Synonyms: EN-67
Compound class:
Synthetic organic
Comment: EN67 is a molecular glue type protein degrader [1]. It is a derivative of EN450, and like its predecsor EN67 forms a covalent bond with the allosteric C111 residue on UBE2D E2 ubiquitin-conjugating enzymes. Direct interaction with the UBE2D2 isozyme has been demonstrated.
EN67 has been conjudated to the BRD4 inhibitor (+)-JQ1, to generate a PROTAC class degrader (named NF90), which demonstrates that E2 ubiquitin ligase components can be recruited by such molecules to promote degradation of neo-substrates, in addition to the many previously reported recruiters that target E3 components of the ubiquitin-proteasome system. |
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References |
1. Forte N, Dovala D, Hesse MJ, McKenna JM, Tallarico JA, chirle M, Nomura DK. (2022)
Targeted Protein Degradation through E2 Recruitment. bioRxiv, Preprint. DOI: 10.1101/2022.12.19.520812 |