Exploiting an Asp-Glu “switch” in glycogen synthase kinase 3 to design paralog-selective inhibitors for use in acute myeloid leukemia-Reference-Cited by-同舟云学术

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

Published:2018-03-07 Issue:431 Volume:10 Page:
ISSN:1946-6234
Container-title:Science Translational Medicine
language:en
Short-container-title:Sci. Transl. Med.

Author:

Wagner Florence F.¹^ORCID,Benajiba Lina²³⁴⁵^ORCID,Campbell Arthur J.¹^ORCID,Weïwer Michel¹^ORCID,Sacher Joshua R.¹^ORCID,Gale Jennifer P.¹^ORCID,Ross Linda³⁴^ORCID,Puissant Alexandre³⁴⁶,Alexe Gabriela²³⁴⁷^ORCID,Conway Amy³⁴^ORCID,Back Morgan³⁴,Pikman Yana²³⁴^ORCID,Galinsky Ilene⁸^ORCID,DeAngelo Daniel J.⁸,Stone Richard M.⁸,Kaya Taner¹^ORCID,Shi Xi¹,Robers Matthew B.⁹,Machleidt Thomas⁹,Wilkinson Jennifer⁹,Hermine Olivier¹⁰¹¹,Kung Andrew¹²^ORCID,Stein Adam J.¹³^ORCID,Lakshminarasimhan Damodharan¹⁴^ORCID,Hemann Michael T.¹⁵^ORCID,Scolnick Edward¹,Zhang Yan-Ling¹,Pan Jen Q.¹,Stegmaier Kimberly²³⁴,Holson Edward B.¹^ORCID

Affiliation:

1. Stanley Center for Psychiatric Research, Broad Institute of Massachusetts Institute of Technology and Harvard University, Cambridge, MA 02142, USA.

2. Broad Institute of Massachusetts Institute of Technology and Harvard University, Cambridge, MA 02142, USA.

3. Department of Pediatric Oncology, Dana-Farber Cancer Institute, Boston, MA 02115, USA.

4. Division of Hematology/Oncology, Boston Children’s Hospital, Boston, MA 02115, USA.

5. INSERM U1163 and CNRS 8254, Imagine Institute, Université Paris Saclay, 91190 Paris, France.

6. INSERM U944, Institute of Hematology, St. Louis Hospital, 75010 Paris, France.

7. Bioinformatics Graduate Program, Boston University, Boston, MA 02215, USA.

8. Department of Medical Oncology, Dana-Farber Cancer Institute, Harvard Medical School, Boston, MA 02215, USA.

9. Promega Corporation, 2800 Woods Hollow Road, Madison, WI 53711, USA.

10. INSERM U1163 and CNRS 8254, Imagine Institute, Université Sorbonne Paris Cité, Paris, France.

11. Department of Hematology, Hôpital Necker, Assistance Publique Hôpitaux de Paris, University Paris Descartes, 75006 Paris, France.

12. Department of Pediatrics, Columbia University Medical Center, New York, NY 10032, USA.

13. Cayman Chemical Co., Ann Arbor, MI 48108, USA.

14. Xtal BioStructures Inc., Natick, MA 01760, USA.

15. Koch Institute for Integrative Cancer Research at MIT, Massachusetts Institute of Technology, Cambridge, MA 02142, USA.

Abstract

Paralog-selective inhibitors of GSK3 kinases were designed by exploiting a single amino acid difference in their ATP-binding domains and studied in AML.

Funder

National Cancer Institute

Stanley Medical Research Institute

Childrenâs Leukemia Research Association

Publisher

American Association for the Advancement of Science (AAAS)

Subject

General Medicine

Reference67 articles.

1. The evolution of gene duplications: classifying and distinguishing between models

2. [48] cDNA cloning and properties of glycogen synthase kinase-3

3. Distinct roles of GSK-3 and GSK-3 phosphorylation in the heart under pressure overload