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

11 August 2017

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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

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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Oncogenic kinase signalling

11 August 2017

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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

31 March 2020

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

31 March 2020

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Structural mechanism for STI-571 inhibition of abelson tyrosine kinase

31 March 2020

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

31 March 2020

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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

31 March 2020

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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

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

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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.

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

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

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

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HER-targeted tyrosine-kinase inhibitors

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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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