PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 32531951-4 2020 LNCaP cells incubated for 30 days in charcoal-stripped medium or with the androgen receptor antagonist 2-hydroxyflutamide developed neuroendocrine morphology and increased the expression of the neuroendocrine markers betaIII-tubulin and neuron specific enolase (NSE). hydroxyflutamide 103-121 androgen receptor Homo sapiens 74-91 3402389-4 1988 Mediation of the action of E2 by the androgen receptor is indicated by the absence of interference of E2 action by the antiestrogen LY156758 while the antiandrogen hydroxyflutamide (3 microM) caused a 50% inhibition of E2 action. hydroxyflutamide 164-180 androgen receptor Homo sapiens 37-54 2788775-6 1989 In comparison the antiandrogens were strong competitors of [3H]R1881 binding to the androgen receptor, the order of decreasing potency, determined from ID50 (mumol/l) values were CPA (0.073) greater than ICI 176344 (0.4) greater than anandron (0.63) greater than hydroxyflutamide (1) greater than flutamide (greater than 100). hydroxyflutamide 263-279 androgen receptor Homo sapiens 84-101 2521824-6 1989 The mitogenic effect of DHT on bone cells was inhibited by antiandrogens (hydroxyflutamide and cyproterone acetate) which compete for binding to the androgen receptor. hydroxyflutamide 74-90 androgen receptor Homo sapiens 149-166 29720561-6 2018 Meanwhile, an antiandrogen hydroxyflutamide enhanced them in AR-positive cells cultured in the presence of androgens. hydroxyflutamide 27-43 androgen receptor Homo sapiens 61-63 31470108-6 2019 Blockade of the AR activity by pre-treatment with an AR antagonist, hydroxyflutamide (HF), or knockdown of AR expression using the shRNA technique abolished the R1881-induced HUVEC proliferation inhibition, suggesting that AR activation can inhibit endothelial cell proliferation. hydroxyflutamide 68-84 androgen receptor Homo sapiens 16-18 31470108-6 2019 Blockade of the AR activity by pre-treatment with an AR antagonist, hydroxyflutamide (HF), or knockdown of AR expression using the shRNA technique abolished the R1881-induced HUVEC proliferation inhibition, suggesting that AR activation can inhibit endothelial cell proliferation. hydroxyflutamide 86-88 androgen receptor Homo sapiens 16-18 30615932-7 2019 Specific compounds inhibit the transactivation of wild-type AR as well as AR mutants that render treatment resistance to hydroxyflutamide, bicalutamide and the second-generation AR antagonist enzalutamide. hydroxyflutamide 121-137 androgen receptor Homo sapiens 60-62 30615932-7 2019 Specific compounds inhibit the transactivation of wild-type AR as well as AR mutants that render treatment resistance to hydroxyflutamide, bicalutamide and the second-generation AR antagonist enzalutamide. hydroxyflutamide 121-137 androgen receptor Homo sapiens 74-76 30615932-7 2019 Specific compounds inhibit the transactivation of wild-type AR as well as AR mutants that render treatment resistance to hydroxyflutamide, bicalutamide and the second-generation AR antagonist enzalutamide. hydroxyflutamide 121-137 androgen receptor Homo sapiens 74-76 26614265-13 2016 Such effects were reverted by hydroxyflutamide, an inhibitor of androgen receptor. hydroxyflutamide 30-46 androgen receptor Homo sapiens 64-81 29392883-6 2018 This suggests the 4,4"-bisphenols, like hydroxyflutamide, are androgen receptor antagonists. hydroxyflutamide 40-56 androgen receptor Homo sapiens 62-79 28711501-6 2017 We show for the first time that the anti-androgenic properties of progesterone and drospirenone are similar to the well-known AR antagonist hydroxyflutamide, while nomegestrol acetate is more potent and nestorone less potent than both hydroxyflutamide and progesterone. hydroxyflutamide 140-156 androgen receptor Homo sapiens 126-128 28832499-0 2017 A Molecular Modeling Study of the Hydroxyflutamide Resistance Mechanism Induced by Androgen Receptor Mutations. hydroxyflutamide 34-50 androgen receptor Homo sapiens 83-100 28832499-1 2017 Hydroxyflutamide (HF), an active metabolite of the first generation antiandrogen flutamide, was used in clinic to treat prostate cancer targeting androgen receptor (AR). hydroxyflutamide 0-16 androgen receptor Homo sapiens 146-163 28832499-1 2017 Hydroxyflutamide (HF), an active metabolite of the first generation antiandrogen flutamide, was used in clinic to treat prostate cancer