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Molecular Cancer Therapeutics
Molecular Cancer Therapeutics
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Small Molecule Therapeutics

Repurposing the Antidepressant Sertraline as SHMT Inhibitor to Suppress Serine/Glycine Synthesis–Addicted Breast Tumor Growth

Shauni Lien Geeraerts, Kim Rosalie Kampen, Gianmarco Rinaldi, Purvi Gupta, Mélanie Planque, Nikolaos Louros, Elien Heylen, Kaat De Cremer, Katrijn De Brucker, Stijn Vereecke, Benno Verbelen, Pieter Vermeersch, Joost Schymkowitz, Frederic Rousseau, David Cassiman, Sarah-Maria Fendt, Arnout Voet, Bruno P.A. Cammue, Karin Thevissen and Kim De Keersmaecker
Shauni Lien Geeraerts
1Laboratory for Disease Mechanisms in Cancer, Department of Oncology, KU Leuven and Leuven Cancer Institute (LKI), Leuven, Belgium.
2Centre of Microbial and Plant Genetics – Plant Fungi Interactions (CMPG-PFI), KU Leuven, Heverlee, Belgium.
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  • ORCID record for Shauni Lien Geeraerts
Kim Rosalie Kampen
1Laboratory for Disease Mechanisms in Cancer, Department of Oncology, KU Leuven and Leuven Cancer Institute (LKI), Leuven, Belgium.
3Maastricht University Medical Center, Department of Radiation Oncology (MAASTRO), GROW School for Oncology and Developmental Biology, Maastricht, the Netherlands.
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  • ORCID record for Kim Rosalie Kampen
Gianmarco Rinaldi
4Laboratory of Cellular Metabolism and Metabolic Regulation, VIB-KU Leuven Center for Cancer Biology, VIB Leuven, Leuven, Belgium.
5Laboratory of Cellular Metabolism and Metabolic Regulation, Department of Oncology, KU Leuven and Leuven Cancer Institute (LKI), Leuven, Belgium.
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  • ORCID record for Gianmarco Rinaldi
Purvi Gupta
6Department of Chemistry, KU Leuven, Heverlee, Belgium.
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  • ORCID record for Purvi Gupta
Mélanie Planque
4Laboratory of Cellular Metabolism and Metabolic Regulation, VIB-KU Leuven Center for Cancer Biology, VIB Leuven, Leuven, Belgium.
5Laboratory of Cellular Metabolism and Metabolic Regulation, Department of Oncology, KU Leuven and Leuven Cancer Institute (LKI), Leuven, Belgium.
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Nikolaos Louros
7Switch Laboratory, VIB Center for Brain and Disease Research, VIB-KU Leuven, Leuven, Belgium.
8Switch Laboratory, Department of Cellular and Molecular Medicine, KU Leuven, Leuven, Belgium.
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  • ORCID record for Nikolaos Louros
Elien Heylen
1Laboratory for Disease Mechanisms in Cancer, Department of Oncology, KU Leuven and Leuven Cancer Institute (LKI), Leuven, Belgium.
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  • ORCID record for Elien Heylen
Kaat De Cremer
2Centre of Microbial and Plant Genetics – Plant Fungi Interactions (CMPG-PFI), KU Leuven, Heverlee, Belgium.
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Katrijn De Brucker
2Centre of Microbial and Plant Genetics – Plant Fungi Interactions (CMPG-PFI), KU Leuven, Heverlee, Belgium.
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Stijn Vereecke
1Laboratory for Disease Mechanisms in Cancer, Department of Oncology, KU Leuven and Leuven Cancer Institute (LKI), Leuven, Belgium.
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Benno Verbelen
1Laboratory for Disease Mechanisms in Cancer, Department of Oncology, KU Leuven and Leuven Cancer Institute (LKI), Leuven, Belgium.
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Pieter Vermeersch
9Department of Cardiovascular Sciences, University Hospitals Leuven, Leuven, Belgium.
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Joost Schymkowitz
7Switch Laboratory, VIB Center for Brain and Disease Research, VIB-KU Leuven, Leuven, Belgium.
8Switch Laboratory, Department of Cellular and Molecular Medicine, KU Leuven, Leuven, Belgium.
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Frederic Rousseau
7Switch Laboratory, VIB Center for Brain and Disease Research, VIB-KU Leuven, Leuven, Belgium.
8Switch Laboratory, Department of Cellular and Molecular Medicine, KU Leuven, Leuven, Belgium.
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David Cassiman
10Department of Hepatology, University Hospitals Leuven, Leuven, Belgium.
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Sarah-Maria Fendt
4Laboratory of Cellular Metabolism and Metabolic Regulation, VIB-KU Leuven Center for Cancer Biology, VIB Leuven, Leuven, Belgium.
5Laboratory of Cellular Metabolism and Metabolic Regulation, Department of Oncology, KU Leuven and Leuven Cancer Institute (LKI), Leuven, Belgium.
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Arnout Voet
6Department of Chemistry, KU Leuven, Heverlee, Belgium.
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Bruno P.A. Cammue
2Centre of Microbial and Plant Genetics – Plant Fungi Interactions (CMPG-PFI), KU Leuven, Heverlee, Belgium.
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Karin Thevissen
2Centre of Microbial and Plant Genetics – Plant Fungi Interactions (CMPG-PFI), KU Leuven, Heverlee, Belgium.
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  • For correspondence: kim.dekeersmaecker@kuleuven.be karin.thevissen@kuleuven.be
Kim De Keersmaecker
1Laboratory for Disease Mechanisms in Cancer, Department of Oncology, KU Leuven and Leuven Cancer Institute (LKI), Leuven, Belgium.
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  • For correspondence: kim.dekeersmaecker@kuleuven.be karin.thevissen@kuleuven.be
DOI: 10.1158/1535-7163.MCT-20-0480 Published January 2021
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Article Information

Volume 20, Issue 1, pp. 50-63

DOI 
https://doi.org/10.1158/1535-7163.MCT-20-0480
PubMed 
33203732

Published By 
American Association for Cancer Research
Print ISSN 
1535-7163
Online ISSN 
1538-8514
History 
  • Received June 11, 2020
  • Revision received August 19, 2020
  • Accepted November 3, 2020
  • Published first November 17, 2020.

