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Src family kinase targeting in head and neck tumor cells using SU6656, PP2 and dasatinib

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Src family kinase targeting in head and neck tumor cells using SU6656, PP2 and dasatinib. / Vu, Anh Thu; Akingunsade, Lara; Hoffer, Konstantin; Petersen, Cordula; Betz, Christian Stephan; Rothkamm, Kai; Rieckmann, Thorsten; Bussmann, Lara; Kriegs, Malte.

In: HEAD NECK-J SCI SPEC, Vol. 45, No. 1, 01.2023, p. 147-155.

Research output: SCORING: Contribution to journal › SCORING: Journal article › Research › peer-review

Harvard

Vu, AT, Akingunsade, L, Hoffer, K, Petersen, C, Betz, CS, Rothkamm, K, Rieckmann, T, Bussmann, L & Kriegs, M 2023, 'Src family kinase targeting in head and neck tumor cells using SU6656, PP2 and dasatinib', HEAD NECK-J SCI SPEC, vol. 45, no. 1, pp. 147-155. https://doi.org/10.1002/hed.27216

APA

Vu, A. T., Akingunsade, L., Hoffer, K., Petersen, C., Betz, C. S., Rothkamm, K., Rieckmann, T., Bussmann, L., & Kriegs, M. (2023). Src family kinase targeting in head and neck tumor cells using SU6656, PP2 and dasatinib. HEAD NECK-J SCI SPEC, 45(1), 147-155. https://doi.org/10.1002/hed.27216

Vancouver

Vu AT, Akingunsade L, Hoffer K, Petersen C, Betz CS, Rothkamm K et al. Src family kinase targeting in head and neck tumor cells using SU6656, PP2 and dasatinib. HEAD NECK-J SCI SPEC. 2023 Jan;45(1):147-155. https://doi.org/10.1002/hed.27216

Bibtex

@article{734457846a224ea5885a4cf95c80e0f5,
title = "Src family kinase targeting in head and neck tumor cells using SU6656, PP2 and dasatinib",
abstract = "BACKGROUND: We have recently shown a frequent upregulation of Src-family kinases (SFK) in head and neck squamous cell carcinoma (HNSCC). Here we tested, if SFK targeting is effective especially in HNSCC cells with upregulated SFK signaling.METHODS: The impact of SFK inhibitors SU6656, PP2 and dasatinib on three HNSCC cell lines with different SFK activity levels was analyzed using proliferation and colony formation assays, Western blot and functional kinomics.RESULTS: Proliferation was blocked by all inhibitors in a micro-molar range. With respect to cell kill, dasatinib was most effective, while SU6656 showed moderate and PP2 minor effects. Cellular signaling was affected differently, with PP2 having no effect on SFK signaling while dasatinib probably has non-SFK specific effects. Only SU6656 showed clear SFK specific effects on signaling.CONCLUSION: The results demonstrate potential benefit of SFK inhibition in HNSCC but they also highlight challenges due to non-specificities of the different drugs.",
author = "Vu, {Anh Thu} and Lara Akingunsade and Konstantin Hoffer and Cordula Petersen and Betz, {Christian Stephan} and Kai Rothkamm and Thorsten Rieckmann and Lara Bussmann and Malte Kriegs",
note = "{\textcopyright} 2022 The Authors. Head & Neck published by Wiley Periodicals LLC.",
year = "2023",
month = jan,
doi = "10.1002/hed.27216",
language = "English",
volume = "45",
pages = "147--155",
journal = "HEAD NECK-J SCI SPEC",
issn = "1043-3074",
publisher = "John Wiley and Sons Inc.",
number = "1",

}

RIS

TY - JOUR

T1 - Src family kinase targeting in head and neck tumor cells using SU6656, PP2 and dasatinib

AU - Vu, Anh Thu

AU - Akingunsade, Lara

AU - Hoffer, Konstantin

AU - Petersen, Cordula

AU - Betz, Christian Stephan

AU - Rothkamm, Kai

AU - Rieckmann, Thorsten

AU - Bussmann, Lara

AU - Kriegs, Malte

N1 - © 2022 The Authors. Head & Neck published by Wiley Periodicals LLC.

PY - 2023/1

Y1 - 2023/1

N2 - BACKGROUND: We have recently shown a frequent upregulation of Src-family kinases (SFK) in head and neck squamous cell carcinoma (HNSCC). Here we tested, if SFK targeting is effective especially in HNSCC cells with upregulated SFK signaling.METHODS: The impact of SFK inhibitors SU6656, PP2 and dasatinib on three HNSCC cell lines with different SFK activity levels was analyzed using proliferation and colony formation assays, Western blot and functional kinomics.RESULTS: Proliferation was blocked by all inhibitors in a micro-molar range. With respect to cell kill, dasatinib was most effective, while SU6656 showed moderate and PP2 minor effects. Cellular signaling was affected differently, with PP2 having no effect on SFK signaling while dasatinib probably has non-SFK specific effects. Only SU6656 showed clear SFK specific effects on signaling.CONCLUSION: The results demonstrate potential benefit of SFK inhibition in HNSCC but they also highlight challenges due to non-specificities of the different drugs.

AB - BACKGROUND: We have recently shown a frequent upregulation of Src-family kinases (SFK) in head and neck squamous cell carcinoma (HNSCC). Here we tested, if SFK targeting is effective especially in HNSCC cells with upregulated SFK signaling.METHODS: The impact of SFK inhibitors SU6656, PP2 and dasatinib on three HNSCC cell lines with different SFK activity levels was analyzed using proliferation and colony formation assays, Western blot and functional kinomics.RESULTS: Proliferation was blocked by all inhibitors in a micro-molar range. With respect to cell kill, dasatinib was most effective, while SU6656 showed moderate and PP2 minor effects. Cellular signaling was affected differently, with PP2 having no effect on SFK signaling while dasatinib probably has non-SFK specific effects. Only SU6656 showed clear SFK specific effects on signaling.CONCLUSION: The results demonstrate potential benefit of SFK inhibition in HNSCC but they also highlight challenges due to non-specificities of the different drugs.

U2 - 10.1002/hed.27216

DO - 10.1002/hed.27216

M3 - SCORING: Journal article

C2 - 36285353

VL - 45

SP - 147

EP - 155

JO - HEAD NECK-J SCI SPEC

JF - HEAD NECK-J SCI SPEC

SN - 1043-3074

IS - 1

ER -