targeting androgen receptor (AR). hydroxyflutamide 0-16 androgen receptor Homo sapiens 165-167 28832499-1 2017 Hydroxyflutamide (HF), an active metabolite of the first generation antiandrogen flutamide, was used in clinic to treat prostate cancer targeting androgen receptor (AR). hydroxyflutamide 18-20 androgen receptor Homo sapiens 146-163 28832499-1 2017 Hydroxyflutamide (HF), an active metabolite of the first generation antiandrogen flutamide, was used in clinic to treat prostate cancer targeting androgen receptor (AR). hydroxyflutamide 18-20 androgen receptor Homo sapiens 165-167 28163245-0 2017 Anti-androgen 2-hydroxyflutamide modulates cadherin, catenin and androgen receptor phosphorylation in androgen-sensitive LNCaP and androgen-independent PC3 prostate cancer cell lines acting via PI3K/Akt and MAPK/ERK1/2 pathways. hydroxyflutamide 14-32 androgen receptor Homo sapiens 65-82 28163245-1 2017 This study aimed to investigate rapid effect of anti-androgen 2-hydroxyflutamide (HF) on cadherin/catenin complex and androgen receptor (AR) phosphorylation in prostate cancer cell lines. hydroxyflutamide 62-80 androgen receptor Homo sapiens 118-135 23436650-5 2013 MDV3100, however, shares its 4-cyano-3-(trifluoromethyl)phenyl group with bicalutamide and hydroxyflutamide required for binding to the AR. hydroxyflutamide 91-107 androgen receptor Homo sapiens 136-138 26265743-0 2015 A Screen of Approved Drugs Identifies the Androgen Receptor Antagonist Flutamide and Its Pharmacologically Active Metabolite 2-Hydroxy-Flutamide as Heterotropic Activators of Cytochrome P450 3A In Vitro and In Vivo. hydroxyflutamide 125-144 androgen receptor Homo sapiens 42-59 24065547-6 2013 Treatment with T induced dose- and time-dependent increase of moesin expression and phosphorylation, which was inhibited by the addition of androgen receptor antagonist hydroxyflutamide (HF). hydroxyflutamide 169-185 androgen receptor Homo sapiens 140-157 24065547-6 2013 Treatment with T induced dose- and time-dependent increase of moesin expression and phosphorylation, which was inhibited by the addition of androgen receptor antagonist hydroxyflutamide (HF). hydroxyflutamide 187-189 androgen receptor Homo sapiens 140-157 26813233-2 2016 All current non-steroidal AR antagonists, such as hydroxyflutamide, bicalutamide, and enzalutamide, target the androgen binding site of the receptor, competing with endogenous androgenic steroids. hydroxyflutamide 50-66 androgen receptor Homo sapiens 26-28 23889773-7 2013 Subsequent in vitro experiments demonstrated that APP mRNA expression was significantly induced by biologically active androgen dihydrotestosterone in both a dose-dependent and a time-dependent manner in MCF-7 breast carcinoma cells, which was potently suppressed by an AR blocker hydroxyflutamide. hydroxyflutamide 281-297 androgen receptor Homo sapiens 270-272 23462715-5 2013 Among the compounds synthesized, AR-selective ligand (S,R)-3b exhibited more potent anti-androgenic activity (IC50=0.072 muM) than hydroxyflutamide, a well-known androgen antagonist (IC50=1.4 muM), in SC-3 cell proliferation assay. hydroxyflutamide 131-147 androgen receptor Homo sapiens 33-35 22922989-7 2012 Combined treatment of EGF and dihydrotestosterone (DHT) further induced AR transactivation while an AR antagonist, hydroxyflutamide (HF), abolished the effect of not only DHT but also EGF. hydroxyflutamide 139-155 androgen receptor Homo sapiens 124-126 22922989-7 2012 Combined treatment of EGF and dihydrotestosterone (DHT) further induced AR transactivation while an AR antagonist, hydroxyflutamide (HF), abolished the effect of not only DHT but also EGF. hydroxyflutamide 157-159 androgen receptor Homo sapiens 124-126 20521823-2 2010 We previously developed a carborane-containing AR antagonist, 3-(12-hydroxymethyl-1,12-dicarba-closo-dodecaborane-1-yl)benzonitrile (BA341), which was more potent than hydroxyflutamide (4) but acted as an agonist toward LNCaP prostate cancer cells expressing T877A AR mutant. hydroxyflutamide 168-184 androgen receptor Homo sapiens 47-49 22746350-5 2012 Notably, 6a maintains its antiandrogenic activity with AR mutants W741L and T877A commonly observed and activated by bicalutamide and hydroxyflutamide, respectively, in prostate cancer patients. hydroxyflutamide 134-150 androgen receptor Homo sapiens 55-57 22522230-5 2012 We examined the influence of