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p300/CBP degradation is required to disable the active AR enhanceosome in prostate cancer.
Luo J, Chen Z, Qiao Y, Tien JC, Young E, Mannan R, Mahapatra S, He T, Eyunni S, Zhang Y, Zheng Y, Su F, Cao X, Wang R, Cheng Y, Seri R, George J, Shahine M, Miner SJ, Vaishampayan U, Wang M, Wang S, Parolia A, Chinnaiyan AM. Luo J, et al. Among authors: wang m, wang s, wang r. bioRxiv [Preprint]. 2024 May 23:2024.03.29.587346. doi: 10.1101/2024.03.29.587346. bioRxiv. 2024. PMID: 38586029 Free PMC article. Preprint.
Discovery of CBPD-409 as a Highly Potent, Selective, and Orally Efficacious CBP/p300 PROTAC Degrader for the Treatment of Advanced Prostate Cancer.
Chen Z, Wang M, Wu D, Zhao L, Metwally H, Jiang W, Wang Y, Bai L, McEachern D, Luo J, Wang M, Li Q, Matvekas A, Wen B, Sun D, Chinnaiyan AM, Wang S. Chen Z, et al. Among authors: wang y, wang m, wang s. J Med Chem. 2024 Apr 11;67(7):5351-5372. doi: 10.1021/acs.jmedchem.3c01789. Epub 2024 Mar 26. J Med Chem. 2024. PMID: 38530938
Discovery of ARD-1676 as a Highly Potent and Orally Efficacious AR PROTAC Degrader with a Broad Activity against AR Mutants for the Treatment of AR + Human Prostate Cancer.
Xiang W, Zhao L, Han X, Xu T, Kregel S, Wang M, Miao B, Qin C, Wang M, McEachern D, Lu J, Bai L, Yang CY, Kirchhoff PD, Takyi-Williams J, Wang L, Wen B, Sun D, Ator M, Mckean R, Chinnaiyan AM, Wang S. Xiang W, et al. Among authors: wang l, wang m, wang s. J Med Chem. 2023 Sep 28;66(18):13280-13303. doi: 10.1021/acs.jmedchem.3c01264. Epub 2023 Sep 8. J Med Chem. 2023. PMID: 37683104
Discovery of CBPD-268 as an Exceptionally Potent and Orally Efficacious CBP/p300 PROTAC Degrader Capable of Achieving Tumor Regression.
Chen Z, Wang M, Wu D, Bai L, Xu T, Metwally H, Wang Y, McEachern D, Zhao L, Li R, Takyi-Williams J, Wang M, Wang L, Li Q, Wen B, Sun D, Wang S. Chen Z, et al. Among authors: wang l, wang y, wang m, wang s. J Med Chem. 2024 Apr 11;67(7):5275-5304. doi: 10.1021/acs.jmedchem.3c02124. Epub 2024 Mar 13. J Med Chem. 2024. PMID: 38477974
Discovery of ARD-69 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor (AR) for the Treatment of Prostate Cancer.
Han X, Wang C, Qin C, Xiang W, Fernandez-Salas E, Yang CY, Wang M, Zhao L, Xu T, Chinnaswamy K, Delproposto J, Stuckey J, Wang S. Han X, et al. Among authors: wang m, wang c, wang s. J Med Chem. 2019 Jan 24;62(2):941-964. doi: 10.1021/acs.jmedchem.8b01631. Epub 2019 Jan 10. J Med Chem. 2019. PMID: 30629437
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