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Lessons in PROTAC Design from Selective Degradation with a Promiscuous Warhead.
Bondeson DP, Smith BE, Burslem GM, Buhimschi AD, Hines J, Jaime-Figueroa S, Wang J, Hamman BD, Ishchenko A, Crews CM. Bondeson DP, et al. Among authors: wang j. Cell Chem Biol. 2018 Jan 18;25(1):78-87.e5. doi: 10.1016/j.chembiol.2017.09.010. Epub 2017 Nov 9. Cell Chem Biol. 2018. PMID: 29129718 Free PMC article.
Oral Estrogen Receptor PROTAC Vepdegestrant (ARV-471) Is Highly Efficacious as Monotherapy and in Combination with CDK4/6 or PI3K/mTOR Pathway Inhibitors in Preclinical ER+ Breast Cancer Models.
Gough SM, Flanagan JJ, Teh J, Andreoli M, Rousseau E, Pannone M, Bookbinder M, Willard R, Davenport K, Bortolon E, Cadelina G, Gordon D, Pizzano J, Macaluso J, Soto L, Corradi J, Digianantonio K, Drulyte I, Morgan A, Quinn C, Békés M, Ferraro C, Chen X, Wang G, Dong H, Wang J, Langley DR, Houston J, Gedrich R, Taylor IC. Gough SM, et al. Among authors: wang g, wang j. Clin Cancer Res. 2024 Aug 15;30(16):3549-3563. doi: 10.1158/1078-0432.CCR-23-3465. Clin Cancer Res. 2024. PMID: 38819400 Free PMC article.
The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study.
Burslem GM, Smith BE, Lai AC, Jaime-Figueroa S, McQuaid DC, Bondeson DP, Toure M, Dong H, Qian Y, Wang J, Crew AP, Hines J, Crews CM. Burslem GM, et al. Among authors: wang j. Cell Chem Biol. 2018 Jan 18;25(1):67-77.e3. doi: 10.1016/j.chembiol.2017.09.009. Epub 2017 Nov 9. Cell Chem Biol. 2018. PMID: 29129716 Free PMC article.
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: wang j. Nat Commun. 2022 Nov 10;13(1):6814. doi: 10.1038/s41467-022-34562-5. Nat Commun. 2022. PMID: 36357397 Free PMC article.
Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4.
Lu J, Qian Y, Altieri M, Dong H, Wang J, Raina K, Hines J, Winkler JD, Crew AP, Coleman K, Crews CM. Lu J, et al. Among authors: wang j. Chem Biol. 2015 Jun 18;22(6):755-63. doi: 10.1016/j.chembiol.2015.05.009. Epub 2015 Jun 4. Chem Biol. 2015. PMID: 26051217 Free PMC article.
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