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Ubiquitin-like (Ubl) post-translational modifications are potential targets for therapeutics. However, the only known mechanism for inhibiting a Ubl-activating enzyme is through targeting its ATP-binding site. Here we identify an allosteric inhibitory site in the small ubiquitin-like modifier (SUMO)-activating enzyme (E1). This site was unexpected because both it and analogous sites are deeply buried in all previously solved structures of E1s of ubiquitin-like modifiers (Ubl). The inhibitor not only suppresses SUMO E1 activity, but also enhances its degradation in vivo, presumably due to a conformational change induced by the compound. In addition, the lead compound increased the expression of miR-34b and reduced c-Myc levels in lymphoma and colorectal cancer cell lines and a colorectal cancer xenograft mouse model. Identification of this first-in-class inhibitor of SUMO E1 is a major advance in modulating Ubl modifications for therapeutic aims.
Pubmed ID: 30581133 RIS Download
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View all literature mentionsThis polyclonal targets Human SAE2 / UBA2
View all literature mentionsThis monoclonal targets Ki-67
View all literature mentionsThis polyclonal targets Ube2i
View all literature mentionsThis monoclonal targets SUMO2 / 3
View all literature mentionsThis monoclonal targets EPCAM
View all literature mentionsThis monoclonal targets c-Myc (D84C12) XP Rabbit mAb
View all literature mentionsThis monoclonal targets β-Actin
View all literature mentionsThis monoclonal targets Sumo1
View all literature mentionsThis monoclonal targets c-Myc antibody [Y69]
View all literature mentionsCell line HCT 116 is a Cancer cell line with a species of origin Homo sapiens (Human)
View all literature mentionsCell line HEK293T is a Transformed cell line with a species of origin Homo sapiens (Human)
View all literature mentionsCell line HEK293 is a Transformed cell line with a species of origin Homo sapiens (Human)
View all literature mentionsCell line OVCAR-3 is a Cancer cell line with a species of origin Homo sapiens (Human)
View all literature mentionsCell line HT-29 is a Cancer cell line with a species of origin Homo sapiens (Human)
View all literature mentionsCell line Raji is a Cancer cell line with a species of origin Homo sapiens (Human)
View all literature mentionsThis monoclonal targets c-Myc (D84C12) XP Rabbit mAb
View all literature mentionsThis polyclonal targets Human SAE2 / UBA2
View all literature mentionsThis polyclonal targets Ube2i
View all literature mentionsThis monoclonal targets c-Myc antibody [Y69]
View all literature mentionsThis monoclonal targets Sumo1
View all literature mentionsThis monoclonal targets β-Actin
View all literature mentionsThis monoclonal targets EPCAM
View all literature mentionsThis monoclonal targets Ki-67
View all literature mentionsThis monoclonal targets SUMO2 / 3
View all literature mentionsCell line HCT 116 is a Cancer cell line with a species of origin Homo sapiens (Human)
View all literature mentionsCell line Raji is a Cancer cell line with a species of origin Homo sapiens (Human)
View all literature mentionsCell line HEK293T is a Transformed cell line with a species of origin Homo sapiens (Human)
View all literature mentionsCell line HT-29 is a Cancer cell line with a species of origin Homo sapiens (Human)
View all literature mentionsCell line HEK293 is a Transformed cell line with a species of origin Homo sapiens (Human)
View all literature mentionsCell line OVCAR-3 is a Cancer cell line with a species of origin Homo sapiens (Human)
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