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

Bio-Agent Context: Research Results

Experts

1.	Thomas, Lynn N: 2 articles (01/2020 - 03/2014)
2.	Fang, Shengyun: 2 articles (04/2017 - 01/2017)
3.	Sun, Junyan: 2 articles (04/2017 - 01/2017)
4.	Wang, Yang: 2 articles (04/2017 - 01/2017)
5.	Xing, Rong: 2 articles (04/2017 - 01/2017)
6.	Danielpour, David: 2 articles (03/2016 - 01/2002)
7.	Trapman, Jan: 2 articles (01/2011 - 11/2005)
8.	Rodriguez, Ronald: 2 articles (03/2010 - 05/2002)
9.	Horie-Inoue, Kuniko: 2 articles (01/2009 - 12/2004)
10.	Inoue, Satoshi: 2 articles (01/2009 - 12/2004)

Related Diseases

1.	Neoplasms (Cancer) 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. " 01/01/1995 - "Inhibitory effects of either T and DHT < R1881 < Pg were observed in tumors co-expressing AR and PgR. "
2.	Prostatic Neoplasms (Prostate Cancer) 01/01/2020 - "RAI16 expression was detected in prostate cancer cells with or without the AR agonist R1881 treatment by quantitative RT-PCR and Western blot. " 01/01/1987 - "Grade and histochemical R-1881 binding in prostatic cancer." 07/01/1984 - "II. Correlation between clinical response to hormonal therapy and change of R1881 receptor content in prostatic cancer during antiandrogenic therapy]." 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). "
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. " 07/01/1984 - "We have studied various properties of the binding of 5 alpha-dihydrotestosterone (DHT) or the synthetic, nonmetabolizable androgen methyltrienolone (R1881; 17 beta-hydroxy-17 alpha-methylestra-4,9,11-trien-3-one) to the androgen receptor of genital skin fibroblasts (GSF) from controls and a subject with familial, receptor-positive, partial androgen insensitivity. "

Related Drugs and Biologics

1.	Androgens
2.	Androgen Receptors (Androgen Receptor)
3.	Testosterone Congeners
4.	Metribolone
5.	Tritium
6.	Dihydrotestosterone (Androstanolone)
7.	Proteins (Proteins, Gene)
8.	Messenger RNA (mRNA)
9.	Steroids
10.	DNA (Deoxyribonucleic Acid)

Related Therapies and Procedures

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