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Selective PROTAC-mediated degradation of SMARCA2 is efficacious in SMARCA4 mutant cancers.
Cantley J, Ye X, Rousseau E, Januario T, Hamman BD, Rose CM, Cheung TK, Hinkle T, Soto L, Quinn C, Harbin A, Bortolon E, Chen X, Haskell R, Lin E, Yu SF, Del Rosario G, Chan E, Dunlap D, Koeppen H, Martin S, Merchant M, Grimmer M, Broccatelli F, Wang J, Pizzano J, Dragovich PS, Berlin M, Yauch RL. Cantley J, et al. Among authors: dragovich ps. Nat Commun. 2022 Nov 10;13(1):6814. doi: 10.1038/s41467-022-34562-5. Nat Commun. 2022. PMID: 36357397 Free PMC article.
The HER2-directed antibody-drug conjugate DHES0815A in advanced and/or metastatic breast cancer: preclinical characterization and phase 1 trial results.
Lewis GD, Li G, Guo J, Yu SF, Fields CT, Lee G, Zhang D, Dragovich PS, Pillow T, Wei B, Sadowsky J, Leipold D, Wilson T, Kamath A, Mamounas M, Lee MV, Saad O, Choeurng V, Ungewickell A, Monemi S, Crocker L, Kalinsky K, Modi S, Jung KH, Hamilton E, LoRusso P, Krop I, Schutten MM, Commerford R, Sliwkowski MX, Cho E. Lewis GD, et al. Among authors: dragovich ps. Nat Commun. 2024 Jan 11;15(1):466. doi: 10.1038/s41467-023-44533-z. Nat Commun. 2024. PMID: 38212321 Free PMC article. Clinical Trial.
Tissue distribution and retention drives efficacy of rapidly clearing VHL-based PROTACs.
Zhang D, Ma B, Dragovich PS, Ma L, Chen S, Chen EC, Ye X, Liu J, Pizzano J, Bortolon E, Chan E, Zhang X, Chen YC, Levy ES, Yauch RL, Khojasteh SC, Hop CECA. Zhang D, et al. Among authors: dragovich ps. Commun Med (Lond). 2024 May 16;4(1):87. doi: 10.1038/s43856-024-00505-y. Commun Med (Lond). 2024. PMID: 38755248 Free PMC article.
PROTACs Targeting BRM (SMARCA2) Afford Selective In Vivo Degradation over BRG1 (SMARCA4) and Are Active in BRG1 Mutant Xenograft Tumor Models.
Berlin M, Cantley J, Bookbinder M, Bortolon E, Broccatelli F, Cadelina G, Chan EW, Chen H, Chen X, Cheng Y, Cheung TK, Davenport K, DiNicola D, Gordon D, Hamman BD, Harbin A, Haskell R, He M, Hole AJ, Januario T, Kerry PS, Koenig SG, Li L, Merchant M, Pérez-Dorado I, Pizzano J, Quinn C, Rose CM, Rousseau E, Soto L, Staben LR, Sun H, Tian Q, Wang J, Wang W, Ye CS, Ye X, Zhang P, Zhou Y, Yauch R, Dragovich PS. Berlin M, et al. Among authors: dragovich ps. J Med Chem. 2024 Jan 25;67(2):1262-1313. doi: 10.1021/acs.jmedchem.3c01781. Epub 2024 Jan 5. J Med Chem. 2024. PMID: 38180485
Degrader-antibody conjugates.
Dragovich PS. Dragovich PS. Chem Soc Rev. 2022 May 23;51(10):3886-3897. doi: 10.1039/d2cs00141a. Chem Soc Rev. 2022. PMID: 35506708 Review.
Antibody-Drug Conjugates for Immunology.
Dragovich PS. Dragovich PS. J Med Chem. 2022 Mar 24;65(6):4496-4499. doi: 10.1021/acs.jmedchem.2c00339. Epub 2022 Mar 14. J Med Chem. 2022. PMID: 35285623
Structure-based optimization of hydroxylactam as potent, cell-active inhibitors of lactate dehydrogenase.
Wei B, Robarge K, Labadie SS, Chen J, Corson LB, DiPasquale A, Dragovich PS, Eigenbrot C, Evangelista M, Fauber BP, Hitz A, Hong R, Lai KW, Liu W, Ma S, Malek S, O'Brien T, Pang J, Peterson D, Salphati L, Sampath D, Sideris S, Ultsch M, Xu Z, Yen I, Yu D, Yue Q, Zhou A, Purkey HE. Wei B, et al. Among authors: dragovich ps. Bioorg Med Chem Lett. 2022 Mar 1;59:128576. doi: 10.1016/j.bmcl.2022.128576. Epub 2022 Jan 19. Bioorg Med Chem Lett. 2022. PMID: 35065235
91 results