Development of Selective Covalent Janus Kinase 3 Inhibitors. (Q38763094)

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22 February 2020

title

Development of Selective Covalent Janus Kinase 3 Inhibitors (English)

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22 February 2020

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22 February 2020

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22 February 2020

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22 February 2020

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22 February 2020

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22 February 2020

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22 February 2020

Nathanael S Gray

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22 February 2020

Li Tan

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22 February 2020

Koshi Akahane

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22 February 2020

Kathleen M S E Reyskens

1 reference

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22 February 2020

Scott B Ficarro

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22 February 2020

Suhu Liu

1 reference

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22 February 2020

Grit S Herter-Sprie

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22 February 2020

Liv Johannessen

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22 February 2020

David A Frank

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22 February 2020

Jarrod A Marto

1 reference

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22 February 2020

Thomas A Look

1 reference

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22 February 2020

J Simon C Arthur

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22 February 2020

Michael J Eck

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22 February 2020

language of work or name

English

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publication date

18 August 2015

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Journal of Medicinal Chemistry

22 February 2020

published in

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22 February 2020

volume

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22 February 2020

issue

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22 February 2020

page(s)

6589-6606

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The JAK-STAT pathway: impact on human disease and therapeutic intervention

22 February 2020

cites work

1 reference

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Mechanisms of Jak/STAT signaling in immunity and disease

6 September 2017

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Image-guided radiotherapy platform using single nodule conditional lung cancer mouse models

6 September 2017

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Therapy for myeloproliferative neoplasms: when, which agent, and how?

6 September 2017

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Covalent docking of large libraries for the discovery of chemical probes

6 September 2017

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6 September 2017

Selective JAK inhibitors

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Scaffold hopping towards potent and selective JAK3 inhibitors: discovery of novel C-5 substituted pyrrolopyrazines

6 September 2017

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The future of JAK inhibition in myelofibrosis and beyond

6 September 2017

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

6 September 2017

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Selective JAK inhibitors in development for rheumatoid arthritis

6 September 2017

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Janus kinase inhibitors for the treatment of myeloproliferative neoplasms.

6 September 2017

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Opposing actions of IL-2 and IL-21 on Th9 differentiation correlate with their differential regulation of BCL6 expression

6 September 2017

1 reference

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Discovery and development of Janus kinase (JAK) inhibitors for inflammatory diseases

6 September 2017

1 reference

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Inhibition of JAK3 with a novel, selective and orally active small molecule induces therapeutic response in T-cell malignancies

6 September 2017

1 reference

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Cross talk between the Akt and p38α pathways in macrophages downstream of Toll-like receptor signaling

6 September 2017

1 reference

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Discovery of a series of novel 5H-pyrrolo[2,3-b]pyrazine-2-phenyl ethers, as potent JAK3 kinase inhibitors

6 September 2017

1 reference

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TYK2-STAT1-BCL2 pathway dependence in T-cell acute lymphoblastic leukemia

6 September 2017

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Developing irreversible inhibitors of the protein kinase cysteinome

6 September 2017

1 reference

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Investigational Janus kinase inhibitors.

6 September 2017

1 reference

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Advances in the discovery of selective JAK inhibitors

6 September 2017

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Ibrutinib (PCI-32765), the first BTK (Bruton's tyrosine kinase) inhibitor in clinical trials

6 September 2017

1 reference

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3-Amido pyrrolopyrazine JAK kinase inhibitors: development of a JAK3 vs JAK1 selective inhibitor and evaluation in cellular and in vivo models

6 September 2017

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Inhibition of JAKs in macrophages increases lipopolysaccharide-induced cytokine production by blocking IL-10-mediated feedback

6 September 2017

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https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4777322

Inborn errors of human JAKs and STATs

6 September 2017

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The JAK-STAT pathway at twenty

6 September 2017

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Discovery of Potent and Selective Covalent Inhibitors of JNK

6 September 2017

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High-throughput kinase profiling: a more efficient approach toward the discovery of new kinase inhibitors

6 September 2017

1 reference

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Overview of the CCP4 suite and current developments

6 September 2017

1 reference

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Identification of a Potent Janus Kinase 3 Inhibitor with High Selectivity within the Janus Kinase Family

6 September 2017

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Discovery of CP-690,550: A Potent and Selective Janus Kinase (JAK) Inhibitor for the Treatment of Autoimmune Diseases and Organ Transplant Rejection

6 September 2017

1 reference

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Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function

6 September 2017

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Features and development of Coot

6 September 2017

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Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms

6 September 2017

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PHENIX: a comprehensive Python-based system for macromolecular structure solution

6 September 2017

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6 September 2017

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Novel mutant-selective EGFR kinase inhibitors against EGFR T790M

6 September 2017

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JAK3: a two-faced player in hematological disorders

6 September 2017

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New insights into the regulation of T cells by gamma(c) family cytokines

6 September 2017

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Phasercrystallographic software

