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FMC-2022-0147 SUpllementary Information.docx (3.64 MB)

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

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posted on 2022-10-10, 08:45 authored by Wu Du


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


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