Going for broke: targeting the human cancer pseudokinome (Q38307398)

2 September 2017

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title

Going for broke: targeting the human cancer pseudokinome (English)

1 reference

2 September 2017

Fiona P Bailey

1

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2 September 2017

Dominic P Byrne

2

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2 September 2017

Daniel McSkimming

3

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2 September 2017

Natarajan Kannan

4

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2 September 2017

Patrick A Eyers

5

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2 September 2017

language of work or name

English

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publication date

1 January 2015

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2 September 2017

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2 September 2017

volume

465

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2 September 2017

issue

2

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2 September 2017

page(s)

195-211

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Structural and functional diversity of the microbial kinome

2 September 2017

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

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Mutation that blocks ATP binding creates a pseudokinase stabilizing the scaffolding function of kinase suppressor of Ras, CRAF and BRAF

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New insights into the structure and function of the pseudokinase domain in JAK2.

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ATP and MO25α Regulate the Conformational State of the STRADα Pseudokinase and Activation of the LKB1 Tumour Suppressor

21 January 2018

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The pseudokinase MLKL mediates necroptosis via a molecular switch mechanism

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A conserved salt bridge in the G loop of multiple protein kinases is important for catalysis and for in vivo Lyn function.

21 January 2018

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Haspin-like proteins: a new family of evolutionarily conserved putative eukaryotic protein kinases

21 January 2018

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21 January 2018

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ErbB3/HER3 intracellular domain is competent to bind ATP and catalyze autophosphorylation

21 January 2018

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The pseudokinase domain of JAK2 is a dual-specificity protein kinase that negatively regulates cytokine signaling

21 January 2018

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CASK Functions as a Mg2+-independent neurexin kinase

21 January 2018

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SGK196 is a glycosylation-specific O-mannose kinase required for dystroglycan function

21 January 2018

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Affinity profiling of the cellular kinome for the nucleotide cofactors ATP, ADP, and GTP.

21 January 2018

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A public-private partnership to unlock the untargeted kinome

21 January 2018

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Receptor tyrosine kinases with intracellular pseudokinase domains

21 January 2018

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Pseudokinases-remnants of evolution or key allosteric regulators?

21 January 2018

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Structural analysis of the catalytically inactive kinase domain of the human EGF receptor 3

21 January 2018

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https://api.crossref.org/works/10.1042%2FBJ20141060

A central role for HER3 in HER2-amplified breast cancer: implications for targeted therapy

21 January 2018

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https://api.crossref.org/works/10.1042%2FBJ20141060

The ErbB2/ErbB3 heterodimer functions as an oncogenic unit: ErbB2 requires ErbB3 to drive breast tumor cell proliferation

21 January 2018

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https://api.crossref.org/works/10.1042%2FBJ20141060

An activated ErbB3/NRG1 autocrine loop supports in vivo proliferation in ovarian cancer cells

21 January 2018

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The rebirth of a phoenix: ovarian cancers are addicted to ErbB-3.

21 January 2018

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MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling

21 January 2018

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https://api.crossref.org/works/10.1042%2FBJ20141060

Dual targeting of EGFR and HER3 with MEHD7945A overcomes acquired resistance to EGFR inhibitors and radiation

21 January 2018

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https://api.crossref.org/works/10.1042%2FBJ20141060

Comprehensive analysis of kinase inhibitor selectivity

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Bosutinib versus imatinib in newly diagnosed chronic-phase chronic myeloid leukemia: results from the BELA trial

21 January 2018

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https://api.crossref.org/works/10.1042%2FBJ20141060

An ATP-Competitive Inhibitor Modulates the Allosteric Function of the HER3 Pseudokinase

21 January 2018

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https://api.crossref.org/works/10.1042%2FBJ20141060

Pseudokinase drug intervention: a potentially poisoned chalice.

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Comprehensive molecular characterization of human colon and rectal cancer

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Activating mutation in the tyrosine kinase JAK2 in polycythemia vera, essential thrombocythemia, and myeloid metaplasia with myelofibrosis

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

A unique clonal JAK2 mutation leading to constitutive signalling causes polycythaemia vera

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

A gain-of-function mutation of JAK2 in myeloproliferative disorders

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Acquired mutation of the tyrosine kinase JAK2 in human myeloproliferative disorders

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

The molecular regulation of Janus kinase (JAK) activation

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Regulation of the Jak2 tyrosine kinase by its pseudokinase domain

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

JAK2 exon 12 mutations in polycythemia vera and idiopathic erythrocytosis

21 January 2018

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https://api.crossref.org/works/10.1042%2FBJ20141060

Heterodimeric JAK-STAT activation as a mechanism of persistence to JAK2 inhibitor therapy

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Mechanism of activation of protein kinase JAK2 by the growth hormone receptor

21 January 2018

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https://api.crossref.org/works/10.1042%2FBJ20141060

Molecular basis for pseudokinase-dependent autoinhibition of JAK2 tyrosine kinase

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

SB1518, a novel macrocyclic pyrimidine-based JAK2 inhibitor for the treatment of myeloid and lymphoid malignancies.

