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. 2020 Nov 26;9(12):421. doi: 10.3390/biology9120421

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© 2020 by the authors.

Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).

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Degradation TAG (dTAG). (A) Heterobifunctional dTAG-13 molecules engage FKBP12^F36V-fused POI and cereblon (CRBN), hijacking it towards endogenous proteasome machinery for POI degradation. dTAG-13 contains AP1867 and thalidomide, FKBP12^F36V and CRBN selective ligands, respectively. CRL4–CRBN E3 ubiquitin ligase recruited by dTAG-13 is composed of cullin scaffold (CUL4A), adaptor protein (DDB1), substrate receptor (CRBN), the RING protein (Rbx1) recruiting an E2 ligase and N8 ubiquitin-like protein (NEDD8). (B) dTAG^V-1 molecule recruits the von Hippel–Lindau (VHL) E3 ligase complex, increasing dTAG system efficiency. VHL complex consists of a cullin scaffold (Cul2), two adaptor proteins (EloB and EloC), a substrate receptor (VHL), and Rbx1. POI: protein of interest. Ub: ubiquitin.