Article Versions

  • Previous version (November 17, 2020 - 00:05).
  • Previous version (December 10, 2020 - 07:44).
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Copyright & Usage 
©2020 American Association for Cancer Research.

Author Information

  1. Shauni Lien Geeraerts1,2,#,
  2. Kim Rosalie Kampen1,3,#,
  3. Gianmarco Rinaldi4,5,
  4. Purvi Gupta6,
  5. Mélanie Planque4,5,
  6. Nikolaos Louros7,8,
  7. Elien Heylen1,
  8. Kaat De Cremer2,
  9. Katrijn De Brucker2,
  10. Stijn Vereecke1,
  11. Benno Verbelen1,
  12. Pieter Vermeersch9,
  13. Joost Schymkowitz7,8,
  14. Frederic Rousseau7,8,
  15. David Cassiman10,
  16. Sarah-Maria Fendt4,5,
  17. Arnout Voet6,
  18. Bruno P.A. Cammue2,
  19. Karin Thevissen2,#,*, and
  20. Kim De Keersmaecker1,#,*
  1. 1Laboratory for Disease Mechanisms in Cancer, Department of Oncology, KU Leuven and Leuven Cancer Institute (LKI), Leuven, Belgium.
  2. 2Centre of Microbial and Plant Genetics – Plant Fungi Interactions (CMPG-PFI), KU Leuven, Heverlee, Belgium.
  3. 3Maastricht University Medical Center, Department of Radiation Oncology (MAASTRO), GROW School for Oncology and Developmental Biology, Maastricht, the Netherlands.
  4. 4Laboratory of Cellular Metabolism and Metabolic Regulation, VIB-KU Leuven Center for Cancer Biology, VIB Leuven, Leuven, Belgium.
  5. 5Laboratory of Cellular Metabolism and Metabolic Regulation, Department of Oncology, KU Leuven and Leuven Cancer Institute (LKI), Leuven, Belgium.
  6. 6Department of Chemistry, KU Leuven, Heverlee, Belgium.
  7. 7Switch Laboratory, VIB Center for Brain and Disease Research, VIB-KU Leuven, Leuven, Belgium.
  8. 8Switch Laboratory, Department of Cellular and Molecular Medicine, KU Leuven, Leuven, Belgium.
  9. 9Department of Cardiovascular Sciences, University Hospitals Leuven, Leuven, Belgium.
  10. 10Department of Hepatology, University Hospitals Leuven, Leuven, Belgium.
  1. ↵*Corresponding Authors:
    Kim De Keersmaecker, KU Leuven, Campus Gasthuisberg O&N1, Box 603, Herestraat 49, 3000 Leuven, Belgium. Phone: 32-16-373-167; E-mail: kim.dekeersmaecker{at}kuleuven.be; and Karin Thevissen, KU Leuven, Centre of Microbial and Plant Genetics – Plant Fungi Interactions (CMPG-PFI), Kasteelpark Arenberg 20, Box 2460, 3001 Heverlee, Belgium. Phone: 32-16-329-688 or 32-16-321-631; E-mail: karin.thevissen{at}kuleuven.be
  1. ↵#S.L. Geeraerts and K.R. Kampen are shared first authors. K. Thevissen and K. De Keersmaecker are shared last authors.

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Molecular Cancer Therapeutics: 20 (1)
January 2021
Volume 20, Issue 1
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Repurposing the Antidepressant Sertraline as SHMT Inhibitor to Suppress Serine/Glycine Synthesis–Addicted Breast Tumor Growth
Shauni Lien Geeraerts, Kim Rosalie Kampen, Gianmarco Rinaldi, Purvi Gupta, Mélanie Planque, Nikolaos Louros, Elien Heylen, Kaat De Cremer, Katrijn De Brucker, Stijn Vereecke, Benno Verbelen, Pieter Vermeersch, Joost Schymkowitz, Frederic Rousseau, David Cassiman, Sarah-Maria Fendt, Arnout Voet, Bruno P.A. Cammue, Karin Thevissen and Kim De Keersmaecker
Mol Cancer Ther January 1 2021 (20) (1) 50-63; DOI: 10.1158/1535-7163.MCT-20-0480

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Repurposing the Antidepressant Sertraline as SHMT Inhibitor to Suppress Serine/Glycine Synthesis–Addicted Breast Tumor Growth
Shauni Lien Geeraerts, Kim Rosalie Kampen, Gianmarco Rinaldi, Purvi Gupta, Mélanie Planque, Nikolaos Louros, Elien Heylen, Kaat De Cremer, Katrijn De Brucker, Stijn Vereecke, Benno Verbelen, Pieter Vermeersch, Joost Schymkowitz, Frederic Rousseau, David Cassiman, Sarah-Maria Fendt, Arnout Voet, Bruno P.A. Cammue, Karin Thevissen and Kim De Keersmaecker
Mol Cancer Ther January 1 2021 (20) (1) 50-63; DOI: 10.1158/1535-7163.MCT-20-0480
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