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. 2020 Nov 25;10:574011. doi: 10.3389/fonc.2020.574011

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Copyright © 2020 Scholz, Kurian, Siebzehnrubl and Licchesi

This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.

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Structural Basis of PROTACs. PROtein-TArgeting Chimeric molecules (PROTACs) are heterobifunctional bridges that link E3 ligase activity to non-canonical substrates. PROTAC MZ1 links bromodomain inhibitor JQ1 to VHL ligand VH032 via a polyethylene glycol (PEG) linker. MZ1 facilitates binding and subsequent ubiquitination of BET (bromodomain and extraterminal) protein family member Brd4 (shown BRD4^BD2) to cullin-RING ligase complex CRL2^VHL. PDB: 5N4W, Cul2-Rbx1-EloBC-VHL ubiquitin ligase complex; 5T35, PROTAC MZ1 in complex with Brd4^BD2 and pVHL : ElonginC:ElonginB.