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Page 1
ARN-509: a novel antiandrogen for prostate cancer treatment.
Clegg NJ, Wongvipat J, Joseph JD, Tran C, Ouk S, Dilhas A, Chen Y, Grillot K, Bischoff ED, Cai L, Aparicio A, Dorow S, Arora V, Shao G, Qian J, Zhao H, Yang G, Cao C, Sensintaffar J, Wasielewska T, Herbert MR, Bonnefous C, Darimont B, Scher HI, Smith-Jones P, Klang M, Smith ND, De Stanchina E, Wu N, Ouerfelli O, Rix PJ, Heyman RA, Jung ME, Sawyers CL, Hager JH. Clegg NJ, et al. Among authors: aparicio a. Cancer Res. 2012 Mar 15;72(6):1494-503. doi: 10.1158/0008-5472.CAN-11-3948. Epub 2012 Jan 20. Cancer Res. 2012. PMID: 22266222 Free PMC article.
Identification 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. Lai A, et al. Among authors: aparicio a. J Med Chem. 2015 Jun 25;58(12):4888-904. doi: 10.1021/acs.jmedchem.5b00054. Epub 2015 May 22. J Med Chem. 2015. PMID: 25879485
The selective estrogen receptor downregulator GDC-0810 is efficacious in diverse models of ER+ breast cancer.
Joseph JD, Darimont B, Zhou W, Arrazate A, Young A, Ingalla E, Walter K, Blake RA, Nonomiya J, Guan Z, Kategaya L, Govek SP, Lai AG, Kahraman M, Brigham D, Sensintaffar J, Lu N, Shao G, Qian J, Grillot K, Moon M, Prudente R, Bischoff E, Lee KJ, Bonnefous C, Douglas KL, Julien JD, Nagasawa JY, Aparicio A, Kaufman J, Haley B, Giltnane JM, Wertz IE, Lackner MR, Nannini MA, Sampath D, Schwarz L, Manning HC, Tantawy MN, Arteaga CL, Heyman RA, Rix PJ, Friedman L, Smith ND, Metcalfe C, Hager JH. Joseph JD, et al. Among authors: aparicio a. Elife. 2016 Jul 13;5:e15828. doi: 10.7554/eLife.15828. Elife. 2016. PMID: 27410477 Free PMC article.
Optimization 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. Govek SP, et al. Among authors: aparicio am. Bioorg Med Chem Lett. 2015 Nov 15;25(22):5163-7. doi: 10.1016/j.bmcl.2015.09.074. Epub 2015 Oct 3. Bioorg Med Chem Lett. 2015. PMID: 26463130
Selective 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. Govek SP, et al. Among authors: aparicio am. Bioorg Med Chem Lett. 2019 Feb 1;29(3):367-372. doi: 10.1016/j.bmcl.2018.12.042. Epub 2018 Dec 19. Bioorg Med Chem Lett. 2019. PMID: 30587451
Identification of an Orally Bioavailable Chromene-Based Selective Estrogen Receptor Degrader (SERD) That Demonstrates Robust Activity in a Model of Tamoxifen-Resistant Breast Cancer.
Nagasawa J, Govek S, Kahraman M, Lai A, Bonnefous C, Douglas K, Sensintaffar J, Lu N, Lee K, Aparicio A, Kaufman J, Qian J, Shao G, Prudente R, Joseph JD, Darimont B, Brigham D, Maheu K, Heyman R, Rix PJ, Hager JH, Smith ND. Nagasawa J, et al. Among authors: aparicio a. J Med Chem. 2018 Sep 13;61(17):7917-7928. doi: 10.1021/acs.jmedchem.8b00921. Epub 2018 Sep 4. J Med Chem. 2018. PMID: 30086626
Maximizing ER-α Degradation Maximizes Activity in a Tamoxifen-Resistant Breast Cancer Model: Identification of GDC-0927.
Kahraman M, Govek SP, Nagasawa JY, Lai A, Bonnefous C, Douglas K, Sensintaffar J, Liu N, Lee K, Aparicio A, Kaufman J, Qian J, Shao G, Prudente R, Joseph JD, Darimont B, Brigham D, Heyman R, Rix PJ, Hager JH, Smith ND. Kahraman M, et al. Among authors: aparicio a. ACS Med Chem Lett. 2018 Dec 6;10(1):50-55. doi: 10.1021/acsmedchemlett.8b00414. eCollection 2019 Jan 10. ACS Med Chem Lett. 2018. PMID: 30655946 Free PMC article.
Correction: The selective estrogen receptor downregulator GDC-0810 is efficacious in diverse models of ER+ breast cancer.
Joseph JD, Darimont B, Zhou W, Arrazate A, Young A, Ingalla E, Walter K, Blake RA, Nonomiya J, Guan Z, Kategaya L, Govek SP, Lai AG, Kahraman M, Brigham D, Sensintaffar J, Lu N, Shao G, Qian J, Grillot K, Moon M, Prudente R, Bischoff E, Lee KJ, Bonnefous C, Douglas KL, Julien JD, Nagasawa JY, Aparicio A, Kaufman J, Haley B, Giltnane JM, Wertz IE, Lackner MR, Nannini MA, Sampath D, Schwarz L, Manning HC, Tantawy MN, Arteaga CL, Heyman RA, Rix PJ, Friedman L, Smith ND, Metcalfe C, Hager JH. Joseph JD, et al. Among authors: aparicio a. Elife. 2019 Jan 7;8:e44851. doi: 10.7554/eLife.44851. Elife. 2019. PMID: 30614786 Free PMC article.
Synthesis and structure-activity relationships of spirohydantoin-derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1).
Rowbottom MW, Vickers TD, Tamiya J, Zhang M, Dyck B, Grey J, Schwarz D, Heise CE, Hedrick M, Wen J, Tang H, Wang H, Fisher A, Aparicio A, Saunders J, Goodfellow VS. Rowbottom MW, et al. Among authors: aparicio a. Bioorg Med Chem Lett. 2007 Apr 15;17(8):2171-8. doi: 10.1016/j.bmcl.2007.01.104. Epub 2007 Feb 4. Bioorg Med Chem Lett. 2007. PMID: 17350839
379 results