an androgen receptor antagonist, 2-hydroxyflutamide (2-Hf), on the incidence of apoptosis in cultured porcine granulosa cells. hydroxyflutamide 62-80 androgen receptor Homo sapiens 32-49 22522230-5 2012 We examined the influence of an androgen receptor antagonist, 2-hydroxyflutamide (2-Hf), on the incidence of apoptosis in cultured porcine granulosa cells. hydroxyflutamide 82-86 androgen receptor Homo sapiens 32-49 21243325-8 2011 This suggested that OH-flutamide enhanced the growth-inhibitory activity of 5-FU in CDX25R cells by reducing TS expression through the AR pathway. hydroxyflutamide 20-32 androgen receptor Homo sapiens 135-137 21829708-6 2011 The AR-regulated expression profiles reflected the AR modifications of respective therapy-resistant sublines: AR overexpression resulted in stronger and broader transcriptional response to R1881 stimulation, AR down-regulation correlated with deficient response of AR-target genes and the T877A mutation resulted in transcriptional response to both R1881 and hydroxyflutamide. hydroxyflutamide 359-375 androgen receptor Homo sapiens 4-6 21829708-6 2011 The AR-regulated expression profiles reflected the AR modifications of respective therapy-resistant sublines: AR overexpression resulted in stronger and broader transcriptional response to R1881 stimulation, AR down-regulation correlated with deficient response of AR-target genes and the T877A mutation resulted in transcriptional response to both R1881 and hydroxyflutamide. hydroxyflutamide 359-375 androgen receptor Homo sapiens 51-53 21829708-6 2011 The AR-regulated expression profiles reflected the AR modifications of respective therapy-resistant sublines: AR overexpression resulted in stronger and broader transcriptional response to R1881 stimulation, AR down-regulation correlated with deficient response of AR-target genes and the T877A mutation resulted in transcriptional response to both R1881 and hydroxyflutamide. hydroxyflutamide 359-375 androgen receptor Homo sapiens 51-53 21829708-6 2011 The AR-regulated expression profiles reflected the AR modifications of respective therapy-resistant sublines: AR overexpression resulted in stronger and broader transcriptional response to R1881 stimulation, AR down-regulation correlated with deficient response of AR-target genes and the T877A mutation resulted in transcriptional response to both R1881 and hydroxyflutamide. hydroxyflutamide 359-375 androgen receptor Homo sapiens 51-53 21829708-6 2011 The AR-regulated expression profiles reflected the AR modifications of respective therapy-resistant sublines: AR overexpression resulted in stronger and broader transcriptional response to R1881 stimulation, AR down-regulation correlated with deficient response of AR-target genes and the T877A mutation resulted in transcriptional response to both R1881 and hydroxyflutamide. hydroxyflutamide 359-375 androgen receptor Homo sapiens 51-53 22496481-2 2012 Current AR antagonists, such as bicalutamide and hydroxyflutamide, have a low affinity for the AR and as a result block AR signaling insufficiently. hydroxyflutamide 49-65 androgen receptor Homo sapiens 8-10 22496481-2 2012 Current AR antagonists, such as bicalutamide and hydroxyflutamide, have a low affinity for the AR and as a result block AR signaling insufficiently. hydroxyflutamide 49-65 androgen receptor Homo sapiens 95-97 22496481-2 2012 Current AR antagonists, such as bicalutamide and hydroxyflutamide, have a low affinity for the AR and as a result block AR signaling insufficiently. hydroxyflutamide 49-65 androgen receptor Homo sapiens 95-97 22496481-10 2012 The activity of two mutant receptors (AR T877A and AR W741C) was shown to be reduced in presence of MEL-3, providing evidence that MEL-3 can potentially be a follow-up treatment for bicalutamide- and hydroxyflutamide-resistant patients. hydroxyflutamide 200-216 androgen receptor Homo sapiens 38-40 21748440-0 2011 Androgen receptor coregulators NOCR1, TIF2, and ARA70 may account for the hydroxyflutamide insensitivity of prostate cancer cells. hydroxyflutamide 74-90 androgen receptor Homo sapiens 0-17 21748440-4 2011 MATERIAL AND METHODS: Prostate cancer cells were continuously treated with competitive androgen receptor inhibitor hydroxyflutamide for 1.5 years, which yielded an flutamide-insensitive LNCaP subline, LNCaP-flu, as confirmed by MTT assays, flow cytometry, and