PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 17654759-0 2007 Structure-activity relationships for a family of benzothiophene selective estrogen receptor modulators including raloxifene and arzoxifene. LY 353381 128-138 estrogen receptor 1 Homo sapiens 74-91 25378950-3 2014 Other selective estrogen receptor modulators (SERMs), such as raloxifene, arzoxifene, and lasofoxifene, have been shown to reduce the incidence of breast cancer by 50%-80%. LY 353381 74-84 estrogen receptor 1 Homo sapiens 16-33 22484799-11 2012 These findings demonstrate that in this study arzoxifene reduced the risk of ER-positive breast cancer in this population of postmenopausal women with low bone mass or osteoporosis, an effect similar to that seen with other SERMs. LY 353381 46-56 estrogen receptor 1 Homo sapiens 77-79 21993078-1 2012 OBJECTIVE: The aim of this study was to report the gynecologic safety findings from the Generations trial, a phase 3 study of the selective estrogen receptor modulator (SERM), arzoxifene. LY 353381 176-186 estrogen receptor 1 Homo sapiens 140-157 19798460-7 2010 RESULTS: All arzoxifene doses significantly reduced osteocalcin (primary endpoint), type 1 collagen C-telopeptide, bone specific alkaline phosphatase, and procollagen type I amino-terminal propeptide versus placebo, and increased lumbar spine BMD. LY 353381 13-23 bone gamma-carboxyglutamate protein Homo sapiens 52-63 19477949-0 2009 Resistance to antiestrogen arzoxifene is mediated by overexpression of cyclin D1. LY 353381 27-37 cyclin D1 Homo sapiens 71-80 19477949-3 2009 Arzoxifene is an effective growth inhibitor of ERalpha-positive breast cancer cells, including tamoxifen-resistant tumors. LY 353381 0-10 estrogen receptor 1 Homo sapiens 47-54 19477949-4 2009 In this study, we show that overexpression of a regular component of the ERalpha transcription factor complex, cyclin D1, which occurs in approximately 40% of breast cancer patients, renders cells resistant to the new promising antiestrogen, arzoxifene. LY 353381 242-252 estrogen receptor 1 Homo sapiens 73-80 19477949-4 2009 In this study, we show that overexpression of a regular component of the ERalpha transcription factor complex, cyclin D1, which occurs in approximately 40% of breast cancer patients, renders cells resistant to the new promising antiestrogen, arzoxifene. LY 353381 242-252 cyclin D1 Homo sapiens 111-120 19477949-5 2009 Overexpression of cyclin D1 alters the conformation of ERalpha in the presence of arzoxifene. LY 353381 82-92 cyclin D1 Homo sapiens 18-27 19477949-5 2009 Overexpression of cyclin D1 alters the conformation of ERalpha in the presence of arzoxifene. LY 353381 82-92 estrogen receptor 1 Homo sapiens 55-62 19477949-6 2009 In this altered conformation, ERalpha still recruits RNA polymerase II to an estrogen response element-containing promoter, inducing transcription of an ERalpha-dependent reporter gene and of endogenous pS2, and promoting arzoxifene-stimulated growth of MCF-7 cells. LY 353381 222-232 estrogen receptor 1 Homo sapiens 30-37 19477949-7 2009 Arzoxifene is then converted from an ERalpha antagonist into an agonist. LY 353381 0-10 estrogen receptor 1 Homo sapiens 37-44 19477949-8 2009 This can be explained by a stabilization of the ERalpha/steroid receptor coactivator-1 complex in the presence of arzoxifene, only when cyclin D1 is overexpressed. LY 353381 114-124 estrogen receptor 1 Homo sapiens 48-55 19477949-8 2009 This can be explained by a stabilization of the ERalpha/steroid receptor coactivator-1 complex in the presence of arzoxifene, only when cyclin D1 is overexpressed. LY 353381 114-124 cyclin D1 Homo sapiens 136-145 17876041-1 2007 The benzothiophene selective estrogen receptor modulators (SERM) raloxifene and arzoxifene are in clinical use and clinical trials for chemoprevention of breast cancer and other indications. LY 353381 80-90 estrogen receptor 1 Homo sapiens 29-46 17876041-6 2007 Livers from female, juvenile rats treated for 3 days with estradiol and/or with the benzothiophene SERMs arzoxifene, DMA, and F-DMA showed substantial induction of NQO1 by the benzothiophene SERMs. LY 353381 105-115 NAD(P)H quinone dehydrogenase 1 Rattus norvegicus 164-168 17020999-0 2006 The combination of the rexinoid, LG100268, and a selective estrogen receptor modulator, either arzoxifene or acolbifene, synergizes in the prevention and treatment of mammary tumors in an estrogen receptor-negative model of breast cancer. LY 353381 95-105 estrogen receptor 1 (alpha) Mus musculus 59-76 17020999-0 2006 The combination of the rexinoid, LG100268, and a selective estrogen receptor modulator, either arzoxifene or acolbifene, synergizes in the prevention and treatment of mammary tumors in an estrogen receptor-negative model of breast cancer. LY 353381 95-105 estrogen receptor 1 (alpha) Mus musculus 188-205 12927029-3 2003 Furthermore, new selective estrogen-receptor modulators such as arzoxifene, currently under clinical development, offer the possibility of selecting one with a more ideal pharmacological profile for treatment and prevention of breast cancer. LY 353381 64-74 estrogen receptor 1 