Binding of 7 alpha, 17 alpha-dimethyl-19-nortestosterone (mibolerone) to androgen and progesterone receptors in human and animal tissues.
In rat uterus and prostate, 7 alpha, 17 alpha-dimethyl-19-nortestosterone (DMNT) binds to the androgen receptor specifically and with high affinity. However, this steroid does not bind to glucocorticoid receptors, since it does not displace binding of [3H]triamcinolone acetonide in calf thymus cytosol. In calf uterine and human breast tumor cytosols DMNT binds to the androgen and progesterone receptors, since binding of [3H] DMNT is displaced by unlabeled 16 alpha-ethyl-21-hydroxy-19-nor-4-pregnene-3, 20-dione triamcinolone acetonide, and 5 alpha-dihydrotestosterone (DHT). Conversely, binding of [3H]16 alpha-ethyl-21-hydroxy-19-nor-4-pregnene-3,20-dione is effectively competed for by unlabeled DMNT but not by DHT. The observed differences in binding of [3H]DMNT to rat and calf uterine cytosols suggest the species specificity of progesterone receptors. Unlike DHT, DMNT has no appreciable binding to human sex-steroid binding globulin. These findings suggest DMNT as a suitable ligand for measurement and characterization of androgen receptors in rat and human prostate.
Traish
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Müller
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Wotiz
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D000818:Animals; D001798:Blood Proteins / Q000378:metabolism; D001940:Breast / Q000378:metabolism; D002417:Cattle; D002467:Cell Nucleus / Q000378:metabolism; D003600:Cytosol / Q000378:metabolism; D013196:Dihydrotestosterone / Q000378:metabolism; D004963:Estrenes / Q000378:metabolism; D005260:Female; D006801:Humans; D008297:Male; D015741:Metribolone; D009277:Nandrolone / Q000031:analogs & derivatives* / Q000378:metabolism; D011282:Pregnenediones / Q000378:metabolism; D011467:Prostate / Q000378:metabolism; D011470:Prostatic Hyperplasia / Q000378:metabolism; D051381:Rats; D011919:Rats, Inbred Strains; D011944:Receptors, Androgen / Q000378:metabolism*; D011980:Receptors, Progesterone / Q000378:metabolism*; D013379:Substrate Specificity; D014599:Uterus / Q000378:metabolism
D001798:Blood Proteins; D004963:Estrenes; D011282:Pregnenediones; D011944:Receptors, Androgen; D011980:Receptors, Progesterone; D013196:Dihydrotestosterone; C020175:16 alpha-ethyl-21-hydroxy-19-nor-4-pregnene-3,20-dione; D015741:Metribolone; D009277:Nandrolone; C100075:mibolerone