electron microscopy. hydroxyflutamide 115-131 androgen receptor Homo sapiens 87-104 21796530-3 2011 The natural ligand of the AR, dihydrotestosterone (DHT), induces a transcriptionally active conformation of the AR while the steroidal antiandrogen cyproterone acetate (CPA) and the nonsteroidal compounds hydroxyflutamide (OHF), bicalutamide (Cas), and atraric acid (AA) prevent acquisition of a transcriptionally active conformation. hydroxyflutamide 205-221 androgen receptor Homo sapiens 26-28 21796530-3 2011 The natural ligand of the AR, dihydrotestosterone (DHT), induces a transcriptionally active conformation of the AR while the steroidal antiandrogen cyproterone acetate (CPA) and the nonsteroidal compounds hydroxyflutamide (OHF), bicalutamide (Cas), and atraric acid (AA) prevent acquisition of a transcriptionally active conformation. hydroxyflutamide 205-221 androgen receptor Homo sapiens 112-114 19787772-2 2010 However, the T877A mutated AR is paradoxically activated by hydroxyflutamide, an active form of flutamide. hydroxyflutamide 60-76 androgen receptor Homo sapiens 27-29 18571420-3 2008 Among the compounds obtained, N-[4-[(benzyl)(4-nitrophenyl)amino]-1-methylpyrrole-2-carbonyl]pyrrolidine (22) is as potent an AR antagonist as the typical anilide-type AR antagonists hydroxyflutamide and bicalutamide. hydroxyflutamide 183-199 androgen receptor Homo sapiens 126-128 18596614-3 2008 This effect was prevented by the androgen receptor antagonist hydroxyflutamide. hydroxyflutamide 62-78 androgen receptor Homo sapiens 33-50 18548383-3 2008 Progestin binding was competed by the progesterone receptor agonists progesterone and levonorgestrel, by the antagonist mifepristone, and also by the androgen dihydrotestosterone, whereas the androgen receptor antagonist hydroxyflutamide was a weak competitor. hydroxyflutamide 221-237 androgen receptor Homo sapiens 192-209 17541168-4 2007 We found that a potent androgen, 5alpha-dihydrotestosterone (DHT) inhibits IL-1alpha mRNA expression induced by TNFalpha and the DHT effect was inhibited by an androgen receptor antagonist, hydroxyflutamide (OHF). hydroxyflutamide 190-206 androgen receptor Homo sapiens 160-177 17656415-5 2007 Dihydrotestosterone (DHT), in a dose-dependent manner, leads to the rapid phosphorylation of the AR on tyrosine, serine and threonine residues and this effect was reduced by the AR antagonist hydroxyflutamide (OH-Flut). hydroxyflutamide 192-208 androgen receptor Homo sapiens 97-99 17656415-5 2007 Dihydrotestosterone (DHT), in a dose-dependent manner, leads to the rapid phosphorylation of the AR on tyrosine, serine and threonine residues and this effect was reduced by the AR antagonist hydroxyflutamide (OH-Flut). hydroxyflutamide 192-208 androgen receptor Homo sapiens 178-180 17553795-9 2007 GAPDH enhanced the transcriptional activity of AR(T875A) activated by an antagonist such as hydroxyflutamide or cyproterone acetate. hydroxyflutamide 92-108 androgen receptor Homo sapiens 47-49 17587566-11 2007 Treatment with the AR antagonist hydroxyflutamide results in nuclear translocation of the AR, but not the coactivator PRMT2. hydroxyflutamide 33-49 androgen receptor Homo sapiens 19-21 17587566-11 2007 Treatment with the AR antagonist hydroxyflutamide results in nuclear translocation of the AR, but not the coactivator PRMT2. hydroxyflutamide 33-49 androgen receptor Homo sapiens 90-92 17223690-6 2007 Although usually an antagonist, hydroxyflutamide was more potent in the recruitment of D11FxxLF or an SRC3-1 LXXLL motif to AR T877A LBD than AR LBD. hydroxyflutamide 32-48 androgen receptor Homo sapiens 124-126 17636177-6 2007 Furthermore, hydroxyflutamide (FLU),a specific AR antagonist, was also supplemented to cultured media. hydroxyflutamide 13-29 androgen receptor Homo sapiens 47-49 15219414-8 2004 Furthermore, the AR antagonists 2-hydroxyflutamide and DDE also repressed GR transactivation in an AR-dependent manner. hydroxyflutamide 32-50 androgen receptor Homo sapiens 17-19 17073766-5 2006 In the presence of the anti-androgens bicalutamide and hydroxyflutamide, a significant proportion of the AR is translocated to the nucleus but remains inactive. hydroxyflutamide 55-71 androgen receptor Homo sapiens 105-107 16129672-7 2005 We have shown that changes induced to the positions of Trp-741, Thr-877, and Met-895 allow for ligand accommodation within the AR binding