Targeting the Estrogen Receptor for the Treatment of Breast Cancer: Recent Advances and Challenges.
Rej RK, Thomas JE, Acharyya RK, Rae JM, Wang S.
J Med Chem · review; journal article · DOI 10.1021/acs.jmedchem.3c00136 PUBLIKATIONSREGISTRET
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Lu J, Chan CC, Sun D, Hu G, He H, Li J, Dong J, Liu K, Shen L, Hu L, Gu Q, Chen S, Wang T, Gong T, Tang W, Li X, Zhu X, Zeng X, Zhu Y, Xia Y, Huang Y, Zhu Y, Liu Z, Ding CZ.
Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2022.128734GDC-9545 (Giredestrant): A Potent and Orally Bioavailable Selective Estrogen Receptor Antagonist and Degrader with an Exceptional Preclinical Profile for ER+ Breast Cancer.
Liang J, Zbieg JR, Blake RA, Chang JH, Daly S, DiPasquale AG, Friedman LS, Gelzleichter T, Gill M, Giltnane JM, Goodacre S, Guan J, Hartman SJ, Ingalla ER, Kategaya L, Kiefer JR, Kleinheinz T, Labadie SS, Lai T, Li J, Liao J, Liu Z, Mody V, McLean N, Metcalfe C, Nannini MA, Oeh J, O'Rourke MG, Ortwine DF, Ran Y, Ray NC, Roussel F, Sambrone A, Sampath D, Schutt LK, Vinogradova M, Wai J, Wang T, Wertz IE, White JR, Yeap SK, Young A, Zhang B, Zheng X, Zhou W, Zhong Y, Wang X.
J Med Chem · research support, u.s. gov't, non-p.h.s.; journal article; research support, n.i.h., extramural · DOI 10.1021/acs.jmedchem.1c00847Discovery of GNE-149 as a Full Antagonist and Efficient Degrader of Estrogen Receptor alpha for ER+ Breast Cancer.
Liang J, Blake R, Chang J, Friedman LS, Goodacre S, Hartman S, Ingalla ER, Kiefer JR, Kleinheinz T, Labadie S, Li J, Lai KW, Liao J, Mody V, McLean N, Metcalfe C, Nannini M, Otwine D, Ran Y, Ray N, Roussel F, Sambrone A, Sampath D, Vinogradova M, Wai J, Wang T, Yeap K, Young A, Zbieg J, Zhang B, Zheng X, Zhong Y, Wang X.
ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/acsmedchemlett.0c00224Selective estrogen receptor degraders with novel structural motifs induce regression in a tamoxifen-resistant breast cancer xenograft.
Govek SP, Bonnefous C, Julien JD, Nagasawa JY, Kahraman M, Lai AG, Douglas KL, Aparicio AM, Darimont BD, Grillot KL, Joseph JD, Kaufman JA, Lee KJ, Lu N, Moon MJ, Prudente RY, Sensintaffar J, Rix PJ, Hager JH, Smith ND.
Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2018.12.042Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer.
Tria GS, Abrams T, Baird J, Burks HE, Firestone B, Gaither LA, Hamann LG, He G, Kirby CA, Kim S, Lombardo F, Macchi KJ, McDonnell DP, Mishina Y, Norris JD, Nunez J, Springer C, Sun Y, Thomsen NM, Wang C, Wang J, Yu B, Tiong-Yip CL, Peukert S.
J Med Chem · research support, u.s. gov't, non-p.h.s.; journal article · DOI 10.1021/acs.jmedchem.7b01682Novel Selective Estrogen Receptor Downregulators (SERDs) Developed against Treatment-Resistant Breast Cancer.
Xiong R, Zhao J, Gutgesell LM, Wang Y, Lee S, Karumudi B, Zhao H, Lu Y, Tonetti DA, Thatcher GR.
J Med Chem · research-article; journal article; research support, n.i.h., extramural · DOI 10.1021/acs.jmedchem.6b01355Optimization of an indazole series of selective estrogen receptor degraders: Tumor regression in a tamoxifen-resistant breast cancer xenograft.
Govek SP, Nagasawa JY, Douglas KL, Lai AG, Kahraman M, Bonnefous C, Aparicio AM, Darimont BD, Grillot KL, Joseph JD, Kaufman JA, Lee KJ, Lu N, Moon MJ, Prudente RY, Sensintaffar J, Rix PJ, Hager JH, Smith ND.
Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2015.09.074Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts.
Lai A, Kahraman M, Govek S, Nagasawa J, Bonnefous C, Julien J, Douglas K, Sensintaffar J, Lu N, Lee KJ, Aparicio A, Kaufman J, Qian J, Shao G, Prudente R, Moon MJ, Joseph JD, Darimont B, Brigham D, Grillot K, Heyman R, Rix PJ, Hager JH, Smith ND.
J Med Chem · journal article · DOI 10.1021/acs.jmedchem.5b00054