Discovery of a small-molecule type II inhibitor of wild-type and gatekeeper mutants of BCR-ABL, PDGFR , Kit, and Src kinases: novel type II inhibitor of gatekeeper mutants - Wikidata - wikimedia - TriplyDB

Discovery of a small-molecule type II inhibitor of wild-type and gatekeeper mutants of BCR-ABL, PDGFR , Kit, and Src kinases: novel type II inhibitor of gatekeeper mutants

Discovery of a small-molecule type II inhibitor of wild-type and gatekeeper mutants of BCR-ABL, PDGFR , Kit, and Src kinases: novel type II inhibitor of gatekeeper mutants

http://www.wikidata.org/entity/Q27660281

about

Mechanisms of drug resistance in kinases.Resistant mutations in CML and Ph(+)ALL - role of ponatinib.Allosteric interactions between the myristate- and ATP-site of the Abl kinase The conformational control inhibitor of tyrosine kinases DCC-2036 is effective for imatinib-resistant cells expressing T674I FIP1L1-PDGFRα Computational modeling of allosteric communication reveals organizing principles of mutation-induced signaling in ABL and EGFR kinases.An update on dual Src/Abl inhibitors.Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors.Outgrowth of drug-resistant carcinomas expressing markers of tumor aggression after long-term TβRI/II kinase inhibition with LY2109761.Evaluating the predictivity of virtual screening for ABL kinase inhibitors to hinder drug resistance From Hen House to Bedside: Tracing Hanafusa's Legacy from Avian Leukemia Viruses to SRC to ABL and Beyond The ABL switch control inhibitor DCC-2036 is active against the chronic myeloid leukemia mutant BCR-ABLT315I and exhibits a narrow resistance profile Vav3 collaborates with p190-BCR-ABL in lymphoid progenitor leukemogenesis, proliferation, and survival.KIDFamMap: a database of kinase-inhibitor-disease family maps for kinase inhibitor selectivity and binding mechanisms.Synthesis and biological evaluation of analogues of the kinase inhibitor nilotinib as Abl and Kit inhibitors.Ponatinib efficiently kills imatinib-resistant chronic eosinophilic leukemia cells harboring gatekeeper mutant T674I FIP1L1-PDGFRα: roles of Mcl-1 and β-catenin.Current status of agents active against the T315I chronic myeloid leukemia phenotype.Occupational hazards: allosteric regulation of protein kinases through the nucleotide-binding pocket.Molecular mechanisms of drug resistance in tyrosine kinases cAbl and cKit.Development of an effective therapy for chronic myelogenous leukemia Targeting chronic myeloid leukemia stem cells.Combination therapy with nilotinib for drug-sensitive and drug-resistant BCR-ABL-positive leukemia and other malignancies.Discovery and characterization of novel mutant FLT3 kinase inhibitors Beneficial effects of combining a type II ATP competitive inhibitor with an allosteric competitive inhibitor of BCR-ABL for the treatment of imatinib-sensitive and imatinib-resistant CML.Development of 'DFG-out' inhibitors of gatekeeper mutant kinases.An amino-indazole scaffold with spectrum selective kinase inhibition of FLT3, PDGFRα and kit.Development of protein degradation inducers of oncogenic BCR-ABL protein by conjugation of ABL kinase inhibitors and IAP ligands.Broad spectrum alkynyl inhibitors of T315I Bcr-Abl.The challenge of developing robust drugs to overcome resistance.Past, present, and future of Bcr-Abl inhibitors: from chemical development to clinical efficacy.Pharmacological difference between degrader and inhibitor against oncogenic BCR-ABL kinase

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Discovery of a small-molecule type II inhibitor of wild-type and gatekeeper mutants of BCR-ABL, PDGFR , Kit, and Src kinases: novel type II inhibitor of gatekeeper mutants

http://www.wikidata.org/entity/Q27660281

description

2010 nî lūn-bûn

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2010 թուականի Մայիսին հրատարակուած գիտական յօդուած

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2010 թվականի մայիսին հրատարակված գիտական հոդված

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2010年の論文

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2010年学术文章

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2010年学术文章

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2010年学术文章

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2010年学术文章

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2010年学术文章

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2010年學術文章

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name

Discovery of a small-molecule ...... nhibitor of gatekeeper mutants

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Discovery of a small-molecule ...... nhibitor of gatekeeper mutants

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Discovery of a small-molecule ...... nhibitor of gatekeeper mutants

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Discovery of a small-molecule ...... nhibitor of gatekeeper mutants

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Discovery of a small-molecule ...... nhibitor of gatekeeper mutants

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Discovery of a small-molecule ...... nhibitor of gatekeeper mutants

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prefLabel

Discovery of a small-molecule ...... nhibitor of gatekeeper mutants

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Discovery of a small-molecule ...... nhibitor of gatekeeper mutants

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Discovery of a small-molecule ...... nhibitor of gatekeeper mutants

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Discovery of a small-molecule ...... nhibitor of gatekeeper mutants

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Arghya Ray

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Catherine Wu

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Daisy Moreno

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Ellen Weisberg

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Hwan Geun Choi

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James D Griffin

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Jianming Zhang

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Jonathan A Fletcher

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Junia V Melo

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Maria Debiec-Rychter

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P2860

AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance

Acquired resistance of lung adenocarcinomas to gefitinib or erlotinib is associated with a second mutation in the EGFR kinase domain

Structural mechanism for STI-571 inhibition of abelson tyrosine kinase

c-Src binds to the cancer drug imatinib with an inactive Abl/c-Kit conformation and a distributed thermodynamic penalty

Crystal structure of the T315I mutant of AbI kinase

Activation of tyrosine kinases by mutation of the gatekeeper threonine

Equally Potent Inhibition of c-Src and Abl by Compounds that Recognize Inactive Kinase Conformations

A tyrosine kinase created by fusion of the PDGFRA and FIP1L1 genes as a therapeutic target of imatinib in idiopathic hypereosinophilic syndrome.

Kinase mutations and imatinib response in patients with metastatic gastrointestinal stromal tumor.

EGFR mutation and resistance of non-small-cell lung cancer to gefitinib.

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4206-4216

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10.1182/BLOOD-2009-11-251751

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Markus A Seeliger

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2010-03-18T00:00:00Z

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42345093

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20299508

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