Non-kinase targets of protein kinase inhibitors (Q39171961)

9 September 2017

title

Non-kinase targets of protein kinase inhibitors (English)

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9 September 2017

Lenka Munoz

1

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9 September 2017

publication date

10 March 2017

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Nature Reviews Drug Discovery

9 September 2017

published in

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9 September 2017

volume

16

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9 September 2017

issue

6

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9 September 2017

page(s)

424-440

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Small-molecule kinase inhibitors: an analysis of FDA-approved drugs.

9 September 2017

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Stereospecific targeting of MTH1 by (S)-crizotinib as an anticancer strategy

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Assessing the Efficacy of Mdm2/Mdm4-Inhibiting Stapled Peptides Using Cellular Thermal Shift Assays.

21 January 2018

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The cellular thermal shift assay for evaluating drug target interactions in cells

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Proteomic profiling of small-molecule inhibitors reveals dispensability of MTH1 for cancer cell survival

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Tracking cancer drugs in living cells by thermal profiling of the proteome

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Erythropoietic protoporphyria

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Chemical Proteomics Reveals Ferrochelatase as a Common Off-target of Kinase Inhibitors

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Thermal proteome profiling monitors ligand interactions with cellular membrane proteins.

21 January 2018

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Proteome-wide drug and metabolite interaction mapping by thermal-stability profiling.

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A Programmable Dual-RNA-Guided DNA Endonuclease in Adaptive Bacterial Immunity

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21 January 2018

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21 January 2018

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CRISPR-Cas9-based target validation for p53-reactivating model compounds.

21 January 2018

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Going for broke: targeting the human cancer pseudokinome

21 January 2018

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Dawn of the dead: protein pseudokinases signal new adventures in cell biology

21 January 2018

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Survival of cancer cells is maintained by EGFR independent of its kinase activity

21 January 2018

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A kinase-independent role for EGF receptor in autophagy initiation

21 January 2018

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EGFR and EGFRvIII interact with PUMA to inhibit mitochondrial translocalization of PUMA and PUMA-mediated apoptosis independent of EGFR kinase activity.

21 January 2018

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RIPK1 maintains epithelial homeostasis by inhibiting apoptosis and necroptosis

21 January 2018

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Cutting edge: RIPK1 Kinase inactive mice are viable and protected from TNF-induced necroptosis in vivo

21 January 2018

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RIP3 induces apoptosis independent of pronecrotic kinase activity

21 January 2018

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Activity of protein kinase RIPK3 determines whether cells die by necroptosis or apoptosis

21 January 2018

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RIPK1 and RIPK3: critical regulators of inflammation and cell death

21 January 2018

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Selective 3-phosphoinositide-dependent kinase 1 (PDK1) inhibitors: dissecting the function and pharmacology of PDK1.

21 January 2018

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Akt is efficiently activated by PIF-pocket- and PtdIns(3,4,5)P3-dependent mechanisms leading to resistance to PDK1 inhibitors

21 January 2018

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PDK1 attenuation fails to prevent tumor formation in PTEN-deficient transgenic mouse models.

21 January 2018

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Substrate-selective inhibition of protein kinase PDK1 by small compounds that bind to the PIF-pocket allosteric docking site

21 January 2018

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A small-molecule mimic of a peptide docking motif inhibits the protein kinase PDK1.

21 January 2018

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Chemoresistance of endothelial cells induced by basic fibroblast growth factor depends on Raf-1-mediated inhibition of the proapoptotic kinase, ASK1.

21 January 2018

1 reference

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Kinase-independent role for CRAF-driving tumour radioresistance via CHK2

21 January 2018

1 reference

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Structure of the BRAF-MEK complex reveals a kinase activity independent role for BRAF in MAPK signaling

21 January 2018

1 reference

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A MEK-independent role for CRAF in mitosis and tumor progression.

21 January 2018

1 reference

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Kinase-independent function of checkpoint kinase 1 (Chk1) in the replication of damaged DNA.

21 January 2018

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A genetically selective inhibitor demonstrates a function for the kinase Zap70 in regulatory T cells independent of its catalytic activity

21 January 2018

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Function of Bruton's tyrosine kinase during B cell development is partially independent of its catalytic activity.

21 January 2018

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A kinase-independent function of AKT promotes cancer cell survival

21 January 2018

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Nuclear AURKA acquires kinase-independent transactivating function to enhance breast cancer stem cell phenotype

21 January 2018

1 reference

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Chemical genetics reveals a kinase-independent role for protein kinase R in pyroptosis

21 January 2018

1 reference

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The secret life of kinases: functions beyond catalysis

21 January 2018

1 reference

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Molecular determinants of the response of glioblastomas to EGFR kinase inhibitors.

21 January 2018

1 reference

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Activation of the pseudokinase MLKL unleashes the four-helix bundle domain to induce membrane localization and necroptotic cell death

21 January 2018

1 reference

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A Small Molecule RAS-Mimetic Disrupts RAS Association with Effector Proteins to Block Signaling

21 January 2018

1 reference

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Allosteric modulation of AURKA kinase activity by a small-molecule inhibitor of its protein-protein interaction with TPX2

21 January 2018

1 reference

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Tackling reproducibility in academic preclinical drug discovery

21 January 2018

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The promise and peril of chemical probes

21 January 2018

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Chemical biology approaches to target validation in cancer

21 January 2018

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Chemistry: Chemical con artists foil drug discovery

21 January 2018

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Feeling Nature's PAINS: Natural Products, Natural Product Drugs, and Pan Assay Interference Compounds (PAINS).

21 January 2018

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Know your target, know your molecule

21 January 2018

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New substructure filters for removal of pan assay interference compounds (PAINS) from screening libraries and for their exclusion in bioassays

21 January 2018

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Fluid shear triggers microvilli formation via mechanosensitive activation of TRPV6

21 January 2018

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Identification of potent and selective MTH1 inhibitors

21 January 2018

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Validation and development of MTH1 inhibitors for treatment of cancer.

21 January 2018

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Application of proteomic profiling based on 2D-DIGE for classification of compounds according to the mechanism of action

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Methyl 3-((6-methoxy-1,4-dihydroindeno[1,2-c]pyrazol-3-yl)amino)benzoate (GN39482) as a tubulin polymerization inhibitor identified by MorphoBase and ChemProteoBase profiling methods.

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Management of crizotinib therapy for ALK-rearranged non-small cell lung carcinoma: an expert consensus.

21 January 2018

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Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes

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The Connectivity Map: using gene-expression signatures to connect small molecules, genes, and disease

21 January 2018

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The Connectivity Map: a new tool for biomedical research

21 January 2018

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An interactive resource to identify cancer genetic and lineage dependencies targeted by small molecules.

21 January 2018

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Harnessing Connectivity in a Large-Scale Small-Molecule Sensitivity Dataset.

21 January 2018

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Correlating chemical sensitivity and basal gene expression reveals mechanism of action.

21 January 2018

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IC261, a specific inhibitor of the protein kinases casein kinase 1-delta and -epsilon, triggers the mitotic checkpoint and induces p53-dependent postmitotic effects

21 January 2018

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The stress-responsive kinases MAPKAPK2/MAPKAPK3 activate starvation-induced autophagy through Beclin 1 phosphorylation

31 March 2020

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Molecular basis for p38 protein kinase inhibitor specificity

31 March 2020

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Crystal structure, biochemical and cellular activities demonstrate separate functions of MTH1 and MTH2

31 March 2020

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31 March 2020

Identifiers

DOI

10.1038/NRD.2016.266

1 reference

9 September 2017

1 reference