6 September 2017

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mzAPI: a new strategy for efficiently sharing mass spectrometry data

6 September 2017

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CYT387, a selective JAK1/JAK2 inhibitor: in vitro assessment of kinase selectivity and preclinical studies using cell lines and primary cells from polycythemia vera patients

6 September 2017

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Janus kinases in immune cell signaling

6 September 2017

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Characterization of dasatinib and its structural analogs as CYP3A4 mechanism-based inactivators and the proposed bioactivation pathways

6 September 2017

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Structural biology of shared cytokine receptors

6 September 2017

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BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models

6 September 2017

1 reference

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High-throughput kinase profiling as a platform for drug discovery

6 September 2017

1 reference

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Hematopoietic cytokine receptor signaling

6 September 2017

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LKB1 modulates lung cancer differentiation and metastasis

6 September 2017

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Cytokine receptor signaling through the Jak-Stat-Socs pathway in disease.

6 September 2017

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Ba/F3 cells and their use in kinase drug discovery

6 September 2017

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Scaling and assessment of data quality

6 September 2017

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PRODRG: a tool for high-throughput crystallography of protein-ligand complexes

6 September 2017

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JAK/STAT signaling pathways and cancer. Janus kinases/signal transducers and activators of transcription.

6 September 2017

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Cytokine signaling in 2002: new surprises in the Jak/Stat pathway

6 September 2017

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Jak-STAT pathways and transcriptional activation in response to IFNs and other extracellular signaling proteins

6 September 2017

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Long-term Benefit of PD-L1 Blockade in Lung Cancer Associated with JAK3 Activation

6 September 2017

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Tricyclic covalent inhibitors selectively target Jak3 through an active site thiol.

6 September 2017

1 reference

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Activation of the PD-1 pathway contributes to immune escape in EGFR-driven lung tumors

6 September 2017

1 reference

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JAK3 deregulation by activating mutations confers invasive growth advantage in extranodal nasal-type natural killer cell lymphoma.

6 September 2017

1 reference

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Janus kinase 3-activating mutations identified in natural killer/T-cell lymphoma

6 September 2017

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Improved electrospray ionization efficiency compensates for diminished chromatographic resolution and enables proteomics analysis of tyrosine signaling in embryonic stem cells

6 September 2017

1 reference

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Kaempferol inhibits IL-4-induced STAT6 activation by specifically targeting JAK3.

14 September 2017

1 reference

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Activating alleles of JAK3 in acute megakaryoblastic leukemia

14 September 2017

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Transforming properties of chimeric TEL-JAK proteins in Ba/F3 cells

14 September 2017

1 reference

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Signaling by IL-2 and related cytokines: JAKs, STATs, and relationship to immunodeficiency

25 September 2017

1 reference

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A randomized, double-blind, placebo-controlled, twelve-week, dose-ranging study of decernotinib, an oral selective JAK-3 inhibitor, as monotherapy in patients with active rheumatoid arthritis

25 September 2017

1 reference

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Crystal structure of the Jak3 kinase domain in complex with a staurosporine analog

23 June 2018

1 reference

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A role for phospholipids in the binding and metabolism of drugs by hepatic microsomes. Use of the fluorescent hydrophobic probe 1-anilinonaphthalene-8-sulphonate

23 June 2018

1 reference

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Anilino-monoindolylmaleimides as potent and selective JAK3 inhibitors.

23 June 2018

1 reference

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Design and synthesis of tricyclic JAK3 inhibitors with picomolar affinities as novel molecular probes

31 August 2018

1 reference

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Newly described activating JAK3 mutations in T-cell acute lymphoblastic leukemia.

31 August 2018

1 reference

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Development and applications of a broad-coverage, TR-FRET-based kinase binding assay platform.

31 August 2018

1 reference

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Prevention of Organ Allograft Rejection by a Specific Janus Kinase 3 Inhibitor

31 August 2018

1 reference

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A universal algorithm for fast and automated charge state deconvolution of electrospray mass-to-charge ratio spectra.

31 August 2018

1 reference

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4-(3'-Bromo-4'hydroxylphenyl)-amino-6,7-dimethoxyquinazoline: a novel quinazoline derivative with potent cytotoxic activity against human glioblastoma cells.

31 August 2018

1 reference

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Development of pyrimidine-based inhibitors of Janus tyrosine kinase 3

31 August 2018

1 reference

PubMed

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inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Chemical and computational methods for the characterization of covalent reactive groups for the prospective design of irreversible inhibitors

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/26258521

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Identifiers

DOI

10.1021/ACS.JMEDCHEM.5B00710

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:26258521%20AND%20SRC:MED&resulttype=core&format=json

22 February 2020

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:26258521%20AND%20SRC:MED&resulttype=core&format=json

22 February 2020

PubMed publication ID

26258521

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:26258521%20AND%20SRC:MED&resulttype=core&format=json