pocket and that a water-mediated hydrogen bond to the backbone oxygen of Leu-873 and the ketone of hydroxyflutamide is present when bound to the T877A AR variant. hydroxyflutamide 237-253 androgen receptor Homo sapiens 127-129 15538745-5 2005 An androgen receptor (AR) antagonist, Casodex antagonized the DHT effect, whereas an AR agonist (due to the mutant AR in LNCaP cells) hydroxyflutamide did not. hydroxyflutamide 134-150 androgen receptor Homo sapiens 85-87 15538745-5 2005 An androgen receptor (AR) antagonist, Casodex antagonized the DHT effect, whereas an AR agonist (due to the mutant AR in LNCaP cells) hydroxyflutamide did not. hydroxyflutamide 134-150 androgen receptor Homo sapiens 85-87 14973257-9 2004 Addition of an AR antagonist, hydroxyflutamide, generally reversed the proliferative responses invoked by DHT but not the steroidogenic responses. hydroxyflutamide 30-46 androgen receptor Homo sapiens 15-17 16054371-3 2005 Today, treatment of prostate cancer is done by inhibition of AR using antiandrogens such as flutamide (pro-drug of hydroxyflutamide), nilutamide, and bicalutamide. hydroxyflutamide 115-131 androgen receptor Homo sapiens 61-63 16129672-4 2005 Recently, our laboratory discovered selective androgen receptor modulators, which structurally resemble the nonsteroidal AR antagonists bicalutamide and hydroxyflutamide but act as agonists for the androgen receptor in a tissue-selective manner. hydroxyflutamide 153-169 androgen receptor Homo sapiens 46-63 16129672-4 2005 Recently, our laboratory discovered selective androgen receptor modulators, which structurally resemble the nonsteroidal AR antagonists bicalutamide and hydroxyflutamide but act as agonists for the androgen receptor in a tissue-selective manner. hydroxyflutamide 153-169 androgen receptor Homo sapiens 121-123 15900601-11 2005 PC346Flu2 carries the well-known T877A AR mutation, causing the receptor to become activated by diverse nonandrogenic ligands including hydroxyflutamide. hydroxyflutamide 136-152 androgen receptor Homo sapiens 39-41 15994236-7 2005 An antagonist ligand, hydroxyflutamide, blocked the NTD-LBD association within AR. hydroxyflutamide 22-38 androgen receptor Homo sapiens 79-81 15219414-8 2004 Furthermore, the AR antagonists 2-hydroxyflutamide and DDE also repressed GR transactivation in an AR-dependent manner. hydroxyflutamide 32-50 androgen receptor Homo sapiens 99-101 12672951-6 2003 Moreover, ADEK could block an adrenal androgen androstenediol-induced AR transactivation that hydroxyflutamide and bicalutamide failed to block. hydroxyflutamide 94-110 androgen receptor Homo sapiens 70-72 14593076-9 2004 We found that mifepristone could induce a strong interaction between AR and corepressors nuclear receptor corepressor and silencing mediator for retinoid and thyroid hormone receptors in both transactivation and two-hybrid assays to a greater degree than hydroxyflutamide, cyproterone acetate, and bicalutamide. hydroxyflutamide 255-271 androgen receptor Homo sapiens 69-71 12573819-5 2002 In contrast to the wild-type AR, the mutant AR conformation induced by cyproterone acetate (CPA) and hydroxyflutamide (OHF) is comparable to that induced by androgens. hydroxyflutamide 101-117 androgen receptor Homo sapiens 44-46 12573820-6 2002 Conversely, both enhanced the magnitude of the AR response in the presence of low levels of androgen (10(-11)-10(-9) M) and this response, increased by twofold, was inhibited by hydroxyflutamide. hydroxyflutamide 178-194 androgen receptor Homo sapiens 47-49 11356108-7 2001 In addition to testosterone, the binding modes of several hydroxyflutamide-like nonsteroidal ligands for the androgen receptor are investigated using flexible docking with FlexX followed by refinement of the initial complexes with molecular dynamics simulations. hydroxyflutamide 58-74 androgen receptor Homo sapiens 109-126 12114440-3 2002 The present study was designed to investigate the regulation of AR expression and function by OSM, as well as the efficacy of the nonsteroidal antiandrogens hydroxyflutamide and bicalutamide in the inhibition of AR-mediated signal transduction. hydroxyflutamide 157-173 androgen receptor Homo sapiens 212-214 12114440-10 2002 In the presence of OSM, hydroxyflutamide behaved as an AR agonist. hydroxyflutamide 24-40 androgen receptor Homo sapiens 55-57 11916967-6 2002 Agonist-bound AR was