PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 6183286-8 1983 In contrast, [3H]methyltrienolone (3H-labeled 17 beta-hydroxy-17 alpha-methyl-estra-4,9,11-trien-3-one) binds to both androgen and progestin receptors, and consequently, the binding of this ligand to the androgen receptor was assessed in the presence of a 500-fold excess of triamcinolone acetonide. Metribolone 13-33 androgen receptor Homo sapiens 204-221 3262343-5 1988 Cells from subjects with mutant androgen receptors generally lack the 56 kD protein and labelling with methyltrienolone fails, but the protein is not the androgen receptor itself. Metribolone 103-119 androgen receptor Homo sapiens 32-49 2457134-2 1988 Two most frequently used ligands are [3H]dihydrotestosterone [( 3H]DHT) and [3H]methyltrienolone [( 3H]R1881), which in addition to binding to AR also bind to sex hormone binding globulin (SHBG; Kd = 1.5 nM) and progesterone receptors (PgR; Human Kd = 1 nM, rat Kd = 6 nM) respectively. Metribolone 76-96 androgen receptor Homo sapiens 143-145 3500883-1 1987 The reproducible photolabeling of the androgen receptor from human skin fibroblasts, using [3H]methyltrienolone (R-1881) as ligand is described. Metribolone 91-111 androgen receptor Homo sapiens 38-55 3500883-1 1987 The reproducible photolabeling of the androgen receptor from human skin fibroblasts, using [3H]methyltrienolone (R-1881) as ligand is described. Metribolone 113-119 androgen receptor Homo sapiens 38-55 3605226-4 1987 The mutant androgen receptor has a normal maximum binding capacity (Bmax), but an increased apparent equilibrium dissociation constant (Kd) with 5 alpha-dihydrotestosterone (DHT) and 2 synthetic androgens, methyltrienolone (MT) and mibolerone (MB). Metribolone 206-222 androgen receptor Homo sapiens 11-28 3297710-2 1987 [3H]methyltrienolone, a synthetic androgen, was used for concurrent determination of the androgen receptor (AR)-binding activity. Metribolone 0-20 androgen receptor Homo sapiens 89-106 3297710-2 1987 [3H]methyltrienolone, a synthetic androgen, was used for concurrent determination of the androgen receptor (AR)-binding activity. Metribolone 0-20 androgen receptor Homo sapiens 108-110 3486876-0 1986 Studies of molecular species of the human androgen receptor (AR): comparison of the physicochemical properties of the [3H]methyltrienolone-AR complex formed in cytosol to the complex produced in intact genital skin fibroblasts. Metribolone 118-138 androgen receptor Homo sapiens 42-59 3486876-0 1986 Studies of molecular species of the human androgen receptor (AR): comparison of the physicochemical properties of the [3H]methyltrienolone-AR complex formed in cytosol to the complex produced in intact genital skin fibroblasts. Metribolone 118-138 androgen receptor Homo sapiens 61-63 3486876-0 1986 Studies of molecular species of the human androgen receptor (AR): comparison of the physicochemical properties of the [3H]methyltrienolone-AR complex formed in cytosol to the complex produced in intact genital skin fibroblasts. Metribolone 118-138 androgen receptor Homo sapiens 139-141 3872888-7 1985 With DHT, the androgen receptor in her genital skin fibroblasts has a normal binding capacity (maximum binding capacity = 25 fmol/mg protein), but an increased rate constant of dissociation (k = 11.6 X 10(-3) min-1; normal, 6 +/- 1.2 (+/- SD)), and a decreased apparent equilibrium binding affinity (Kd = 0.6 nM; normal, 0.22 +/- 0.09) that is evident in the results of 2-h assays but not of those lasting 0.5 h. With the synthetic androgen, methyltrienolone, all three binding properties of the receptor are normal, and her receptor activity up-regulates normally. Metribolone 442-458 androgen receptor Homo sapiens 14-31 6333553-3 1984 Initial experiments indicated that photoaffinity labelling of the androgen receptor protein may be readily achieved and with extensive covalent attachment of [3H]methyltrienolone. Metribolone 158-178 androgen receptor Homo sapiens 66-83 6333553-6 1984 Our findings raise doubts concerning the efficiency and usefulness of [3H]methyltrienolone as a photoaffinity reagent for androgen receptor proteins. Metribolone 70-90 androgen receptor Homo sapiens 122-139 6580856-1 1983 Androgen receptor binding of radiolabelled methyltrienolone (3H-R1881) was determined in cultured genital skin fibroblasts from 17 normal male controls and from 65 males with genital abnormalities. Metribolone 43-59 androgen receptor Homo sapiens 0-17 6601205-5 1983 Prolonged incubation with methyltrienolone (R1881), a nonmetabolizable synthetic androgen, causes a greater, more persistent increment of androgen receptor activity than does equimolar DHT. Metribolone 26-42 androgen receptor Homo sapiens 138-155 2796102-3 1989 Androgen receptor was