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PROTACs for BRDs proteins in cancer therapy: a review

, , , &
Pages 1694-1703 | Received 07 Dec 2021, Accepted 18 May 2022, Published online: 14 Jun 2022

Figures & data

Figure 1. PROTAC-mediated degradation of target proteins through the UPS.

Figure 1. PROTAC-mediated degradation of target proteins through the UPS.

Figure 2. (A) Structure of the human BRDs of transcriptional coactivator CREB-binding protein CREBBP (PDB: 5NU3). The KAc binding site is blocked by the inhibitor XDM-CBP (shown in yellow)Citation27,Citation58. (B) Phylogenetic tree of the human BRDs family. The green branches represent proteins such as BRD2, BRD3, BRD4, etc. The purple branches represent proteins such as BRD1, BRD7, and BRD9Citation59.

Figure 2. (A) Structure of the human BRDs of transcriptional coactivator CREB-binding protein CREBBP (PDB: 5NU3). The KAc binding site is blocked by the inhibitor XDM-CBP (shown in yellow)Citation27,Citation58. (B) Phylogenetic tree of the human BRDs family. The green branches represent proteins such as BRD2, BRD3, BRD4, etc. The purple branches represent proteins such as BRD1, BRD7, and BRD9Citation59.

Figure 3. Representative BRDs inhibitors.

Figure 3. Representative BRDs inhibitors.

Figure 4. Representative PROTACs targeting BRD4.

Figure 4. Representative PROTACs targeting BRD4.

Figure 5. Representative PROTACs targeting BRD2/3/4.

Figure 5. Representative PROTACs targeting BRD2/3/4.

Figure 6. Representative PROTACs targeting BRD9.

Figure 6. Representative PROTACs targeting BRD9.

Figure 7. Representative PROTACs targeting BRD4.

Figure 7. Representative PROTACs targeting BRD4.

Figure 8. Representative PROTACs targeting BRD4.

Figure 8. Representative PROTACs targeting BRD4.

Figure 9. Representative PROTACs targeting BRD2/3/4.

Figure 9. Representative PROTACs targeting BRD2/3/4.

Figure 10. Representative PROTACs targeting BRD2/4.

Figure 10. Representative PROTACs targeting BRD2/4.

Figure 11. Representative PROTACs targeting BRD7/9.

Figure 11. Representative PROTACs targeting BRD7/9.