required because the AR antagonists casodex and hydroxyflutamide failed to translocate beta-catenin. hydroxyflutamide 69-85 androgen receptor Homo sapiens 14-16 12153751-6 2002 Inhibition of OPG mRNA levels and protein production by 5alpha-DHT was completely abrogated by the AR antagonist, hydroxyflutamide (OHF), indicating that these effects are directly mediated by the AR. hydroxyflutamide 114-130 androgen receptor Homo sapiens 99-101 12153751-6 2002 Inhibition of OPG mRNA levels and protein production by 5alpha-DHT was completely abrogated by the AR antagonist, hydroxyflutamide (OHF), indicating that these effects are directly mediated by the AR. hydroxyflutamide 114-130 androgen receptor Homo sapiens 197-199 12123801-3 2002 By contrast, AR complexed to the antiandrogens hydroxyflutamide and bicalutamide fails to influence nuclear distribution of GRIP1. hydroxyflutamide 47-63 androgen receptor Homo sapiens 13-15 11501969-6 2001 Characterization of the functional relationship between the AR and these coregulators indicated that ARA70 and ARA55 could enhance the androgenic effects of 17beta-estradiol (E2) and hydroxyflutamide (HF), an antiandrogen commonly used in the treatment of prostate cancer. hydroxyflutamide 183-199 androgen receptor Homo sapiens 60-62 11501969-6 2001 Characterization of the functional relationship between the AR and these coregulators indicated that ARA70 and ARA55 could enhance the androgenic effects of 17beta-estradiol (E2) and hydroxyflutamide (HF), an antiandrogen commonly used in the treatment of prostate cancer. hydroxyflutamide 201-203 androgen receptor Homo sapiens 60-62 10855693-0 2000 Isolation and characterization of the androgen receptor mutants with divergent transcriptional activity in response to hydroxyflutamide. hydroxyflutamide 119-135 androgen receptor Homo sapiens 38-55 12083956-6 2001 Although functional characterization of only some mutant AR detected in prostate cancer tissue has been performed, data available suggest that they are activated by dihydrotestosterone, its precursors and metabolites, synthetic androgens, estrogenic and progestagenic steroids and hydroxyflutamide. hydroxyflutamide 281-297 androgen receptor Homo sapiens 57-59 10706107-8 2000 The AR antagonist hydroxyflutamide did not reverse the effect of DHT on SKOV-3 cells but by itself down-regulated TbetaR-II mRNA. hydroxyflutamide 18-34 androgen receptor Homo sapiens 4-6 10706107-9 2000 This apparent androgen-mimetic action of hydroxyflutamide and the ability of SKOV-3 and HEY cells to respond to DHT may be due to their expression of AR-associating protein 70, an AR co-activator reported to amplify AR transactivation and to result in agonist activity of AR antagonists. hydroxyflutamide 41-57 androgen receptor Homo sapiens 150-152 10706107-9 2000 This apparent androgen-mimetic action of hydroxyflutamide and the ability of SKOV-3 and HEY cells to respond to DHT may be due to their expression of AR-associating protein 70, an AR co-activator reported to amplify AR transactivation and to result in agonist activity of AR antagonists. hydroxyflutamide 41-57 androgen receptor Homo sapiens 180-182 10706107-9 2000 This apparent androgen-mimetic action of hydroxyflutamide and the ability of SKOV-3 and HEY cells to respond to DHT may be due to their expression of AR-associating protein 70, an AR co-activator reported to amplify AR transactivation and to result in agonist activity of AR antagonists. hydroxyflutamide 41-57 androgen receptor Homo sapiens 180-182 10855693-1 2000 A yeast genetic screening was developed to isolate androgen receptor (AR) mutants with divergent transactivation characteristics in response to hydroxyflutamide (HF), an active metabolite of flutamide used for prostate cancer treatment. hydroxyflutamide 144-160 androgen receptor Homo sapiens 51-68 10645914-9 2000 Lipid-loading studies were performed on male (n=9) macrophages treated with the androgen dihydrotestosterone (DHT) and/or the AR antagonist hydroxyflutamide. hydroxyflutamide 140-156 androgen receptor Homo sapiens 126-128 10597231-6 1999 This action of the androgen receptor differs from its known transcriptional activity since it is rapid and insensitive to androgen antagonists such as hydroxyflutamide or casodex. hydroxyflutamide 151-167 androgen receptor Homo sapiens 19-36 11025427-15 2000 Both androgen and the nonsteroidal