measured using methyltrienolone (R1881) as the ligand according to the assay technique of Eil et al. Metribolone 37-53 androgen receptor Homo sapiens 0-17 2705470-6 1989 The androgen receptor in his genital skin fibroblasts has a distinctively mutant phenotype: it has a low affinity (increased apparent equilibrium dissociation constant, Kd) for 5 alpha-dihydrotestosterone and two synthetic androgens, mibolerone (MB) and methyltrienolone (MT), and its binding capacity (Bmax) is normal for the other two ligands, but questionably low for MT. Metribolone 254-270 androgen receptor Homo sapiens 4-21 2901218-7 1988 Androgen receptor levels and binding affinity were normal for the androgen-specific ligands dihydrotestosterone and metribolone in both skin fibroblasts and testicular cells. Metribolone 116-127 androgen receptor Homo sapiens 0-17 6332533-0 1984 Familial external genital ambiguity due to a transformation defect of androgen-receptor complexes that is expressed with 5 alpha-dihydrotestosterone and the synthetic androgen methyltrienolone. Metribolone 176-192 androgen receptor Homo sapiens 70-87 6183286-8 1983 In contrast, [3H]methyltrienolone (3H-labeled 17 beta-hydroxy-17 alpha-methyl-estra-4,9,11-trien-3-one) binds to both androgen and progestin receptors, and consequently, the binding of this ligand to the androgen receptor was assessed in the presence of a 500-fold excess of triamcinolone acetonide. Metribolone 46-102 androgen receptor Homo sapiens 204-221 22877652-4 2012 Methyltrienolone (R1881), a synthetic AR agonist, represses GnRH expression through multiple sites in the proximal promoter. Metribolone 0-16 androgen receptor Homo sapiens 38-40 436741-0 1979 Androgen receptor assay with [3H]methyltrienolone (R1881) in the presence of progesterone receptors. Metribolone 29-49 androgen receptor Homo sapiens 0-17 442131-1 1979 A microassay utilizing R 1881 (methyltrienolone) has been developed for the measurement of androgen receptor sites in the cytosol and nuclear extract of human prostatic tissue. Metribolone 31-47 androgen receptor Homo sapiens 91-108 32509382-8 2020 In TNBC/HER2+ cell lines, CPD and EDD protein expression were upregulated by PRL or synthetic androgen methyltrienolone (R1881) at 3-6 h. PRL/R1881-induced CPD in TNBC and HER2+ cells increased intracellular NO production, which was abolished by PRLR antagonist 1-9-G129R-hPRL and AR antagonist flutamide. Metribolone 103-119 androgen receptor Homo sapiens 282-284 29749659-4 2018 Here, we assayed the role for a synthetic AR ligand methyltrienolone (R1881) in expressions of AKTs and AR. Metribolone 52-68 androgen receptor Homo sapiens 42-44 29749659-4 2018 Here, we assayed the role for a synthetic AR ligand methyltrienolone (R1881) in expressions of AKTs and AR. Metribolone 52-68 androgen receptor Homo sapiens 104-106 29749659-4 2018 Here, we assayed the role for a synthetic AR ligand methyltrienolone (R1881) in expressions of AKTs and AR. Metribolone 70-75 androgen receptor Homo sapiens 42-44 29749659-4 2018 Here, we assayed the role for a synthetic AR ligand methyltrienolone (R1881) in expressions of AKTs and AR. Metribolone 70-75 androgen receptor Homo sapiens 104-106 11118046-8 2000 Regardless of AR receptor type, all of our novel compounds were effective at preventing binding of the synthetic androgen methyl-trienolone[17alpha-methyl-(3H)-R1881 to both the LNCaP AR and the wildtype AR. Metribolone 122-139 androgen receptor Homo sapiens 184-186 23344235-3 2012 In LNCaP prostate cancer cells, gymnotic silencing of the AR by a 2"F-ANA phosphorothioate gapmer oligo led to downstream silencing of cellular prostate-specific antigen (PSA) expression even in the presence of the androgenic steroid R1881 (metribolone), which stabilizes cytoplasmic levels of the AR. Metribolone 241-252 androgen receptor Homo sapiens 58-60 17595765-10 2007 Moreover, the relative binding affinity of DBM to AR was lower than that of the synthetic androgen R1881 (methyltrienolone) suggesting that DBM must suppress AR expression independent of an AR-DBM bound interaction. Metribolone 106-122 androgen receptor Homo sapiens 158-160 17595765-10 2007 Moreover, the relative binding affinity of DBM to AR was lower than that of the synthetic androgen R1881 (methyltrienolone) suggesting that DBM must suppress AR expression independent of an AR-DBM bound interaction. Metribolone 106-122 androgen receptor Homo sapiens 158-160 14751668-4 2004 In order to be able to screen for compounds with affinity for the androgen receptor (AR), we developed an AR binding assay using a recombinant AR as receptor source and the synthetic androgen methyltrienolone (R 1881) as ligand. Metribolone 192-208 androgen receptor Homo sapiens 66-83 14751668-4 2004 In order to be