(Q35181271)

7 August 2017

title

Bruton's TK inhibitors: structural insights and evolution of clinical candidates (English)

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7 August 2017

Li Xing

1

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7 August 2017

Adrian Huang

series ordinal

2

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7 August 2017

publication date

1 April 2014

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Future Medicinal Chemistry

7 August 2017

published in

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7 August 2017

volume

6

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7 August 2017

issue

6

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7 August 2017

page(s)

675-695

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Bruton's tyrosine kinase: cell biology, sequence conservation, mutation spectrum, siRNA modifications, and expression profiling.

7 August 2017

cites work

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Bruton's tyrosine kinase as a molecular target in treatment of leukemias and lymphomas as well as inflammatory disorders and autoimmunity

21 January 2018

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B-cell targeting in rheumatoid arthritis and other autoimmune diseases

21 January 2018

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Role of Bruton's tyrosine kinase in B cell development

21 January 2018

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Signaling network of the Btk family kinases

21 January 2018

1 reference

Tyrosine kinases and their substrates in B lymphocytes

21 January 2018

1 reference

Bruton's tyrosine kinase (Btk): function, regulation, and transformation with special emphasis on the PH domain

21 January 2018

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BLNK mediates Syk-dependent Btk activation

21 January 2018

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Altered B-cell receptor signaling kinetics distinguish human follicular lymphoma B cells from tumor-infiltrating nonmalignant B cells

21 January 2018

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B cell signaling and tumorigenesis

21 January 2018

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Deficient expression of a B cell cytoplasmic tyrosine kinase in human X-linked agammaglobulinemia

21 January 2018

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The gene involved in X-linked agammaglobulinaemia is a member of the src family of protein-tyrosine kinases

21 January 2018

1 reference

Mutation of unique region of Bruton's tyrosine kinase in immunodeficient XID mice

21 January 2018

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Translational Mini-Review Series on B Cell-Directed Therapies: The pathogenic role of B cells in autoantibody-associated autoimmune diseases--lessons from B cell-depletion therapy

21 January 2018

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Efficacy of B-cell-targeted therapy with rituximab in patients with rheumatoid arthritis

21 January 2018

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Sustained improvement in rheumatoid arthritis following a protocol designed to deplete B lymphocytes

21 January 2018

1 reference

Drug discovery: New Btk inhibitor holds promise.

21 January 2018

1 reference

Specific Btk inhibition suppresses B cell– and myeloid cell–mediated arthritis

21 January 2018

1 reference

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

Discovery of selective irreversible inhibitors for Bruton's tyrosine kinase

21 January 2018

1 reference

Targeted covalent drugs of the kinase family

21 January 2018

1 reference

The Bruton tyrosine kinase inhibitor PCI-32765 ameliorates autoimmune arthritis by inhibition of multiple effector cells

21 January 2018

1 reference

Bruton tyrosine kinase inhibitor ibrutinib (PCI-32765) has significant activity in patients with relapsed/refractory B-cell malignancies

21 January 2018

1 reference

Trial watch: BTK inhibitor shows positive results in B cell malignancies.

21 January 2018

1 reference

Inhibition of Btk with CC-292 provides early pharmacodynamic assessment of activity in mice and humans

21 January 2018

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The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib

21 January 2018

1 reference

Chronic active B-cell-receptor signalling in diffuse large B-cell lymphoma

21 January 2018

1 reference

The evolution of protein kinase inhibitors from antagonists to agonists of cellular signaling

21 January 2018

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Targeting the unactivated conformations of protein kinases for small molecule drug discovery

21 January 2018

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Mechanism of activation of the RAF-ERK signaling pathway by oncogenic mutations of B-RAF

21 January 2018

1 reference

A unique structure for epidermal growth factor receptor bound to GW572016 (Lapatinib): relationships among protein conformation, inhibitor off-rate, and receptor activity in tumor cells

21 January 2018

1 reference

Crystal structure of Bruton's tyrosine kinase domain suggests a novel pathway for activation and provides insights into the molecular basis of X-linked agammaglobulinemia

21 January 2018

1 reference

Insights into the conformational flexibility of Bruton's tyrosine kinase from multiple ligand complex structures

21 January 2018

1 reference

Structural basis for the autoinhibition of calcium/calmodulin-dependent protein kinase I

21 January 2018

1 reference

Crystal structures of c-Src reveal features of its autoinhibitory mechanism

21 January 2018

1 reference

Crystal structure of Hck in complex with a Src family-selective tyrosine kinase inhibitor