androgen receptor antagonist hydroxyflutamide induced a 2- to 4-fold higher activation of androgen receptor in LNCaP-abl than in LNCaP cells. hydroxyflutamide 64-80 androgen receptor Homo sapiens 35-52 11025427-15 2000 Both androgen and the nonsteroidal androgen receptor antagonist hydroxyflutamide induced a 2- to 4-fold higher activation of androgen receptor in LNCaP-abl than in LNCaP cells. hydroxyflutamide 64-80 androgen receptor Homo sapiens 125-142 10334909-7 1999 Significant increases in levels of both mRNA and protein of prostate-specific antigen (PSA), a natural AR target gene, occur following the treatment of LNCaP cells with DHT, beta-estradiol, or hydroxyflutamide. hydroxyflutamide 193-209 androgen receptor Homo sapiens 103-105 10500149-8 1999 Interestingly, these compounds, in combination with hydroxyflutamide, further suppressed the Adiol-induced AR transactivation. hydroxyflutamide 52-68 androgen receptor Homo sapiens 107-109 10496349-12 1999 The non-steroidal AR blocker hydroxyflutamide exerted stimulatory effects on AR activity in both LNCaP and LNCaP-abl cells; however, the induction of reporter gene activity by hydroxyflutamide was 2.4- to 4-fold higher in the LNCaP-abl subline. hydroxyflutamide 29-45 androgen receptor Homo sapiens 18-20 10496349-12 1999 The non-steroidal AR blocker hydroxyflutamide exerted stimulatory effects on AR activity in both LNCaP and LNCaP-abl cells; however, the induction of reporter gene activity by hydroxyflutamide was 2.4- to 4-fold higher in the LNCaP-abl subline. hydroxyflutamide 29-45 androgen receptor Homo sapiens 77-79 10496349-12 1999 The non-steroidal AR blocker hydroxyflutamide exerted stimulatory effects on AR activity in both LNCaP and LNCaP-abl cells; however, the induction of reporter gene activity by hydroxyflutamide was 2.4- to 4-fold higher in the LNCaP-abl subline. hydroxyflutamide 176-192 androgen receptor Homo sapiens 18-20 10402478-8 1999 Competition experiments with DHT and the antiandrogens hydroxyflutamide and casodex confirmed the involvement of the AR in the regulation of GCDFP-15. hydroxyflutamide 55-71 androgen receptor Homo sapiens 117-119 10318905-5 1999 Furthermore, we found this HER2/Neu --> MAP kinase --> AR-ARAs --> PSA pathway could not be blocked completely by hydroxyflutamide, an antiandrogen used in the treatment of prostate cancer. hydroxyflutamide 123-139 androgen receptor Homo sapiens 61-63 10075738-5 1999 Transient transfection assay in prostate cancer DU145 cells further demonstrates that ARA55 can enhance AR transcriptional activity in the presence of 1 nM dihydrotestosterone or its antagonists such as 100 nM 17beta-estradiol or 1 microM hydroxyflutamide. hydroxyflutamide 239-255 androgen receptor Homo sapiens 86-88 10076535-7 1998 Analogous to the antiandrogens, bicalutamide and hydroxyflutamide, binding of estramustine phosphate metabolites to the androgen receptor was observed. hydroxyflutamide 49-65 androgen receptor Homo sapiens 120-137 8643607-3 1996 Using a yeast two-hybrid system, we were able to isolate a ligand-dependent AR-associated protein (ARA70), which functions as an activator to enhance AR transcriptional activity 10-fold in the presence of 10(-10) M dihydrotestosterone or 10(-9) M testosterone, but not 10(-6) M hydroxyflutamide in human prostate cancer DU145 cells. hydroxyflutamide 278-294 androgen receptor Homo sapiens 76-78 9351907-9 1997 In assays performed using this cell line transfected with the cDNA for the androgen receptor, flutamide is a pure antagonist, and 2-hydroxyflutamide, while a more potent androgen receptor (AR) antagonist, activates the AR at higher concentrations. hydroxyflutamide 130-148 androgen receptor Homo sapiens 75-92 9351907-9 1997 In assays performed using this cell line transfected with the cDNA for the androgen receptor, flutamide is a pure antagonist, and 2-hydroxyflutamide, while a more potent androgen receptor (AR) antagonist, activates the AR at higher concentrations. hydroxyflutamide 130-148 androgen receptor Homo sapiens 219-221 9282332-9 1997 Moreover, 5 alpha-DHT-induced ARE-CAT expression was inhibited by the selective androgen receptor antagonist, hydroxyflutamide. hydroxyflutamide 110-126 androgen receptor Homo sapiens 80-97 7748811-5 1995 Co-incubation of cultures with 1 nM DHT and a 100-fold excess of the androgen receptor antagonist, hydroxyflutamide, resulted