Resistance to kinase inhibition through shortened target engagement

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 k...

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Autores principales: Rangwala, Aziz M., Berger, Benedict-Tilman, Robers, Matthew B., Knapp, Stefan, Seeliger, Markus A.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Taylor & Francis 2022
Materias:
Author’s Views
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8890393/
https://www.ncbi.nlm.nih.gov/pubmed/35252553
http://dx.doi.org/10.1080/23723556.2022.2029999
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author Rangwala, Aziz M.
Berger, Benedict-Tilman
Robers, Matthew B.
Knapp, Stefan
Seeliger, Markus A.
author_facet Rangwala, Aziz M.
Berger, Benedict-Tilman
Robers, Matthew B.
Knapp, Stefan
Seeliger, Markus A.
author_sort Rangwala, Aziz M.
collection PubMed
description 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.
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spelling pubmed-88903932022-03-03 Resistance to kinase inhibition through shortened target engagement Rangwala, Aziz M. Berger, Benedict-Tilman Robers, Matthew B. Knapp, Stefan Seeliger, Markus A. Mol Cell Oncol Author’s Views 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. Taylor & Francis 2022-01-22 /pmc/articles/PMC8890393/ /pubmed/35252553 http://dx.doi.org/10.1080/23723556.2022.2029999 Text en © 2022 The Author(s). Published with license by Taylor & Francis Group, LLC. https://creativecommons.org/licenses/by/4.0/This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) ), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Author’s Views
Rangwala, Aziz M.
Berger, Benedict-Tilman
Robers, Matthew B.
Knapp, Stefan
Seeliger, Markus A.
Resistance to kinase inhibition through shortened target engagement
title Resistance to kinase inhibition through shortened target engagement
title_full Resistance to kinase inhibition through shortened target engagement
title_fullStr Resistance to kinase inhibition through shortened target engagement
title_full_unstemmed Resistance to kinase inhibition through shortened target engagement
title_short Resistance to kinase inhibition through shortened target engagement
title_sort resistance to kinase inhibition through shortened target engagement
topic Author’s Views
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8890393/
https://www.ncbi.nlm.nih.gov/pubmed/35252553
http://dx.doi.org/10.1080/23723556.2022.2029999
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AT knappstefan resistancetokinaseinhibitionthroughshortenedtargetengagement
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