Therapeutic targeting of c-KIT in cancer (Q38057806)

27 August 2017

Therapeutic targeting of c-KIT in cancer (English)

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27 August 2017

Leonie K Ashman

1

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27 August 2017

Renate Griffith

series ordinal

2

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27 August 2017

language of work or name

English

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publication date

6 November 2012

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Expert Opinion on Investigational Drugs

27 August 2017

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27 August 2017

22

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27 August 2017

1

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27 August 2017

103-115

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The biology of stem cell factor and its receptor C-kit

27 August 2017

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https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Normal and oncogenic forms of the receptor tyrosine kinase kit.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Identification of mutations in the coding sequence of the proto-oncogene c-kit in a human mast cell leukemia cell line causing ligand-independent activation of c-kit product

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Gain-of-function mutations of c-kit in human gastrointestinal stromal tumors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Biology of gastrointestinal stromal tumors.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Genetics of myeloid leukemias

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

C-KIT mutation cooperates with full-length AML1-ETO to induce acute myeloid leukemia in mice

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

KIT with D816 mutations cooperates with CBFB-MYH11 for leukemogenesis in mice

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Prognostic impact of c-KIT mutations in core binding factor acute myeloid leukemia.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Prevalence and prognostic significance of KIT mutations in pediatric patients with core binding factor AML enrolled on serial pediatric cooperative trials for de novo AML.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

KIT mutations are common in testicular seminomas

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Ovarian dysgerminomas are characterised by frequent KIT mutations and abundant expression of pluripotency markers

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

KIT gene mutations and copy number in melanoma subtypes

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Mutations of the BRAF gene in human cancer

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Progression of human cutaneous melanoma is associated with loss of expression of c-kit proto-oncogene receptor.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Structural basis for activation of the receptor tyrosine kinase KIT by stem cell factor

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Extracellular KIT receptor mutants, commonly found in core binding factor AML, are constitutively active and respond to imatinib mesylate

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Juxtamembrane autoinhibition in receptor tyrosine kinases.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Structural basis for the autoinhibition and STI-571 inhibition of c-Kit tyrosine kinase

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Function of activation loop tyrosine phosphorylation in the mechanism of c-Kit auto-activation and its implication in sunitinib resistance

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Structural biology of protein tyrosine kinases

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Structure of a c-kit product complex reveals the basis for kinase transactivation

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

AML1-ETO and C-KIT mutation/overexpression in t(8;21) leukemia: implication in stepwise leukemogenesis and response to Gleevec.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Molecular basis of the constitutive activity and STI571 resistance of Asp816Val mutant KIT receptor tyrosine kinase.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

KIT kinase mutants show unique mechanisms of drug resistance to imatinib and sunitinib in gastrointestinal stromal tumor patients

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Signal transduction via the stem cell factor receptor/c-Kit

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Targeted mutations of the juxtamembrane tyrosines in the Kit receptor tyrosine kinase selectively affect multiple cell lineages

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Mechanisms of oncogenic KIT signal transduction in primary gastrointestinal stromal tumors (GISTs).

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Phosphatidylinositol 3 kinase contributes to the transformation of hematopoietic cells by the D816V c-Kit mutant

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Signal transducer and activator of transcription 3 activation is required for Asp(816) mutant c-Kit-mediated cytokine-independent survival and proliferation in human leukemia cells

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Neoplasia driven by mutant c-KIT is mediated by intracellular, not plasma membrane, receptor signaling.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Receptor trafficking controls weak signal delivery: a strategy used by c-Met for STAT3 nuclear accumulation.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

The D816V mutation of c-Kit circumvents a requirement for Src family kinases in c-Kit signal transduction

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Oncogenic mutation in the Kit receptor tyrosine kinase alters substrate specificity and induces degradation of the protein tyrosine phosphatase SHP-1

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Pushing the limits of targeted therapy in chronic myeloid leukaemia.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

The c-KIT mutation causing human mastocytosis is resistant to STI571 and other KIT kinase inhibitors; kinases with enzymatic site mutations show different inhibitor sensitivity profiles than wild-type kinases and those with regulatory-type mutations

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Structural mechanism for STI-571 inhibition of abelson tyrosine kinase

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Signal transduction by several KIT juxtamembrane domain mutations

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Advances in adjuvant therapy of gastrointestinal stromal tumors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

KIT mutations and dose selection for imatinib in patients with advanced gastrointestinal stromal tumours

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Mastocytosis: pathology, genetics, and current options for therapy

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Recent advances in the understanding of mastocytosis: the role of KIT mutations.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Dasatinib (BMS-354825), a dual SRC/ABL kinase inhibitor, inhibits the kinase activity of wild-type, juxtamembrane, and activation loop mutant KIT isoforms associated with human malignancies

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Synergistic growth-inhibitory effects of two tyrosine kinase inhibitors, dasatinib and PKC412, on neoplastic mast cells expressing the D816V-mutated oncogenic variant of KIT.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Dasatinib (BMS-354825) inhibits KITD816V, an imatinib-resistant activating mutation that triggers neoplastic growth in most patients with systemic mastocytosis

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Systemic mastocytosis in adults: a review on prognosis and treatment based on 342 Mayo Clinic patients and current literature

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

The clinical development of FLT3 inhibitors in acute myeloid leukemia

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Colony stimulating factor-1 receptor as a target for small molecule inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Activation mutations of human c-KIT resistant to imatinib mesylate are sensitive to the tyrosine kinase inhibitor PKC412.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Activity of the tyrosine kinase inhibitor PKC412 in a patient with mast cell leukemia with the D816V KIT mutation.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Acquired resistance to imatinib in gastrointestinal stromal tumor occurs through secondary gene mutation

