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. 2020 Jun 8;11(8):1539–1547. doi: 10.1021/acsmedchemlett.0c00194

Figure 1.

Figure 1

(A) AR ligand 2 in complex with AR ligand binding domain (pdb id: 3v49). The linker attachment point is circled in red. (B) Structures of compounds 1–5, derived from AR ligands, for incorporation into PROTACs. The linker attachment point is indicated in red. (C) Proteolysis directing groups 6–9; the attachment point when incorporated into PROTACs is indicated in blue. (D) Lenalidomide bound to Cereblon E3 ubiquitin ligase (pdb id: 4ci2). The linker attachment point is circled in blue. (E) General AR PROTAC structure of PROTAC Sets 1 and 2.