Strategies to overcome resistance to targeted protein kinase inhibitors (Q35968384)

11 August 2017

title

Strategies to overcome resistance to targeted protein kinase inhibitors (English)

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11 August 2017

Henrik Daub

1

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11 August 2017

Katja Specht

series ordinal

2

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11 August 2017

Axel Ullrich

series ordinal

3

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11 August 2017

publication date

1 December 2004

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Nature Reviews Drug Discovery

11 August 2017

language of work or name

English

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published in

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11 August 2017

volume

3

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11 August 2017

issue

12

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11 August 2017

page(s)

1001-1010

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publication type of scholarly work

11 August 2017

review article

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Oncogenic kinase signalling

cites work

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Protein kinases--the major drug targets of the twenty-first century?

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Issues and progress with protein kinase inhibitors for cancer treatment

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Tyrosine kinase activity and transformation potency of bcr-abl oncogene products.

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Activity of a specific inhibitor of the BCR-ABL tyrosine kinase in the blast crisis of chronic myeloid leukemia and acute lymphoblastic leukemia with the Philadelphia chromosome

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Targeting oncogene dependence and resistance

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MDR1 gene overexpression confers resistance to imatinib mesylate in leukemia cell line models

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Active transport of imatinib into and out of cells: implications for drug resistance

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BCR-ABL independence and LYN kinase overexpression in chronic myelogenous leukemia cells selected for resistance to STI571.

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A Bcr/Abl-independent, Lyn-dependent form of imatinib mesylate (STI-571) resistance is associated with altered expression of Bcl-2.

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Clinical resistance to STI-571 cancer therapy caused by BCR-ABL gene mutation or amplification

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Primitive, quiescent, Philadelphia-positive stem cells from patients with chronic myeloid leukemia are insensitive to STI571 in vitro

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High frequency of point mutations clustered within the adenosine triphosphate-binding region of BCR/ABL in patients with chronic myeloid leukemia or Ph-positive acute lymphoblastic leukemia who develop imatinib (STI571) resistance

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Ph(+) acute lymphoblastic leukemia resistant to the tyrosine kinase inhibitor STI571 has a unique BCR-ABL gene mutation

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Clinical resistance to the kinase inhibitor STI-571 in chronic myeloid leukemia by mutation of Tyr-253 in the Abl kinase domain P-loop

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Multiple BCR-ABL kinase domain mutations confer polyclonal resistance to the tyrosine kinase inhibitor imatinib (STI571) in chronic phase and blast crisis chronic myeloid leukemia

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BCR-ABL gene mutations in relation to clinical resistance of Philadelphia-chromosome-positive leukaemia to STI571: a prospective study

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Several Bcr-Abl kinase domain mutants associated with imatinib mesylate resistance remain sensitive to imatinib

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Structural mechanism for STI-571 inhibition of abelson tyrosine kinase

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Characterization of a conserved structural determinant controlling protein kinase sensitivity to selective inhibitors.

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Detection of BCR-ABL mutations in patients with CML treated with imatinib is virtually always accompanied by clinical resistance, and mutations in the ATP phosphate-binding loop (P-loop) are associated with a poor prognosis

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Mechanisms of autoinhibition and STI-571/imatinib resistance revealed by mutagenesis of BCR-ABL.

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Response to imatinib mesylate in patients with chronic myeloproliferative diseases with rearrangements of the platelet-derived growth factor receptor beta

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Efficacy and safety of imatinib mesylate in advanced gastrointestinal stromal tumors

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A new mutation in the KIT ATP pocket causes acquired resistance to imatinib in a gastrointestinal stromal tumor patient

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Late resistance to imatinib therapy in a metastatic gastrointestinal stromal tumour is associated with a second KIT mutation

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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

31 March 2020

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Dose escalation of imatinib mesylate can overcome resistance to standard-dose therapy in patients with chronic myelogenous leukemia

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Overriding imatinib resistance with a novel ABL kinase inhibitor

31 March 2020

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Inhibition of wild-type and mutant Bcr-Abl by AP23464, a potent ATP-based oncogenic protein kinase inhibitor: implications for CML.

31 March 2020

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The protein kinase complement of the human genome

31 March 2020

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Conversion of SB 203580-insensitive MAP kinase family members to drug-sensitive forms by a single amino-acid substitution

31 March 2020

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Mutation of threonine 766 in the epidermal growth factor receptor reveals a hotspot for resistance formation against selective tyrosine kinase inhibitors

31 March 2020

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Structure of the epidermal growth factor receptor kinase domain alone and in complex with a 4-anilinoquinazoline inhibitor

31 March 2020

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31 March 2020

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United States Food and Drug Administration Drug Approval summary: Gefitinib (ZD1839; Iressa) tablets

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Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib

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EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy

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EGF receptor gene mutations are common in lung cancers from "never smokers" and are associated with sensitivity of tumors to gefitinib and erlotinib

31 March 2020

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Gefitinib-sensitizing EGFR mutations in lung cancer activate anti-apoptotic pathways

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PKC412 overcomes resistance to imatinib in a murine model of FIP1L1-PDGFRα-induced myeloproliferative disease.

31 March 2020

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Structures of the tyrosine kinase domain of fibroblast growth factor receptor in complex with inhibitors

31 March 2020

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Several types of mutations of the Abl gene can be found in chronic myeloid leukemia patients resistant to STI571, and they can pre-exist to the onset of treatment.

31 March 2020

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A mutation conferring resistance to imatinib at the time of diagnosis of chronic myelogenous leukemia.

31 March 2020

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Presence of the BCR-ABL mutation Glu255Lys prior to STI571 (imatinib) treatment in patients with Ph+ acute lymphoblastic leukemia

31 March 2020

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"Promiscuous" anticancer drugs that hit multiple targets may thwart resistance

31 March 2020

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From magic bullets to designed multiple ligands

31 March 2020

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Benefits of targeting both pericytes and endothelial cells in the tumor vasculature with kinase inhibitors

31 March 2020

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Angiogenesis inhibitors in clinical development; where are we now and where are we going?

31 March 2020

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Rhebbing up mTOR: New Insights on TSC1 and TSC2, and the Pathogenesis of Tuberous Sclerosis

31 March 2020

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SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo

31 March 2020

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The specificities of protein kinase inhibitors: an update

31 March 2020

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An efficient proteomics method to identify the cellular targets of protein kinase inhibitors.

31 March 2020

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Proteome-wide identification of cellular targets affected by bisindolylmaleimide-type protein kinase C inhibitors

31 March 2020

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Evaluation of kinase inhibitor selectivity by chemical proteomics

31 March 2020

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Treatment-specific changes in gene expression discriminate in vivo drug response in human leukemia cells

31 March 2020

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Simultaneous suppression of epidermal growth factor receptor and c-erbB-2 reverses aneuploidy and malignant phenotype of a human ovarian carcinoma cell line.

31 March 2020

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HER-targeted tyrosine-kinase inhibitors

31 March 2020

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Overcoming STI571 resistance with the farnesyl transferase inhibitor SCH66336.

31 March 2020

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BCR-ABL point mutants isolated from patients with imatinib mesylate-resistant chronic myeloid leukemia remain sensitive to inhibitors of the BCR-ABL chaperone heat shock protein 90.

31 March 2020

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31 March 2020

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31 March 2020

Identifiers

DOI

10.1038/NRD1579

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Dimensions Publication ID

11 August 2017

1036720660

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