able to screen for compounds with affinity for the androgen receptor (AR), we developed an AR binding assay using a recombinant AR as receptor source and the synthetic androgen methyltrienolone (R 1881) as ligand. Metribolone 192-208 androgen receptor Homo sapiens 85-87 14613328-9 2003 This relative binding affinity is encouraging in light of the cocrystal structure of human androgen receptor ligand binding domain bound to the steroid Metribolone which predicts very limited space for a tether connecting the antiandrogen on the inside to the cytotoxin on the outside. Metribolone 152-163 androgen receptor Homo sapiens 91-108 11223178-4 2001 In transactivation assays using a PC-3 cell line stably transfected with the AR (PC-3/AR), the -1253 element placed as two or four copies upstream of the TK minimal promoter yielded a strong induction of luciferase reporter gene activity in the presence of the androgen methyltrienolone (R1881). Metribolone 270-286 androgen receptor Homo sapiens 77-79 11223178-4 2001 In transactivation assays using a PC-3 cell line stably transfected with the AR (PC-3/AR), the -1253 element placed as two or four copies upstream of the TK minimal promoter yielded a strong induction of luciferase reporter gene activity in the presence of the androgen methyltrienolone (R1881). Metribolone 270-286 androgen receptor Homo sapiens 81-88 19590256-3 2009 Binding affinities to the human androgen receptor were characterized by Ki values of 3.8 nM for CMA, 83 nM for 3alpha-OH-CMA, 20 nM for 3beta-OH-CMA and 2.9 nM for the reference androgen methyltrienolone. Metribolone 187-203 androgen receptor Homo sapiens 32-49 17803706-7 2008 Stimulation of these cells with the synthetic androgen methyltrienolone (R1881) caused AR translocation in the nucleus, suggesting its activation. Metribolone 55-71 androgen receptor Homo sapiens 87-89 9788616-6 1998 We show that IL-6 up-regulates AR activity in a ligand-independent manner, as well as synergistically, with very low doses of the synthetic androgen methyltrienolone (5-10 pM). Metribolone 149-165 androgen receptor Homo sapiens 31-33 10840043-2 2000 The crystal structures of the human androgen receptor (hAR) and human progesterone receptor ligand-binding domains in complex with the same ligand metribolone (R1881) have been determined. Metribolone 147-158 androgen receptor Homo sapiens 36-53 8823308-4 1996 The rate of dissociation of [3H]methyltrienolone from the EK2 mutant (half-time [t1/2] = 1.7 +/- 0.08 SE h) was increased compared with wild type AR (t1/2 = 2.4 +/- 0.11 h). Metribolone 28-48 androgen receptor Homo sapiens 146-148 9033395-3 1997 In the presence of androgen [methyltrienolone (R1881) or dihydrotestosterone (DHT)] a transcriptionally active complex was formed, reflecting an association between the AR(LBD) and the AR(TAD). Metribolone 29-45 androgen receptor Homo sapiens 169-171 9039340-10 1996 Transcriptional activation studies of two mutant ARs revealed that an approximately tenfold higher androgen concentration (methyltrienolone) is necessary to achieve maximal response as compared to the wild type AR. Metribolone 123-139 androgen receptor Homo sapiens 49-51 7852512-2 1995 Binding of the synthetic androgen methyltrienolone (R1881) was measured in a monolayer assay, and Scatchard analysis was performed to determine the total number of binding sites and the apparent binding affinity (Kd) of the AR for androgen. Metribolone 34-50 androgen receptor Homo sapiens 224-226 7590636-3 1995 When 25.8 nM 5-alpha-dihydrotestosterone (DHT) or methyltrienolone was added to the medium, some AR were translocated into the nucleus in 13 experiments with 8 strains of normal fibroblasts; of 8 strains of patients with PAIS 3 failed to translocate to a detectable extent in the presence of androgen in the medium and none of the 6 strains from patients with CAIS translocated. Metribolone 50-66 androgen receptor Homo sapiens 97-99 8471057-4 1993 Partial proteolysis of androgen receptor protein metabolically labelled with [32P]P(i) and photolabelled with [3H]R1881 (methyltrienolone) revealed that phosphorylation occurs mainly in the N-terminal trans-activation domain, whereas no phosphorylation was detected in the steroid- and DNA-binding domains. Metribolone 121-137 androgen receptor Homo sapiens 23-40 35524041-3 2022 The human AR coordinate in this study is derived from human AR in complex with the ligand metribolone (R18) (PBD ID: 1E3G) template using (MODELER version. Metribolone 90-101 androgen receptor Homo sapiens 10-12 35524041-3 2022 The human AR coordinate in this study is derived from human AR in complex with the ligand metribolone (R18) (PBD ID: 1E3G) template using (MODELER version. Metribolone 90-101 androgen receptor Homo sapiens 60-62