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Molecular Cancer Therapeutics
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Models and Technologies

Target Identification in Small Cell Lung Cancer via Integrated Phenotypic Screening and Activity-Based Protein Profiling

Jiannong Li, Bin Fang, Fumi Kinose, Yun Bai, Jae-Young Kim, Yian A. Chen, Uwe Rix, John M. Koomen and Eric B. Haura
Jiannong Li
1Department of Thoracic Oncology, H. Lee Moffitt Cancer Center and Research Institute, Tampa, Florida.
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Bin Fang
2Proteomics Core Facility, H. Lee Moffitt Cancer Center and Research Institute, Tampa, Florida
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Fumi Kinose
1Department of Thoracic Oncology, H. Lee Moffitt Cancer Center and Research Institute, Tampa, Florida.
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Yun Bai
1Department of Thoracic Oncology, H. Lee Moffitt Cancer Center and Research Institute, Tampa, Florida.
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Jae-Young Kim
1Department of Thoracic Oncology, H. Lee Moffitt Cancer Center and Research Institute, Tampa, Florida.
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Yian A. Chen
3Department of Biostatistics and Bioinformatics, H. Lee Moffitt Cancer Center and Research Institute, Tampa, Florida
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Uwe Rix
4Department of Drug Discovery, H. Lee Moffitt Cancer Center and Research Institute, Tampa, Florida
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John M. Koomen
5Department of Molecular Oncology, H. Lee Moffitt Cancer Center and Research Institute, Tampa, Florida.
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Eric B. Haura
1Department of Thoracic Oncology, H. Lee Moffitt Cancer Center and Research Institute, Tampa, Florida.
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  • For correspondence: eric.haura@moffitt.org
DOI: 10.1158/1535-7163.MCT-15-0444 Published February 2016
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Abstract

To overcome hurdles in identifying key kinases in small cell lung cancer (SCLC), we integrated a target-agnostic phenotypic screen of kinase inhibitors with target identification using activity-based protein profiling (ABPP) in which a desthiobiotin-ATP probe was used. We screened 21 SCLC cell lines with known c-MYC amplification status for alterations in viability using a chemical library of 235 small-molecule kinase inhibitors. One screen hit compound was interrogated with ABPP, and, through this approach, we reidentified Aurora kinase B as a critical kinase in MYC-amplified SCLC cells. We next extended the platform to a second compound that had activity in SCLC cell lines lacking c-MYC amplification and identified TANK-binding kinase 1, a kinase that affects cell viability, polo-like kinase-1 signaling, G2–M arrest, and apoptosis in SCLC cells lacking MYC amplification. These results demonstrate that phenotypic screening combined with ABPP can identify key disease drivers, suggesting that this approach, which combines new chemical probes and disease cell screens, has the potential to identify other important targets in other cancer types. Mol Cancer Ther; 15(2); 334–42. ©2016 AACR.

Footnotes

  • Note: Supplementary data for this article are available at Molecular Cancer Therapeutics Online (http://mct.aacrjournals.org/).

  • Received June 2, 2015.
  • Revision received October 14, 2015.
  • Accepted November 30, 2015.
  • ©2016 American Association for Cancer Research.
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Molecular Cancer Therapeutics: 15 (2)
February 2016
Volume 15, Issue 2
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Target Identification in Small Cell Lung Cancer via Integrated Phenotypic Screening and Activity-Based Protein Profiling
Jiannong Li, Bin Fang, Fumi Kinose, Yun Bai, Jae-Young Kim, Yian A. Chen, Uwe Rix, John M. Koomen and Eric B. Haura
Mol Cancer Ther February 1 2016 (15) (2) 334-342; DOI: 10.1158/1535-7163.MCT-15-0444

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Target Identification in Small Cell Lung Cancer via Integrated Phenotypic Screening and Activity-Based Protein Profiling
Jiannong Li, Bin Fang, Fumi Kinose, Yun Bai, Jae-Young Kim, Yian A. Chen, Uwe Rix, John M. Koomen and Eric B. Haura
Mol Cancer Ther February 1 2016 (15) (2) 334-342; DOI: 10.1158/1535-7163.MCT-15-0444
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