in reversal of both inhibitory and stimulatory effects of DHT on T47-D, MCF-7 and MDA-MB-453 cell proliferation, indicating that DHT action is mediated by the AR in these lines. hydroxyflutamide 99-115 androgen receptor Homo sapiens 69-86 7650017-0 1995 Androgen receptor antagonist versus agonist activities of the fungicide vinclozolin relative to hydroxyflutamide. hydroxyflutamide 96-112 androgen receptor Homo sapiens 0-17 7650017-6 1995 In the absence of dihydrotestosterone, concentrations of 10 microM M2 or hydroxyflutamide promote AR binding to androgen response element DNA and activation of transcription. hydroxyflutamide 73-89 androgen receptor Homo sapiens 98-100 7650017-7 1995 Agonist activities of M2 and hydroxyflutamide occur at 10-fold lower concentrations with the mutant AR (Thr877 to Ala) endogenous to LNCaP human prostate cancer cells. hydroxyflutamide 29-45 androgen receptor Homo sapiens 100-102 8594318-8 1996 In a separate series of experiments, HEL cells were incubated with the androgen receptor antagonist hydroxyflutamide (2.5mM). hydroxyflutamide 100-116 androgen receptor Homo sapiens 71-88 7748811-5 1995 Co-incubation of cultures with 1 nM DHT and a 100-fold excess of the androgen receptor antagonist, hydroxyflutamide, resulted in reversal of both inhibitory and stimulatory effects of DHT on T47-D, MCF-7 and MDA-MB-453 cell proliferation, indicating that DHT action is mediated by the AR in these lines. hydroxyflutamide 99-115 androgen receptor Homo sapiens 285-287 8274406-5 1993 The mutated androgen receptor was fully activated by R1881, cyproterone acetate and hydroxyflutamide, but not by ICI 176,334. hydroxyflutamide 84-100 androgen receptor Homo sapiens 12-29 8043498-9 1994 Hydroxyflutamide could only inhibit tight nuclear binding of the wild-type AR. hydroxyflutamide 0-16 androgen receptor Homo sapiens 75-77 1540595-3 1992 Estrogens, progestagens, and some anti-androgens (e.g., cyproterone acetate, hydroxyflutamide, nilutamide) stimulate LNCaP cell growth rate through the AR. hydroxyflutamide 77-93 androgen receptor Homo sapiens 152-154 1616884-1 1992 The purpose of our study was to evaluate the effects of 5 alpha-dihydrotestosterone (DHT) and hydroxyflutamide (HF), alone or in combination, on androgen receptor (AR) dynamics and on cellular growth in cultured breast cancer cells (EVSA-T). hydroxyflutamide 94-110 androgen receptor Homo sapiens 145-162 1616884-1 1992 The purpose of our study was to evaluate the effects of 5 alpha-dihydrotestosterone (DHT) and hydroxyflutamide (HF), alone or in combination, on androgen receptor (AR) dynamics and on cellular growth in cultured breast cancer cells (EVSA-T). hydroxyflutamide 94-110 androgen receptor Homo sapiens 164-166 1668832-5 1991 In PC-3 cells expressing LNCaP AR, however, CAT activity was also induced by progestins and the antiandrogen hydroxyflutamide, which had little activity in cells expressing normal AR. hydroxyflutamide 109-125 androgen receptor Homo sapiens 31-33 1668832-5 1991 In PC-3 cells expressing LNCaP AR, however, CAT activity was also induced by progestins and the antiandrogen hydroxyflutamide, which had little activity in cells expressing normal AR. hydroxyflutamide 109-125 androgen receptor Homo sapiens 180-182 1668832-6 1991 Steroid-binding competition assays using in vitro synthesized ARs showed that LNCaP AR had a higher affinity than normal AR for progestins, 17 beta-estradiol, and hydroxyflutamide. hydroxyflutamide 163-179 androgen receptor Homo sapiens 62-64 1668832-6 1991 Steroid-binding competition assays using in vitro synthesized ARs showed that LNCaP AR had a higher affinity than normal AR for progestins, 17 beta-estradiol, and hydroxyflutamide. hydroxyflutamide 163-179 androgen receptor Homo sapiens 84-86 2159274-4 1990 2-Hydroxy-4"-nitro-3"-trifluoromethyldiphenylamine (13), which shows a relative binding affinity (RBA) to the androgen receptor (AR) of 6.5% of that of testosterone, exerts a higher affinity than hydroxyflutamide (RBA = 4.5). hydroxyflutamide 196-212 androgen receptor Homo sapiens 110-127 2159274-4 1990 2-Hydroxy-4"-nitro-3"-trifluoromethyldiphenylamine (13), which shows a relative binding affinity (RBA) to the androgen receptor (AR) of 6.5% of that of testosterone, exerts a higher affinity than hydroxyflutamide (RBA = 4.5). hydroxyflutamide 196-212 androgen receptor Homo sapiens 129-131