Characterization of a hepatic protein in nonhuman primates that binds mibolerone but not dihydrotestosterone or methyltrienolone

Koritnik, Donald R.; Marschke, Keith B.; Koshy, A

doi:10.1016/0039-128x(95)00116-8

Cited by 3 publications

(3 citation statements)

References 34 publications

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“…ERα and ERβ are expressed in various cell types and tissues and the expression levels of their respective mRNAs appear to be regulated in a tissue‐specific and temporal manner. Furthermore, the ER mRNA levels are influenced by estrogen itself [14–16] or by other hormones [17–19]. A more complete understanding of the mechanism(s) that regulate(s) the tissue‐specific and temporal expression of ERs is essential towards understanding how the pleiotropic effects of estrogens are achieved in complex organisms.…”

Section: Introductionmentioning

confidence: 99%

Tissue‐specific expression of multiple mRNA variants of the mouse estrogen receptor α gene

et al. 2000

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The isolation of five new mouse estrogen receptor K K mRNA variants (mERK K A, B, F1, F2 and H) is described. All of these transcripts are generated by alternative splicing and all encode the 66 kDa ERK K protein that the previously identified mRNA C variant generates. However, these transcripts differ in their 5P P untranslated regions. RT-PCR and S1 nuclease protection assays revealed a tissue-and sex-specific expression pattern of all variants. The C and F mRNA variants are the predominantly expressed mERK K variants in mouse. The expression of mERK K H mRNA is restricted to liver, although female mice produce around a five fold higher level of this transcript than males. Our results show that the mERK K gene is a complex genomic unit in mice that exhibits alternative splicing which is regulated in a tissue-specific manner. ß

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Section: Introductionmentioning

confidence: 99%

Tissue‐specific expression of multiple mRNA variants of the mouse estrogen receptor α gene

et al. 2000

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“…However, nuclear binding in lamprey did not reach a complete saturation at 3 nM, similar to a slow saturation found in the nPR of zebrafish (Hanna et al, 2010). This result could be due to low affinity binding (Koritnik et al, 1995) or insufficient striping with charcoal (Wang et al, 1992). Charcoal separation method was widely used to separate free steroid hormones from steroid receptors, especially nPRs in fishes (Pinter and Thomas, 1995;Hanna et al, 2010).…”

Section: Discussionmentioning

confidence: 55%

Evidence that progestins play an important role in spermiation and pheromone production in male sea lamprey (Petromyzon marinus)

Bryan

Chung-Davidson

Ren

et al. 2015

General and Comparative Endocrinology

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“…Mibolerone has been used widely as a ligand for the study of androgen receptor (AR) because of its high-affinity binding and its greater stability compared to methyltrienolone [8] . When assayed orally in the rats, mibolerone was found to be approximately 18 times than methyltestosterone as an androgen agent [8−10] .…”

Section: Introductionmentioning

confidence: 99%

Synthesis and characterization of mibolerone

Yang

Fan

Tang

2007

J Cent. South Univ. Technol.

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Abstract：A simple and effective route for the synthesis of mibolerone was described starting from the estr-5(10)-en-3,17-dione in four steps with the overall yield of 47.0 %. Thus, two methods for key intermediate methylnorandrost were investigated: one(method A) starting from estr-4-en-3,17-dione underwent 3-keto group protected with ethyl orthoformate to give 3-ethoxy-3,5-dien-estr-17-one, the other(method B) from estr-5(10)-en-3,17-dione and protected 3-keto group to give 3,3-dimethoxy-estr-5(10)-7-one in a mild acidic condition. Then, two intermediates were subsequently reacted with methyllithium followed by a mild hydrolytic procedure and gave methylnorandrost with total yield 25.0% and 86.0 %, respectively. In the preparation of 6-dehydrogenation product of methylnorandrost, two procedures(method C and method D) were investigated: one was the protected 17α-methyl-17β-hydroxy ∆ 3,5 -enol ethers estrendiene brominated and the resulting 6-bromo-19-methylnortestosterone was then immediately dehydrohaloenated to give 6-dehydro-19-methylnortestosterone, the total yield only reaches 36.0%; the other was directly dehydrogenated with chloranil and the yield reaches 75.6% under the optimum conditions: in refluxing tetrahydrofuran, the molar ratio of methylnorandrost to chloranil is 0.66 and reaction time of 5 h. The titled compound and intermediates were characterized by 1 H and 13 C NMR, IRMS and elemental analysis.

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Characterization of a hepatic protein in nonhuman primates that binds mibolerone but not dihydrotestosterone or methyltrienolone

Cited by 3 publications

References 34 publications

Tissue‐specific expression of multiple mRNA variants of the mouse estrogen receptor α gene

Tissue‐specific expression of multiple mRNA variants of the mouse estrogen receptor α gene

Evidence that progestins play an important role in spermiation and pheromone production in male sea lamprey (Petromyzon marinus)

Synthesis and characterization of mibolerone

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