Our paper studying the effect of linking on the mechanism of action of BET degraders

Read our paper open access here. The article will be published as part of the a Special Issue on “Inducing Protein Degradation as a Therapeutic Strategy“.

ToC Graphics
ToC Graphics
Chart 1. Chemical Structures of Ligands for VHL (1) and CRBN (2) and BET Inhibitors 3 (JQ1) and 4 (I- BET726)
Chart 1. Chemical Structures of Ligands for VHL (1) and CRBN (2) and BET Inhibitors 3 (JQ1) and 4 (I- BET726)
Chart 2. Chemical Structures of VHL-Targeting PROTACs Based on 4 and 3 Used in This Study and Chemical Structure of CRBN-Targeting PROTAC 11 (ARV-825)
Chart 2. Chemical Structures of VHL-Targeting PROTACs Based on 4 and 3 Used in This Study and Chemical Structure of CRBN-Targeting PROTAC 11 (ARV-825)
Figure 1. Co-crystal structures to guide PROTAC linking design
Figure 1. Co-crystal structures to guide PROTAC linking design
Figure 2. Protein degradation profile of VHL-based BET degraders
Figure 2. Protein degradation profile of VHL-based BET degraders
Figure 3. Measuring cooperativities of ternary complex formation by ITC
Figure 3. Measuring cooperativities of ternary complex formation by ITC
Figure 4. Antiproliferative and Myc-suppression activity of BET degraders and inhibitors
Figure 4. Antiproliferative and Myc-suppression activity of BET degraders and inhibitors
Figure 5. PROTACs’ SAR correlation plots."
Figure 5. PROTACs’ SAR correlation plots.”
J. Med. Chem. Special Issue on "Inducing Protein Degradation as a Therapeutic Strategy
J. Med. Chem. Special Issue on “Inducing Protein Degradation as a Therapeutic Strategy

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