Advances in AR-targeting chimeras: a case study of proteolysis-targeting chimeras from bench to bedside - Supplementary Information.docx

  

Figure S1. Therapy options in the management of prostate cancer [9b]

  

Figure S2. The structure of full-length AR [11] 

  

Figure S3. Examples of hydrophobic tags that promoted protein degradation

  

Figure S4. AR degrader SARD279 and SARD033 [24]

  

Figure S5. AR degrader SNIPER(AR)-51

  

Figure S6. Structures of ARCC-4 and its epimer

  

Figure S7. in vitro profile of ARCC-4 [27]

  

Figure S8. Degradation of AR point mutants by ARCC-4 [27]

  

Figure S9. CRNB E3 ligand-based AR PROTACs PAP508 and Compound 13b

  

Figure S10. Synthesis of AR PROTACs using click chemistry

  

Figure S11. AR binder comparison in PROTACs [33]

  

Figure S12. Antitumor efficacy of ARD-61 [33]

  

Figure S13. AR ligand moiety modification in A301

  

Figure S14. Optimization strategy of TD-802

  

Figure S15. ARD-2128 reduced AR level in tumor tissue upon single oral dose of 20 mg/kg [37]

  

Table S1. ARD-2128 drug concentrations in plasma and tumor tissues after single dose of 20 mg/kg

  

Figure S16. Antitumor efficacy of ARD-2128 [37]

  

Table S2. Tissue distribution of ARD-2585 in mice bearing VCaP tumor [38]

  

Figure S17. PD study of ARD-2585 [38]

  

Figure S18. ARD-2585 was efficacious in VCaP xenograft mice model [38].

  

Figure S19. AR DBD targeting PROTACs