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Exploiting an Asp-Glu “switch” in glycogen synthase kinase 3 to design paralog-selective inhibitors for use in acute myeloid leukemia

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Science Translational Medicine  07 Mar 2018:
Vol. 10, Issue 431, eaam8460
DOI: 10.1126/scitranslmed.aam8460

Article Information

vol. 10 no. 431

PubMed: 
Print ISSN: 
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History: 
  • Received for publication January 24, 2017
  • Resubmitted August 30, 2017
  • Accepted for publication November 9, 2017

Author Information

  1. Florence F. Wagner1,*,,
  2. Lina Benajiba2,3,4,5,,
  3. Arthur J. Campbell1,
  4. Michel Weïwer1,
  5. Joshua R. Sacher1,
  6. Jennifer P. Gale1,
  7. Linda Ross3,4,
  8. Alexandre Puissant3,4,6,
  9. Gabriela Alexe2,3,4,7,
  10. Amy Conway3,4,
  11. Morgan Back3,4,
  12. Yana Pikman2,3,4,
  13. Ilene Galinsky8,
  14. Daniel J. DeAngelo8,
  15. Richard M. Stone8,
  16. Taner Kaya1,
  17. Xi Shi1,
  18. Matthew B. Robers9,
  19. Thomas Machleidt9,
  20. Jennifer Wilkinson9,
  21. Olivier Hermine10,11,
  22. Andrew Kung12,
  23. Adam J. Stein13,
  24. Damodharan Lakshminarasimhan14,
  25. Michael T. Hemann15,
  26. Edward Scolnick1,
  27. Yan-Ling Zhang1,
  28. Jen Q. Pan1,
  29. Kimberly Stegmaier2,3,4,*, and
  30. Edward B. Holson1,,§
  1. 1Stanley Center for Psychiatric Research, Broad Institute of Massachusetts Institute of Technology and Harvard University, Cambridge, MA 02142, USA.
  2. 2Broad Institute of Massachusetts Institute of Technology and Harvard University, Cambridge, MA 02142, USA.
  3. 3Department of Pediatric Oncology, Dana-Farber Cancer Institute, Boston, MA 02115, USA.
  4. 4Division of Hematology/Oncology, Boston Children’s Hospital, Boston, MA 02115, USA.
  5. 5INSERM U1163 and CNRS 8254, Imagine Institute, Université Paris Saclay, 91190 Paris, France.
  6. 6INSERM U944, Institute of Hematology, St. Louis Hospital, 75010 Paris, France.
  7. 7Bioinformatics Graduate Program, Boston University, Boston, MA 02215, USA.
  8. 8Department of Medical Oncology, Dana-Farber Cancer Institute, Harvard Medical School, Boston, MA 02215, USA.
  9. 9Promega Corporation, 2800 Woods Hollow Road, Madison, WI 53711, USA.
  10. 10INSERM U1163 and CNRS 8254, Imagine Institute, Université Sorbonne Paris Cité, Paris, France.
  11. 11Department of Hematology, Hôpital Necker, Assistance Publique Hôpitaux de Paris, University Paris Descartes, 75006 Paris, France.
  12. 12Department of Pediatrics, Columbia University Medical Center, New York, NY 10032, USA.
  13. 13Cayman Chemical Co., Ann Arbor, MI 48108, USA.
  14. 14Xtal BioStructures Inc., Natick, MA 01760, USA.
  15. 15Koch Institute for Integrative Cancer Research at MIT, Massachusetts Institute of Technology, Cambridge, MA 02142, USA.
  1. *Corresponding author. Email: fwagner{at}broadinstitute.org (F.F.W.); kimberly_stegmaier{at}dfci.harvard.edu (K.S.)
    • These authors contributed equally as co-first authors.

    • These authors contributed equally as co-senior authors.

    • § Present address: Amathus Therapeutics, LabCentral, Cambridge, MA 02139, USA.

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