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Novel Pyrrolopyridone Bromodomain and Extra-Terminal Motif (BET) Inhibitors Effective in Endocrine-Resistant ER+ Breast Cancer with Acquired Resistance to Fulvestrant and Palbociclib.
Li Y, Zhao J, Gutgesell LM, Shen Z, Ratia K, Dye K, Dubrovskyi O, Zhao H, Huang F, Tonetti DA, Thatcher GRJ, Xiong R. Li Y, et al. Among authors: gutgesell lm. J Med Chem. 2020 Jul 9;63(13):7186-7210. doi: 10.1021/acs.jmedchem.0c00456. Epub 2020 Jun 15. J Med Chem. 2020. PMID: 32453591 Free PMC article.
Design and Synthesis of Basic Selective Estrogen Receptor Degraders for Endocrine Therapy Resistant Breast Cancer.
Lu Y, Gutgesell LM, Xiong R, Zhao J, Li Y, Rosales CI, Hollas M, Shen Z, Gordon-Blake J, Dye K, Wang Y, Lee S, Chen H, He D, Dubrovyskyii O, Zhao H, Huang F, Lasek AW, Tonetti DA, Thatcher GRJ. Lu Y, et al. Among authors: gutgesell lm. J Med Chem. 2019 Dec 26;62(24):11301-11323. doi: 10.1021/acs.jmedchem.9b01580. Epub 2019 Dec 10. J Med Chem. 2019. PMID: 31746603 Free PMC article.
G1T48, an oral selective estrogen receptor degrader, and the CDK4/6 inhibitor lerociclib inhibit tumor growth in animal models of endocrine-resistant breast cancer.
Andreano KJ, Wardell SE, Baker JG, Desautels TK, Baldi R, Chao CA, Heetderks KA, Bae Y, Xiong R, Tonetti DA, Gutgesell LM, Zhao J, Sorrentino JA, Thompson DA, Bisi JE, Strum JC, Thatcher GRJ, Norris JD. Andreano KJ, et al. Among authors: gutgesell lm. Breast Cancer Res Treat. 2020 Apr;180(3):635-646. doi: 10.1007/s10549-020-05575-9. Epub 2020 Mar 4. Breast Cancer Res Treat. 2020. PMID: 32130619 Free PMC article.