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Ruxolitinib for myelofibrosis--an update of its clinical effects

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Discovery and characterization of LY2784544, a small-molecule tyrosine kinase inhibitor of JAK2V617F.

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

JAK2 the future: therapeutic strategies for JAK-dependent malignancies

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Regulation of WNK1 by an autoinhibitory domain and autophosphorylation

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Crystal structure of the kinase domain of WNK1, a kinase that causes a hereditary form of hypertension

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

WNK1, a novel mammalian serine/threonine protein kinase lacking the catalytic lysine in subdomain II

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Properties of WNK1 and implications for other family members

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Chloride Sensing by WNK1 Involves Inhibition of Autophosphorylation

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

WNK kinases, a novel protein kinase subfamily in multi-cellular organisms

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

WNK1 and OSR1 regulate the Na+, K+, 2Cl- cotransporter in HeLa cells

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

The WNK-SPAK/OSR1 pathway: master regulator of cation-chloride cotransporters

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

WNK1-OSR1 kinase-mediated phospho-activation of Na+-K+-2Cl- cotransporter facilitates glioma migration

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

LKB1 is a master kinase that activates 13 kinases of the AMPK subfamily, including MARK/PAR-1

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Structure of the LKB1-STRAD-MO25 complex reveals an allosteric mechanism of kinase activation

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Role of Lkb1, the causative gene of Peutz-Jegher's syndrome, in embryogenesis and polyposis

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Insights into the evolution of divergent nucleotide-binding mechanisms among pseudokinases revealed by crystal structures of human and mouse MLKL

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Mixed lineage kinase domain-like protein mediates necrosis signaling downstream of RIP3 kinase

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Kinases and pseudokinases: lessons from RAF.

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

The dual function of KSR1: a pseudokinase and beyond

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

C-TAK1 regulates Ras signaling by phosphorylating the MAPK scaffold, KSR1

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

KSR is a scaffold required for activation of the ERK/MAPK module

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

The protein kinase KSR interacts with 14-3-3 protein and Raf.

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

A Raf-induced allosteric transition of KSR stimulates phosphorylation of MEK

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Kinase suppressor of Ras signals through Thr269 of c-Raf-1.

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Kinase suppressor of Ras transphosphorylates c-Raf-1.

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Kinase suppressor of Ras-1 protects intestinal epithelium from cytokine-mediated apoptosis during inflammation

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Pharmacologic inactivation of kinase suppressor of ras-1 abrogates Ras-mediated pancreatic cancer

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

The molecular scaffold KSR1 regulates the proliferative and oncogenic potential of cells

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Kinase suppressor of ras 1 (KSR1) regulates PGC1α and estrogen-related receptor α to promote oncogenic Ras-dependent anchorage-independent growth

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Kinase suppressor of Ras 2 (KSR2) regulates tumor cell transformation via AMPK

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

The kinase domain of Drosophila Tribbles is required for turnover of fly C/EBP during cell migration.

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

The level of C/EBP protein is critical for cell migration during Drosophila oogenesis and is tightly controlled by regulated degradation

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Transformation by Tribbles homolog 2 (Trib2) requires both the Trib2 kinase domain and COP1 binding

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Overexpression of TRIB2 in human lung cancers contributes to tumorigenesis through downregulation of C/EBPα

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Human TRIB2 is a repressor of FOXO that contributes to the malignant phenotype of melanoma cells.

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

TRIB2 acts downstream of Wnt/TCF in liver cancer cells to regulate YAP and C/EBPα function

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Trib1 and Evi1 cooperate with Hoxa and Meis1 in myeloid leukemogenesis.

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Trib1 links the MEK1/ERK pathway in myeloid leukemogenesis

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Identification of TRIB1 R107L gain-of-function mutation in human acute megakaryocytic leukemia.