Homo sapiens 27-44 15720120-0 2005 Bioactivation of the selective estrogen receptor modulator desmethylated arzoxifene to quinoids: 4"-fluoro substitution prevents quinoid formation. LY 353381 73-83 estrogen receptor 1 Homo sapiens 31-48 15150113-0 2004 The selective estrogen receptor modulator arzoxifene and the rexinoid LG100268 cooperate to promote transforming growth factor beta-dependent apoptosis in breast cancer. LY 353381 42-52 distal membrane arm assembly component 2 like Rattus norvegicus 120-131 14559845-1 2003 Arzoxifene (ARZ) is a selective estrogen receptor (ER) modulator with greater bioavailability than raloxifene which is being developed as treatment for breast cancer. LY 353381 0-10 estrogen receptor 1 Homo sapiens 32-49 14559845-1 2003 Arzoxifene (ARZ) is a selective estrogen receptor (ER) modulator with greater bioavailability than raloxifene which is being developed as treatment for breast cancer. LY 353381 0-10 estrogen receptor 1 Homo sapiens 51-53 14559845-1 2003 Arzoxifene (ARZ) is a selective estrogen receptor (ER) modulator with greater bioavailability than raloxifene which is being developed as treatment for breast cancer. LY 353381 12-15 estrogen receptor 1 Homo sapiens 32-49 14559845-1 2003 Arzoxifene (ARZ) is a selective estrogen receptor (ER) modulator with greater bioavailability than raloxifene which is being developed as treatment for breast cancer. LY 353381 12-15 estrogen receptor 1 Homo sapiens 51-53 14559845-7 2003 ARZ and TAM resulted in a significant (P < 0.001) increase in ER expression and reduction in progesterone receptor expression, whereas changes in cyclin D1 score were inversely related to p27(kip1) score. LY 353381 0-3 progesterone receptor Homo sapiens 96-117 14559845-7 2003 ARZ and TAM resulted in a significant (P < 0.001) increase in ER expression and reduction in progesterone receptor expression, whereas changes in cyclin D1 score were inversely related to p27(kip1) score. LY 353381 0-3 interferon alpha inducible protein 27 Homo sapiens 191-194 14559845-7 2003 ARZ and TAM resulted in a significant (P < 0.001) increase in ER expression and reduction in progesterone receptor expression, whereas changes in cyclin D1 score were inversely related to p27(kip1) score. LY 353381 0-3 cyclin dependent kinase inhibitor 1B Homo sapiens 195-199 15149724-4 2004 Northern analysis revealed that arzoxifene exerts a statistically significant inhibition of pS2 and progesterone receptor B mRNA expression. LY 353381 32-42 trefoil factor 1 Homo sapiens 92-95 14559845-0 2003 Comparison of the selective estrogen receptor modulator arzoxifene (LY353381) with tamoxifen on tumor growth and biomarker expression in an MCF-7 human breast cancer xenograft model. LY 353381 56-66 estrogen receptor 1 Homo sapiens 28-45 14559845-0 2003 Comparison of the selective estrogen receptor modulator arzoxifene (LY353381) with tamoxifen on tumor growth and biomarker expression in an MCF-7 human breast cancer xenograft model. LY 353381 68-76 estrogen receptor 1 Homo sapiens 28-45 14555537-8 2003 CONCLUSIONS: Arzoxifene and 4OHT can inhibit specifically the repopulation of ER+ breast cancer cells between courses of chemotherapy. LY 353381 13-23 estrogen receptor 1 Homo sapiens 78-80 11283133-0 2001 Phase I study of a third-generation selective estrogen receptor modulator, LY353381.HCL, in metastatic breast cancer. LY 353381 75-83 estrogen receptor 1 Homo sapiens 46-63 11911997-9 2002 There was a significant increase in TPH total signal (positive pixelsxOD) with E, raloxifene and arzoxifene, respectively. LY 353381 97-107 tryptophan hydroxylase 1 Macaca mulatta 36-39 11911997-13 2002 In conclusion, the selective estrogen receptor modulators, raloxifene and arzoxifene, act in a manner similar to natural E on TPH and SERT mRNA expression in serotonin neurons. LY 353381 74-84 tryptophan hydroxylase 1 Macaca mulatta 126-129 11911997-13 2002 In conclusion, the selective estrogen receptor modulators, raloxifene and arzoxifene, act in a manner similar to natural E on TPH and SERT mRNA expression in serotonin neurons. LY 353381 74-84 solute carrier family 6 member 4 Macaca mulatta 134-138 11911997-14 2002 This suggests that raloxifene and arzoxifene are agonists at ER beta in the context of the serotonin neuron. LY 353381 34-44 estrogen receptor 2 Macaca mulatta 61-68 11283133-1 2001 PURPOSE: We conducted this phase I trial to determine the safety and toxicity profile of LY353381.HCl-a novel, potent, third-generation selective estrogen receptor modulator (SERM)-because this benzothiophene derivative demonstrated an SERM profile in preclinical studies. LY 353381 89-97 estrogen receptor 1 Homo sapiens 146-163 10965916-5 2000 The dose of chemical necessary to activate IGF-I signaling varied, with the order of potency: E2 = diethylstilbestrol > LY353381 > 4-hydroxytamoxifen > genistein > HPTE > bisphenol A. LY 353381 123-131 insulin-like growth factor 1 Mus musculus 43-48 9794476-13 1998 Additionally, when PTH was discontinued at 45 days, LY353381 x HCl prevented the rapid loss of bone observed in controls. LY 353381 52-60 parathyroid hormone Equus caballus 19-22