specific inhibitor of human p38 MAP kinase binds in the ATP pocket
- The Protein Kinase Complement of the Human Genome
- A protein kinase involved in the regulation of inflammatory cytokine biosynthesis
- Dual-specific Src and Abl kinase inhibitors, PP1 and CGP76030, inhibit growth and survival of cells expressing imatinib mesylate-resistant Bcr-Abl kinases.
- Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.
Cited by
- Computational and experimental studies of protein kinase-inhibitor interactions
- Proteomics-based strategies in kinase drug discovery.
- The Eph/ephrin gene family in the european Amphioxus: an Evo-Devo approach
- Targeted covalent inactivation of protein kinases by resorcylic acid lactone polyketides.
- The JAK kinases: not just another kinase drug discovery target.
- Identification of a nonkinase target mediating cytotoxicity of novel kinase inhibitors
- Efficacy of Erlotinib for Brain and Leptomeningeal Metastases in Patients with Lung Adenocarcinoma Who Showed Initial Good Response to Gefitinib
- Molecular predictors of response to trastuzumab and lapatinib in breast cancer
- Comprehensive identification of staurosporine-binding kinases in the hepatocyte cell line HepG2 using Capture Compound Mass Spectrometry (CCMS).
- Lck is a key target of imatinib and dasatinib in T-cell activation
- Bevacizumab in combination with taxanes for the first-line treatment of metastatic breast cancer.
- Structure-activity relationships of benzimidazole-based selective inhibitors of the mitogen activated kinase-5 signaling pathway.
- Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).
- Development of a highly selective c-Src kinase inhibitor
- Multiplexed mass cytometry profiling of cellular states perturbed by small-molecule regulators
- A Targeted Library Screen Reveals a New Inhibitor Scaffold for Protein Kinase D
- Successful treatment of renal cell carcinoma with sorafenib after effective but hepatotoxic sunitinib exposure.
- Sorafenib Inhibits Lymphoma Xenografts by Targeting MAPK/ERK and AKT Pathways in Tumor and Vascular Cells
- erbB3 Is an Active Tyrosine Kinase Capable of Homo- and Heterointeractions
- Discovery of a Highly Selective STK16 Kinase Inhibitor.
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