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Differential ability of Tribbles family members to promote degradation of C/EBPalpha and induce acute myelogenous leukemia

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Abnormal expression of TRIB3 in colorectal cancer: a novel marker for prognosis

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

High throughput kinase inhibitor screens reveal TRB3 and MAPK-ERK/TGFβ pathways as fundamental Notch regulators in breast cancer.

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Tribbles homolog 3 denotes a poor prognosis in breast cancer and is involved in hypoxia response.

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

TRIB3 mediates glucose-induced insulin resistance via a mechanism that requires the hexosamine biosynthetic pathway

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Deletion of STK40 protein in mice causes respiratory failure and death at birth

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

A novel protein tyrosine kinase NOK that shares homology with platelet- derived growth factor/fibroblast growth factor receptors induces tumorigenesis and metastasis in nude mice

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Point mutation at single tyrosine residue of novel oncogene NOK abrogates tumorigenesis in nude mice

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Overexpression of serine threonine tyrosine kinase 1/novel oncogene with kinase domain mRNA in patients with acute leukemia

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Diagnostic relevance of overexpressed mRNA of novel oncogene with kinase-domain (NOK) in lung cancers

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Aberrant STYK1 expression in ovarian cancer tissues and cell lines

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Overexpression of the potential kinase serine/ threonine/tyrosine kinase 1 (STYK 1) in castration-resistant prostate cancer

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

A novel gene STYK1/NOK is upregulated in estrogen receptor-alpha negative estrogen receptor-beta positive breast cancer cells following estrogen treatment

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

JAK2 V617F constitutive activation requires JH2 residue F595: a pseudokinase domain target for specific inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Oncogenic ERBB3 mutations in human cancers

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Paradoxical activation of Raf by a novel Raf inhibitor

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Identification of a Novel Family of BRAF V600E Inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

BRAFV600E: implications for carcinogenesis and molecular therapy

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Higher-Order Substrate Recognition of eIF2α by the RNA-Dependent Protein Kinase PKR

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Protein-protein interactions in the allosteric regulation of protein kinases

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

New mutations and pathogenesis of myeloproliferative neoplasms.

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Crystal structures of the JAK2 pseudokinase domain and the pathogenic mutant V617F

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Structure of the pseudokinase-kinase domains from protein kinase TYK2 reveals a mechanism for Janus kinase (JAK) autoinhibition

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Pseudokinases from a structural perspective

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

ROP2 from Toxoplasma gondii: a virulence factor with a protein-kinase fold and no enzymatic activity

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

The Pseudoactive Site of ILK Is Essential for Its Binding to α-Parvin and Localization to Focal Adhesions

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Biophysical and X-ray crystallographic analysis of Mps1 kinase inhibitor complexes

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Type-II kinase inhibitor docking, screening, and profiling using modified structures of active kinase states

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Evolution of CASK into a Mg2+-sensitive kinase

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Targeting Bcr–Abl by combining allosteric with ATP-binding-site inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Targeted covalent inactivation of protein kinases by resorcylic acid lactone polyketides.

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC.

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Developing irreversible inhibitors of the protein kinase cysteinome

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Ponatinib in Philadelphia chromosome-positive leukemias.

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Pharmacological targeting of the pseudokinase Her3

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Discovery of a novel and potent series of dianilinopyrimidineurea and urea isostere inhibitors of VEGFR2 tyrosine kinase

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

ProKinO: an ontology for integrative analysis of protein kinases in cancer

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

On the molecular mechanisms of mitotic kinase activation

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

A three-stage biophysical screening cascade for fragment-based drug discovery.

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Techniques to examine nucleotide binding by pseudokinases

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

The use of differential scanning fluorimetry to detect ligand interactions that promote protein stability

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

A fluorescence-based thermal shift assay identifies inhibitors of mitogen activated protein kinase kinase 4

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Selective inhibition of BET bromodomains

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Dual kinase-bromodomain inhibitors for rationally designed polypharmacology

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

Seeding collaborations to advance kinase science with the GSK Published Kinase Inhibitor Set (PKIS)

21 January 2018

1 reference

https://api.crossref.org/works/10.1042%2FBJ20141060

21 January 2018

Identifiers

DOI

10.1042/BJ20141060

1 reference

release_dtd3anrzxfgr3nq4q7uxsr7ouu

2 September 2017

Fatcat ID

1 reference

Fatcat

https://api.fatcat.wiki/v0/release/dtd3anrzxfgr3nq4q7uxsr7ouu

mapped directly with Wikidata item

24 November 2022

based on heuristic

1 reference