21 January 2018

1 reference

Crystal structures of IL-2-inducible T cell kinase complexed with inhibitors: insights into rational drug design and activity regulation

21 January 2018

1 reference

Bruton's tyrosine kinase inhibitors: approaches to potent and selective inhibition, preclinical and clinical evaluation for inflammatory diseases and B cell malignancies

21 January 2018

1 reference

Crystal structure of the EphA4 protein tyrosine kinase domain in the apo- and dasatinib-bound state

21 January 2018

1 reference

Crystal structures of the Lyn protein tyrosine kinase domain in its Apo- and inhibitor-bound state

21 January 2018

1 reference

X-ray crystal structure of bone marrow kinase in the x chromosome: a Tec family kinase

21 January 2018

1 reference

Hybrid compound design to overcome the gatekeeper T338M mutation in cSrc

21 January 2018

1 reference

The structure of Dasatinib (BMS-354825) bound to activated ABL kinase domain elucidates its inhibitory activity against imatinib-resistant ABL mutants

21 January 2018

1 reference

The crystal structure of a c-Src complex in an active conformation suggests possible steps in c-Src activation

21 January 2018

1 reference

Discovery of S-[5-amino-1-(4-fluorophenyl)-1H-pyrazol-4-yl]-[3-(2,3-dihydroxypropoxy)phenyl]methanone (RO3201195), an orally bioavailable and highly selective inhibitor of p38 MAP kinase

21 January 2018

1 reference

An Oral Spleen Tyrosine Kinase (Syk) Inhibitor for Rheumatoid Arthritis

21 January 2018

1 reference

Metabolism of fostamatinib, the oral methylene phosphate prodrug of the spleen tyrosine kinase inhibitor R406 in humans: contribution of hepatic and gut bacterial processes to the overall biotransformation

21 January 2018

1 reference

Structural insights for design of potent spleen tyrosine kinase inhibitors from crystallographic analysis of three inhibitor complexes

21 January 2018

1 reference

Transitions to catalytically inactive conformations in EGFR kinase

21 January 2018

1 reference

The kinetics of binding to p38MAP kinase by analogues of BIRB 796.

21 January 2018

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Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site

21 January 2018

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Features of selective kinase inhibitors

21 January 2018

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Binding kinetics and mechanism of action: toward the discovery and development of better and best in class drugs

21 January 2018

1 reference

X-ray crystallographic structure-based design of selective thienopyrazole inhibitors for interleukin-2-inducible tyrosine kinase

21 January 2018

1 reference

Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors

21 January 2018

1 reference

Crystal structures of interleukin-2 tyrosine kinase and their implications for the design of selective inhibitors

21 January 2018

1 reference

Anti-breast cancer activity of LFM-A13, a potent inhibitor of Polo-like kinase (PLK).

21 January 2018

1 reference

Bruton's tyrosine kinase as a new therapeutic target

21 January 2018

1 reference

Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors.

21 January 2018

1 reference

Structural bioinformatics-based design of selective, irreversible kinase inhibitors

21 January 2018

1 reference

Neratinib, an irreversible ErbB receptor tyrosine kinase inhibitor, in patients with advanced ErbB2-positive breast cancer

21 January 2018

1 reference

Antiarthritis effect of a novel Bruton's tyrosine kinase (BTK) inhibitor in rat collagen-induced arthritis and mechanism-based pharmacokinetic/pharmacodynamic modeling: relationships between inhibition of BTK phosphorylation and efficacy

21 January 2018

1 reference

Significant species difference in amide hydrolysis of GDC-0834, a novel potent and selective Bruton's tyrosine kinase inhibitor

21 January 2018

1 reference

RN486, a selective Bruton's tyrosine kinase inhibitor, abrogates immune hypersensitivity responses and arthritis in rodents

21 January 2018

1 reference

Targeting BTK with ibrutinib in relapsed chronic lymphocytic leukemia

21 January 2018

1 reference

The safety and efficacy of a JAK inhibitor in patients with active rheumatoid arthritis: Results of a double-blind, placebo-controlled phase IIa trial of three dosage levels of CP-690,550 versus placebo

21 January 2018

1 reference

Targeting BTK with ibrutinib in relapsed or refractory mantle-cell lymphoma

21 January 2018

1 reference

Imidazo[1,5-a]quinoxalines as irreversible BTK inhibitors for the treatment of rheumatoid arthritis

21 January 2018

1 reference

The resurgence of covalent drugs

21 January 2018

1 reference

Covalent modifiers: an orthogonal approach to drug design

21 January 2018

1 reference

21 January 2018

Identifiers

DOI

10.4155/FMC.14.24

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7 August 2017

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