Year |
Citation |
Score |
2019 |
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, et al. Maximizing ER-α Degradation Maximizes Activity in a Tamoxifen-Resistant Breast Cancer Model: Identification of GDC-0927. Acs Medicinal Chemistry Letters. 10: 50-55. PMID 30655946 DOI: 10.1021/Acsmedchemlett.8B00414 |
0.358 |
|
2019 |
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, et al. Correction: The selective estrogen receptor downregulator GDC-0810 is efficacious in diverse models of ER+ breast cancer. Elife. 8. PMID 30614786 DOI: 10.7554/Elife.44851 |
0.377 |
|
2018 |
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, et al. Selective estrogen receptor degraders with novel structural motifs induce regression in a tamoxifen-resistant breast cancer xenograft. Bioorganic & Medicinal Chemistry Letters. PMID 30587451 DOI: 10.1016/J.Bmcl.2018.12.042 |
0.386 |
|
2018 |
Kahraman M, Govek SP, Nagasawa JY, 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, et al. Abstract 1648: Discovery and evolution of orally bioavailable selective estrogen receptor degraders for ER+ breast cancer: From GDC-0810 to GDC-0927 Cancer Research. 78: 1648-1648. DOI: 10.1158/1538-7445.Am2018-1648 |
0.426 |
|
2016 |
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, et al. The selective estrogen receptor downregulator GDC-0810 is efficacious in diverse models of ER+ breast cancer. Elife. 5. PMID 27410477 DOI: 10.7554/Elife.15828 |
0.405 |
|
2015 |
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, et al. Optimization of an indazole series of selective estrogen receptor degraders: Tumor regression in a tamoxifen-resistant breast cancer xenograft. Bioorganic & Medicinal Chemistry Letters. PMID 26463130 DOI: 10.1016/J.Bmcl.2015.09.074 |
0.384 |
|
2015 |
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, ... ... Darimont B, et al. Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts. Journal of Medicinal Chemistry. 58: 4888-904. PMID 25879485 DOI: 10.1021/Acs.Jmedchem.5B00054 |
0.416 |
|
2015 |
Joseph J, Govek S, Darimont B, Brigham D, Aparicio A, Bischoff E, Kahraman M, Nannini M, Kaufman J, Lai A, Lee K, Oeh J, Lu N, Zhou W, Moon M, et al. Abstract 5053: Discovery of GDC-0810 a novel, non-steroidal selective estrogen receptor degrader with robust activity in pre-clinical models of endocrine-resistant breast cancer Cancer Research. 75: 5053-5053. DOI: 10.1158/1538-7445.Am2015-5053 |
0.457 |
|
2014 |
Joseph JD, Darimont B, Govek S, Brigham D, Qian J, Sensintaffar J, Shao G, Aparicio A, Kahraman M, Lai A, Lee K, Lu N, Nagasawa J, Moon M, Rix P, et al. Abstract 4757: A novel class of selective estrogen receptors degraders regresses tumors in pre-clinical models of endocrine-resistant breast cancer Cancer Research. 74: 4757-4757. DOI: 10.1158/1538-7445.Am2014-4757 |
0.452 |
|
2013 |
Joseph JD, Lu N, Qian J, Sensintaffar J, Shao G, Brigham D, Moon M, Maneval EC, Chen I, Darimont B, Hager JH. A clinically relevant androgen receptor mutation confers resistance to second-generation antiandrogens enzalutamide and ARN-509. Cancer Discovery. 3: 1020-9. PMID 23779130 DOI: 10.1158/2159-8290.Cd-13-0226 |
0.343 |
|
2013 |
Joseph JD, Darimont B, Govek S, Brigham D, Aparicio A, Kahraman M, Lai A, Lee K, Lu N, Nagasawa J, Kaufman J, Moon M, Prudente R, Qian J, Sensintaffar J, et al. Abstract A37: A novel class of selective estrogen receptor degraders display activity in pre-clinical models of ERα+ ovarian cancer Clinical Cancer Research. 19. DOI: 10.1158/1078-0432.Ovca13-A37 |
0.467 |
|
2012 |
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, ... ... Darimont B, et al. ARN-509: a novel antiandrogen for prostate cancer treatment. Cancer Research. 72: 1494-503. PMID 22266222 DOI: 10.1158/0008-5472.Can-11-3948 |
0.36 |
|
2012 |
Darimont B, Lu N, Sensintaffar J, Lee K, Aparicio A, Kaufman J, Bischoff E, Rix P, Heyman R, Smith N, Hager J, Joseph J, Grillot K, Qian J, Gang S, et al. Abstract A4: A novel class of selective ERα degraders acts as full antagonists/ inverse agonists and displays efficacy in pre-clinical models of endocrine-resistant breast cancer and endometrial cancer Clinical Cancer Research. 18. DOI: 10.1158/1078-0432.Mechres-A4 |
0.436 |
