Metribolone

A synthetic non-aromatizable androgen and anabolic steroid. It binds strongly to the androgen receptor and has therefore also been used as an affinity label for this receptor in the prostate and in prostatic tumors.

Also Known As:

Networked: 104 relevant articles (0 outcomes, 10 trials/studies)

Bio-Agent Context: Research Results

Experts

1.	Trapman, Jan: 2 articles (01/2011 - 11/2005)
2.	Rodriguez, Ronald: 2 articles (03/2010 - 05/2002)
3.	Horie-Inoue, Kuniko: 2 articles (01/2009 - 12/2004)
4.	Inoue, Satoshi: 2 articles (01/2009 - 12/2004)
5.	Rennie, Paul S: 2 articles (11/2007 - 11/2006)
6.	Onate, Sergio A: 2 articles (05/2006 - 09/2003)
7.	Gao, Allen C: 2 articles (05/2006 - 09/2003)
8.	Too, Catherine K L: 1 article (03/2014)
9.	Thomas, Lynn N: 1 article (03/2014)
10.	Koirala, Samir: 1 article (03/2014)

Related Diseases

1.	Neoplasms (Cancer) 11/01/1978 - "In this study biopsies from 16 cancer patients were taken before therapy was given, and the specimens were analyzed with regard to content of specific methyltrienolone-binding sites. " 01/01/2014 - "Principal component analysis with linear discriminant analysis of the Raman spectra was able to differentiate between cancer cells that were treated with MPA, R1881, and untreated." 11/01/2005 - "PC346Flu1 proliferation was inhibited in vitro by R1881 at 0.1 nM concentration, consistent with a slower tumor growth rate in intact males than in castrated mice. " 04/01/2001 - "AR from all of the tumors and cell lines bound [3H]R1881 with similar high affinity (mean Kd, 0.12 nM). " 01/01/1995 - "The inhibitory effect of R 1881 on a PgR-positive/AR-negative tumor suggested that R 1881 action was partially PgR-mediated. "
2.	Prostatic Neoplasms (Prostate Cancer) 05/14/2009 - "Although several studies have used microarrays to identify AR-regulated genes in prostate cancer cell lines and in prostate tumours, we present here the results of gene expression microarray profiling of the androgen-responsive LNCaP prostate-cancer cell line treated with R1881 for the identification of androgen-regulated genes. " 05/01/2002 - "In vitro studies showed that our viral constructs preferentially kill PSA-positive prostate cancer cells in the presence of exogenous androgen (R1881). " 01/01/2011 - "Androgen regulation of TMPRSS2 is measured in commonly used LNCaP prostate cancer cells grown with and without the synthetic androgen R1881. " 12/01/2007 - "To investigate possible effects of androgen on SOCS-3 protein expression, two prostate cancer cell lines (PC3-AR and LAPC4) were treated with different concentrations of R1881. " 01/01/2006 - "We present the utility of massively parallel sequencing by synthesis for profiling the transcriptome of a human prostate cancer cell-line, LNCaP, that has been treated with the synthetic androgen, R1881. "
3.	Breast Neoplasms (Breast Cancer) 03/01/2014 - "In summary, PRL and R1881, acting through Stat5 and AR, act cooperatively to stimulate CPD gene transcription in breast cancer cells. " 10/01/1988 - "Specific [3H]R1881 binding was found in four different gubernaculum fibroblast cultures (9,000-42,000 sites/cell) and MCF-7 human breast cancer cells (34,000 sites/cell) which were used as controls. " 12/01/1970 - "Antitumor efficacy and toxicity of methyltrienolone (NSC-92858) in advanced breast cancer." 03/01/2014 - "This study showed that synthetic androgen R1881 and PRL elevated CPD mRNA/protein levels in human MCF-7 and T47D breast cancer cells in a time-/dose-dependent manner. " 03/01/2014 - "Prolactin/Stat5 and androgen R1881 coactivate carboxypeptidase-D gene in breast cancer cells."
4.	Adenocarcinoma 12/01/1985 - "This paper describes the dose-response inhibitory effects of a synthetic androgen, methyltrienolone, on the growth of a grade II endometrial adenocarcinoma in vitro. " 01/01/1986 - "The synthetic androgen 17 beta-hydroxy-17 alpha-[3H]methyl-4,9,11-estratrien-3-one (R1881) has been used as photoaffinity label to characterize androgen receptors in rat prostate, in a human transplantable prostatic adenocarcinoma (PC-82) and in calf uterus. " 01/11/2002 - "We show that androgens (dihydrotestosterone and R1881) down-regulate TGF-beta1-induced expression of TGF-beta1, c-Fos, and Egr-1 in the human prostate adenocarcinoma cell line, LNCaP. " 09/10/1999 - "In the present study we explored whether androgens (R1881), retinoids (all-trans- and 9-cis-retinoic acid: atRA and 9cRA), deltanoids (1alpha,25-dihydroxycholecalciferol: VD3) and thyroid hormone (triiodothyronine: T3) influence the production of IGFBPs by LNCaP prostatic adenocarcinoma cells and whether the observed changes affect tumor cell growth. "
5.	Androgen-Insensitivity Syndrome (Testicular Feminization) 11/01/1984 - "Using conditions for optimal recovery of androgen receptor from human testes established by previous studies, we detected the presence of a high-affinity (dissociation constant = 3.2 X 10(-10) mol/L), low-capacity (4.2 X 10(-12) mol/mg DNA), androgen-binding protein when tritium-labeled R1881 was incubated at 4 degrees C with nuclear extracts from the gonads of control patients or from a patient with testicular feminization syndrome but not when incubated at 37 degrees C. " 07/01/1978 - "We have found a specific binding protein for synthetic progestins 6,7-[3H]methyltrienolone (R1881) and 17,21-dimethyl-19-norpregna-4,9-diene-3,20-dione (R5020) and in the testis cytosol from three "sisters" with the complete form of the testicular feminization syndrome. "

Related Drugs and Biologics

1.	Androgen Receptors (Androgen Receptor)
2.	Metribolone
3.	Androgens
4.	Tritium
5.	Dihydrotestosterone (Androstanolone)
6.	Messenger RNA (mRNA)
7.	DNA (Deoxyribonucleic Acid)
8.	Hormones
9.	Tretinoin (Retinoic Acid)
10.	Small Interfering RNA (siRNA)

Related Therapies and Procedures

1.	Castration
2.	Injections
3.	Aftercare (After-Treatment)