Resistance to kinase inhibition through shortened target engagement

Aziz M. Rangwala; Benedict Tilman Berger; Matthew B. Robers; Stefan Knapp; Markus A. Seeliger

doi:10.1080/23723556.2022.2029999

Resistance to kinase inhibition through shortened target engagement

Aziz M. Rangwala
, Benedict Tilman Berger
, Matthew B. Robers
, Stefan Knapp
, Markus A. Seeliger

Stony Brook University
Goethe University Frankfurt
Promega Corporation

Research output: Contribution to journal › Comment/debate

4 Scopus citations

Abstract

Imatinib, a selective inhibitor of the breakpoint cluster region (BCR)-ABL kinase, is the poster child for targeted cancer therapeutics. However, its efficacy is limited by resistance mutations. Using a quantitative bioluminescence resonance energy transfer assay in living cells, we identified ABL kinase mutations that could cause imatinib resistance by altering drug residence time.

Original language	English
Article number	2029999
Journal	Molecular and Cellular Oncology
Volume	9
Issue number	1
DOIs	https://doi.org/10.1080/23723556.2022.2029999
State	Published - 2022

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10.1080/23723556.2022.2029999

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@article{40670fd08aef4f53a4178597635d2857,

title = "Resistance to kinase inhibition through shortened target engagement",

abstract = "Imatinib, a selective inhibitor of the breakpoint cluster region (BCR)-ABL kinase, is the poster child for targeted cancer therapeutics. However, its efficacy is limited by resistance mutations. Using a quantitative bioluminescence resonance energy transfer assay in living cells, we identified ABL kinase mutations that could cause imatinib resistance by altering drug residence time.",

author = "Rangwala, \{Aziz M.\} and Berger, \{Benedict Tilman\} and Robers, \{Matthew B.\} and Stefan Knapp and Seeliger, \{Markus A.\}",

note = "Publisher Copyright: {\textcopyright} 2022 The Author(s). Published with license by Taylor \& Francis Group, LLC.",

year = "2022",

doi = "10.1080/23723556.2022.2029999",

language = "English",

volume = "9",

journal = "Molecular and Cellular Oncology",

issn = "2372-3556",

number = "1",

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TY - JOUR

T1 - Resistance to kinase inhibition through shortened target engagement

AU - Rangwala, Aziz M.

AU - Berger, Benedict Tilman

AU - Robers, Matthew B.

AU - Knapp, Stefan

AU - Seeliger, Markus A.

PY - 2022

Y1 - 2022

N2 - Imatinib, a selective inhibitor of the breakpoint cluster region (BCR)-ABL kinase, is the poster child for targeted cancer therapeutics. However, its efficacy is limited by resistance mutations. Using a quantitative bioluminescence resonance energy transfer assay in living cells, we identified ABL kinase mutations that could cause imatinib resistance by altering drug residence time.

AB - Imatinib, a selective inhibitor of the breakpoint cluster region (BCR)-ABL kinase, is the poster child for targeted cancer therapeutics. However, its efficacy is limited by resistance mutations. Using a quantitative bioluminescence resonance energy transfer assay in living cells, we identified ABL kinase mutations that could cause imatinib resistance by altering drug residence time.

UR - https://www.scopus.com/pages/publications/85123622976

U2 - 10.1080/23723556.2022.2029999

DO - 10.1080/23723556.2022.2029999

M3 - Comment/debate

AN - SCOPUS:85123622976

SN - 2372-3556

VL - 9

JO - Molecular and Cellular Oncology

JF - Molecular and Cellular Oncology

IS - 1

M1 - 2029999

ER -

Resistance to kinase inhibition through shortened target engagement

Abstract

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