|
2012 |
Hager J, Darimont B, Joseph J, Govek S, Grillot K, Aparicio A, Bischoff E, Kahraman M, Kaufman J, Lai A, Lee K, Lu N, Nagasawa J, Prudente R, Qian J, et al. Abstract P6-04-12: Novel selective estrogen receptors degraders regress tumors in pre-clinical models of endocrine-resistant breast cancer Cancer Research. 72. DOI: 10.1158/0008-5472.Sabcs12-P6-04-12 |
0.449 |
|
2011 |
Darimont B, Govek S, Joseph J, Grillot K, Bischoff E, Aparicio A, Bonnefous C, Douglas K, Julien J, Kahraman M, Kaufman J, Lai A, Lee K, Lu N, Nagasawa J, et al. Abstract A133: A novel class of selective estrogen receptor degraders regresses tumors in preclinical models of endocrine-resistant breast cancer. Molecular Cancer Therapeutics. 18. DOI: 10.1158/1535-7163.Targ-11-A133 |
0.459 |
|
2008 |
Takayama S, Hostick U, Haendel M, Eisen J, Darimont B. An F-domain introduced by alternative splicing regulates activity of the zebrafish thyroid hormone receptor alpha. General and Comparative Endocrinology. 155: 176-89. PMID 17583703 DOI: 10.1016/J.Ygcen.2007.04.012 |
0.549 |
|
2007 |
Ricketson D, Hostick U, Fang L, Yamamoto KR, Darimont BD. A conformational switch in the ligand-binding domain regulates the dependence of the glucocorticoid receptor on Hsp90. Journal of Molecular Biology. 368: 729-41. PMID 17367809 DOI: 10.1016/J.Jmb.2007.02.057 |
0.361 |
|
2006 |
Fang L, Ricketson D, Getubig L, Darimont B. Unliganded and hormone-bound glucocorticoid receptors interact with distinct hydrophobic sites in the Hsp90 C-terminal domain. Proceedings of the National Academy of Sciences of the United States of America. 103: 18487-92. PMID 17130446 DOI: 10.1073/Pnas.0609163103 |
0.365 |
|
2006 |
Takayama S, Rogatsky I, Schwarcz LE, Darimont BD. The glucocorticoid receptor represses cyclin D1 by targeting the Tcf-beta-catenin complex. The Journal of Biological Chemistry. 281: 17856-63. PMID 16644723 DOI: 10.1074/Jbc.M602290200 |
0.457 |
|
2003 |
Rogatsky I, Wang JC, Derynck MK, Nonaka DF, Khodabakhsh DB, Haqq CM, Darimont BD, Garabedian MJ, Yamamoto KR. Target-specific utilization of transcriptional regulatory surfaces by the glucocorticoid receptor. Proceedings of the National Academy of Sciences of the United States of America. 100: 13845-50. PMID 14617768 DOI: 10.1073/Pnas.2336092100 |
0.415 |
|
2003 |
Darimont BD. Finding specificity within a conserved interaction site. Chemistry & Biology. 10: 675-6. PMID 12954326 DOI: 10.1016/S1074-5521(03)00177-7 |
0.364 |
|
2002 |
Serber Z, Lai HC, Yang A, Ou HD, Sigal MS, Kelly AE, Darimont BD, Duijf PH, Van Bokhoven H, McKeon F, Dötsch V. A C-terminal inhibitory domain controls the activity of p63 by an intramolecular mechanism. Molecular and Cellular Biology. 22: 8601-11. PMID 12446779 DOI: 10.1128/Mcb.22.24.8601-8611.2002 |
0.316 |
|
2001 |
Jenkins BD, Pullen CB, Darimont BD. Novel glucocorticoid receptor coactivator effector mechanisms Trends in Endocrinology and Metabolism. 12: 122-126. PMID 11306337 DOI: 10.1016/S1043-2760(00)00357-X |
0.464 |
|
1999 |
Hammer GD, Krylova I, Zhang Y, Darimont BD, Simpson K, Weigel NL, Ingraham HA. Phosphorylation of the nuclear receptor SF-1 modulates cofactor recruitment: integration of hormone signaling in reproduction and stress. Molecular Cell. 3: 521-6. PMID 10230405 DOI: 10.1016/S1097-2765(00)80480-3 |
0.429 |
|
1999 |
Hong H, Darimont BD, Ma H, Yang L, Yamamoto KR, Stallcup MR. An additional region of coactivator GRIP1 required for interaction with the hormone-binding domains of a subset of nuclear receptors. The Journal of Biological Chemistry. 274: 3496-502. PMID 9920895 DOI: 10.1074/Jbc.274.6.3496 |
0.302 |
|
1998 |
Darimont BD, Wagner RL, Apriletti JW, Stallcup MR, Kushner PJ, Baxter JD, Fletterick RJ, Yamamoto KR. Structure and specificity of nuclear receptor-coactivator interactions. Genes & Development. 12: 3343-56. PMID 9808622 DOI: 10.1101/Gad.12.21.3343 |
0.384 |
|
1995 |
Sterner R, Dahm A, Darimont B, Ivens A, Liebl W, Kirschner K. (Beta alpha)8-barrel proteins of tryptophan biosynthesis in the hyperthermophile Thermotoga maritima. The Embo Journal. 14: 4395-4402. DOI: 10.1002/J.1460-2075.1995.Tb00118.X |
0.337 |
|
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