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Imatinib binding and cKIT inhibition is abrogated by the cKIT kinase domain I missense mutation Val654Ala

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Efficacy and safety of sunitinib in patients with advanced gastrointestinal stromal tumour after failure of imatinib: a randomised controlled trial

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Primary and secondary kinase genotypes correlate with the biological and clinical activity of sunitinib in imatinib-resistant gastrointestinal stromal tumor

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Efficacy and safety of imatinib mesylate in advanced gastrointestinal stromal tumors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Comparison of two doses of imatinib for the treatment of unresectable or metastatic gastrointestinal stromal tumors: a meta-analysis of 1,640 patients

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Discontinuation of imatinib in patients with advanced gastrointestinal stromal tumours after 3 years of treatment: an open-label multicentre randomised phase 3 trial.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Adjuvant imatinib mesylate after resection of localised, primary gastrointestinal stromal tumour: a randomised, double-blind, placebo-controlled trial

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Phase II trial of neoadjuvant/adjuvant imatinib mesylate for advanced primary and metastatic/recurrent operable gastrointestinal stromal tumors: long-term follow-up results of Radiation Therapy Oncology Group 0132.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Molecular correlates of imatinib resistance in gastrointestinal stromal tumors.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Polyclonal evolution of multiple secondary KIT mutations in gastrointestinal stromal tumors under treatment with imatinib mesylate

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Mechanisms of sunitinib resistance in gastrointestinal stromal tumors harboring KITAY502-3ins mutation: an in vitro mutagenesis screen for drug resistance

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Sunitinib-resistant gastrointestinal stromal tumors harbor cis-mutations in the activation loop of the KIT gene.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Imatinib mesylate in the treatment of newly diagnosed or refractory/resistant c-KIT positive acute myeloid leukemia. Results of an Italian Multicentric Phase II Study

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Imatinib mesylate in the treatment of Core Binding Factor leukemias with KIT mutations. A report of three cases

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Cytoreductive therapy in 108 adults with systemic mastocytosis: Outcome analysis and response prediction during treatment with interferon-alpha, hydroxyurea, imatinib mesylate or 2-chlorodeoxyadenosine

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Phase II study of imatinib mesylate as therapy for patients with systemic mastocytosis

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Effects of AMN107, a novel aminopyrimidine tyrosine kinase inhibitor, on human mast cells bearing wild-type or mutated codon 816 c-kit

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Dasatinib therapy for systemic mastocytosis: four cases

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Systemic mastocytosis in adults: 2011 update on diagnosis, risk stratification, and management

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

KIT as a therapeutic target in metastatic melanoma

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Phase II, open-label, single-arm trial of imatinib mesylate in patients with metastatic melanoma harboring c-Kit mutation or amplification

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Activate and resist: L576P-KIT in GIST.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Activity of dasatinib against L576P KIT mutant melanoma: molecular, cellular, and clinical correlates

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

A phase 2 trial of dasatinib in advanced melanoma

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Kitlow stem cells cause resistance to Kit/platelet-derived growth factor alpha inhibitors in murine gastrointestinal stromal tumors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Minute gastric sclerosing stromal tumors (GIST tumorlets) are common in adults and frequently show c-KIT mutations

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Frequency, phenotype, and genotype of minute gastrointestinal stromal tumors in the stomach: an autopsy study.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

ETV1 is a lineage survival factor that cooperates with KIT in gastrointestinal stromal tumours

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Detection of an activating c-kit mutation by real-time PCR in patients with anaphylaxis

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

KIT-D816V-independent oncogenic signaling in neoplastic cells in systemic mastocytosis: role of Lyn and Btk activation and disruption by dasatinib and bosutinib

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Autophagy inhibition and antimalarials promote cell death in gastrointestinal stromal tumor (GIST).

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Synergistic induction of apoptosis by the Bcl-2 inhibitor ABT-737 and imatinib mesylate in gastrointestinal stromal tumor cells

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Role for the proapoptotic factor BIM in mediating imatinib-induced apoptosis in a c-KIT-dependent gastrointestinal stromal tumor cell line

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

17-Allylamino-17-demethoxygeldanamycin (17-AAG) is effective in down-regulating mutated, constitutively activated KIT protein in human mast cells

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

The heat shock protein 90 inhibitor IPI-504 induces KIT degradation, tumor shrinkage, and cell proliferation arrest in xenograft models of gastrointestinal stromal tumors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

KIT oncogenic signaling mechanisms in imatinib-resistant gastrointestinal stromal tumor: PI3-kinase/AKT is a crucial survival pathway

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Systemic therapy for advanced gastrointestinal stromal tumors: beyond imatinib

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Essential requirement for PP2A inhibition by the oncogenic receptor c-KIT suggests PP2A reactivation as a strategy to treat c-KIT+ cancers

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Reactivating PP2A by FTY720 as a novel therapy for AML with C-KIT tyrosine kinase domain mutation

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

The concept of synthetic lethality in the context of anticancer therapy

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Development of computational and graphical tools for analysis of movement and flexibility in large molecules.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

Functional analyses and molecular modeling of two c-Kit mutations responsible for imatinib secondary resistance in GIST patients

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.2013.740010

10.1517/13543784.2013.740010

21 January 2018

Identifiers

DOI

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release_bvj7b5qfzfcnbbmnb7pe2xbn6i

27 August 2017

1 reference

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mapped directly with Wikidata item

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based on heuristic

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