Discovery of a First-In-Class Covalent Allosteric Inhibitor of SUMO E1 Activating Enzyme

Robert S Magin; Laura M Doherty; Sara J Buhrlage

doi:10.1016/j.chembiol.2019.02.006

Discovery of a First-In-Class Covalent Allosteric Inhibitor of SUMO E1 Activating Enzyme

Cell Chem Biol. 2019 Feb 21;26(2):153-155. doi: 10.1016/j.chembiol.2019.02.006.

Authors

Robert S Magin¹, Laura M Doherty², Sara J Buhrlage³

Affiliations

¹ Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02215, USA; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA 02115, USA.
² Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02215, USA; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA 02115, USA; Department of Systems Biology and Laboratory of Systems Pharmacology, Harvard Medical School, Boston, MA 02115, USA.
³ Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02215, USA; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA 02115, USA. Electronic address: saraj_buhrlage@dfci.harvard.edu.

PMID: 30794786
DOI: 10.1016/j.chembiol.2019.02.006

Abstract

SUMOylation is a post-translational modification with important roles in normal physiology and whose dysregulation is associated with human diseases. In this issue of Cell Chemical Biology, Li et al. (2019) describe a covalent, allosteric inhibitor of the SUMO E1 enzyme and demonstrate its anti-tumor activity in preclinical models of colorectal cancer.

Publication types

Comment

MeSH terms

Humans
Sumoylation*
Ubiquitin*

Substances

Ubiquitin