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509 results

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ESR1 F404 Mutations and Acquired Resistance to Fulvestrant in ESR1-Mutant Breast Cancer.
Kingston B, Pearson A, Herrera-Abreu MT, Sim LX, Cutts RJ, Shah H, Moretti L, Kilburn LS, Johnson H, Macpherson IR, Ring A, Bliss JM, Hou Y, Toy W, Katzenellenbogen JA, Chandarlapaty S, Turner NC. Kingston B, et al. Among authors: katzenellenbogen ja. Cancer Discov. 2024 Feb 8;14(2):274-289. doi: 10.1158/2159-8290.CD-22-1387. Cancer Discov. 2024. PMID: 37982575 Free PMC article.
PI3K inhibition results in enhanced estrogen receptor function and dependence in hormone receptor-positive breast cancer.
Bosch A, Li Z, Bergamaschi A, Ellis H, Toska E, Prat A, Tao JJ, Spratt DE, Viola-Villegas NT, Castel P, Minuesa G, Morse N, Rodón J, Ibrahim Y, Cortes J, Perez-Garcia J, Galvan P, Grueso J, Guzman M, Katzenellenbogen JA, Kharas M, Lewis JS, Dickler M, Serra V, Rosen N, Chandarlapaty S, Scaltriti M, Baselga J. Bosch A, et al. Among authors: katzenellenbogen ja. Sci Transl Med. 2015 Apr 15;7(283):283ra51. doi: 10.1126/scitranslmed.aaa4442. Sci Transl Med. 2015. PMID: 25877889 Free PMC article.
Estrogen receptor alpha somatic mutations Y537S and D538G confer breast cancer endocrine resistance by stabilizing the activating function-2 binding conformation.
Fanning SW, Mayne CG, Dharmarajan V, Carlson KE, Martin TA, Novick SJ, Toy W, Green B, Panchamukhi S, Katzenellenbogen BS, Tajkhorshid E, Griffin PR, Shen Y, Chandarlapaty S, Katzenellenbogen JA, Greene GL. Fanning SW, et al. Among authors: katzenellenbogen bs, katzenellenbogen ja. Elife. 2016 Feb 2;5:e12792. doi: 10.7554/eLife.12792. Elife. 2016. PMID: 26836308 Free PMC article.
Activating ESR1 Mutations Differentially Affect the Efficacy of ER Antagonists.
Toy W, Weir H, Razavi P, Lawson M, Goeppert AU, Mazzola AM, Smith A, Wilson J, Morrow C, Wong WL, De Stanchina E, Carlson KE, Martin TS, Uddin S, Li Z, Fanning S, Katzenellenbogen JA, Greene G, Baselga J, Chandarlapaty S. Toy W, et al. Among authors: katzenellenbogen ja. Cancer Discov. 2017 Mar;7(3):277-287. doi: 10.1158/2159-8290.CD-15-1523. Epub 2016 Dec 16. Cancer Discov. 2017. PMID: 27986707 Free PMC article.
New Class of Selective Estrogen Receptor Degraders (SERDs): Expanding the Toolbox of PROTAC Degrons.
Wang L, Guillen VS, Sharma N, Flessa K, Min J, Carlson KE, Toy W, Braqi S, Katzenellenbogen BS, Katzenellenbogen JA, Chandarlapaty S, Sharma A. Wang L, et al. Among authors: katzenellenbogen bs, katzenellenbogen ja. ACS Med Chem Lett. 2018 Jul 5;9(8):803-808. doi: 10.1021/acsmedchemlett.8b00106. eCollection 2018 Aug 9. ACS Med Chem Lett. 2018. PMID: 30128071 Free PMC article.
Antagonists for Constitutively Active Mutant Estrogen Receptors: Insights into the Roles of Antiestrogen-Core and Side-Chain.
Sharma A, Toy W, Guillen VS, Sharma N, Min J, Carlson KE, Mayne CG, Lin S, Sabio M, Greene G, Katzenellenbogen BS, Chandarlapaty S, Katzenellenbogen JA. Sharma A, et al. Among authors: katzenellenbogen bs, katzenellenbogen ja. ACS Chem Biol. 2018 Dec 21;13(12):3374-3384. doi: 10.1021/acschembio.8b00877. Epub 2018 Nov 26. ACS Chem Biol. 2018. PMID: 30404440 Free PMC article.
The SERM/SERD bazedoxifene disrupts ESR1 helix 12 to overcome acquired hormone resistance in breast cancer cells.
Fanning SW, Jeselsohn R, Dharmarajan V, Mayne CG, Karimi M, Buchwalter G, Houtman R, Toy W, Fowler CE, Han R, Lainé M, Carlson KE, Martin TA, Nowak J, Nwachukwu JC, Hosfield DJ, Chandarlapaty S, Tajkhorshid E, Nettles KW, Griffin PR, Shen Y, Katzenellenbogen JA, Brown M, Greene GL. Fanning SW, et al. Among authors: katzenellenbogen ja. Elife. 2018 Nov 29;7:e37161. doi: 10.7554/eLife.37161. Elife. 2018. PMID: 30489256 Free PMC article.
Defining the Energetic Basis for a Conformational Switch Mediating Ligand-Independent Activation of Mutant Estrogen Receptors in Breast Cancer.
Mayne CG, Toy W, Carlson KE, Bhatt T, Fanning SW, Greene GL, Katzenellenbogen BS, Chandarlapaty S, Katzenellenbogen JA, Tajkhorshid E. Mayne CG, et al. Among authors: katzenellenbogen bs, katzenellenbogen ja. Mol Cancer Res. 2021 Sep;19(9):1559-1570. doi: 10.1158/1541-7786.MCR-20-1017. Epub 2021 May 21. Mol Cancer Res. 2021. PMID: 34021071 Free PMC article.
509 results