Metabolism and Protein Binding of Sex Steroids in Target Organs: An Approach to the Mechanism of Hormone Action

Baulieu, Étienne-Émile; Alberga, Audrey; Jung, Ioan; Lebeau, Marie‐Claire; Mercier-Bodard, Christine; Milgröm, Edwin; Raynaud, Jean‐Pierre; Raynaud-Jammet, C.; Rochefort, Henri; Truong, H; Röbel, P

doi:10.1016/b978-0-12-571127-2.50033-x

Cited by 48 publications

(28 citation statements)

References 50 publications

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“…These macromolecules are present in both immature and mature rat testis cytosol and have a sedimentation coefficient of approx. 8 S. The affinity constant of 4 ~ l09 M -1 at 4 ° for this oestrogen-macromolecular complex is of the same order of magnitude as the affinity constants reported for cytoplasmic receptors for oestradiol and dihydrotestosterone in uterus and prostate tissue [8]. Other steroids did not compete with oestradiol binding to the testis cytoplasmic receptor, indicating a high specificity of the binding sites for oestradiol.…”

Section: Discussionsupporting

confidence: 58%

An Oestradiol receptor in rat testis interstitial tissue

et al. 1972

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Section: Discussionsupporting

confidence: 58%

An Oestradiol receptor in rat testis interstitial tissue

et al. 1972

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“…The above observations are in keeping with the results of others, indicating that dihydrotestosterone is the major intranuclear androgen in prostate and seminal vesicle and caput epididymis (11)(12)(13), whereas testosterone is observed in testicular nuclei. Smaller amounts of testosterone were also present and were displaceable Six testes were perfused with 85nM 3H-testosterone and the KCI extract of the nuclei placed on the sucrose gradients after charcoal adsorption.…”

Section: Androgen Binding In Testicular Nucleisupporting

confidence: 78%

Methods for Perfusing the Male Reproductive Tract: Models for Studying Drug and Hormone Metabolism

Bardin¹,

Baker²,

Jefferson³

et al. 1978

Environmental Health Perspectives

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Methods for perfusing rat testis and accessory sex organs in situ by recirculating artificial medium to the hemicorpus preparation are described. The advantages and limitations of this system for studying the male reproductive tract were examined. The preparation was then used to study the uptake of androgens into the nuclei of caput epididymis, ventral prostate, seminal vesicle and testis. The accumulation of dihydrotestosterone and accessory sex organ nuclei was saturable and inhibited by perfusion of excess testosterone or cypr(terone acetate. By contrast, testosterone was the major nuclear androgen in the testis of mature hypophysectomized preparations perfused with testosterone. In all parts of the reproductive tract, 'H-nuclear androgens were associated with 3S, salt-extractable macromolecules within the properties of androgen receptors.The hemicorpus preparation was extensively compared with two techniques (selective and isolated) for perfusing the testis directly. Of these two procedures, the isolated method was superior when only the testes were studied. However, the hemicorpus preparation offers the advantage of studying testes along with the remainder of the male reproductive tract. A variety of observations suggest that these perfusion procedures will be useful for the study of drug as well as hormone metabolism and mechanism of action.Investigations of drug and hormone metabolism and mechanism of action are facilitated by the use of perfusion techniques. Perfusion offers several advantages over methods employing dissected tissue or intact animals including: control of medium composition entering the organ, delivery of substrates via the vascular bed, metabolism of drug or hormone only by the organ under study and quantitative analysis of hormone or drug transfer between functional compartments. Studies from this laboratory have characterized a method for in situ perfusion of the male rat reproductive tract using a hemicorpus preparation (/, 2). In addition, a technique for direct perfusion of isolated testis was de-

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“…supernatant) frac tion of target tissue homogenates in low ionic strength buffer. All receptors thus ob tained sediment as a 8-1 OS hormone-bind ing entity (designated as 8S-R), of apparent MW ~ 300,000 daltons [9,10]. If the extrac tion is performed with high ionic strength buffer (usually >0.25 M KC1), or if second arily the 8S-R is exposed to such a salt-con taining medium, the hormone-binding peak sediments with a ~4 S sedimentation coeffi cient (4S-R).…”

Section: Generalities and Complexitymentioning

confidence: 99%

Antihormone-Steroid Hormonal Activity, Heat-Shock Protein hsp 90 and Receptors

Baulieu¹

1987

Horm Res

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Antisteroid hormones compete for hormone binding at the receptor level and prevent the hormonal response. A new concept is proposed for explaining the antiglucocorticosteroid activity of RU 486 in the chick oviduct system. It is based on the ability of the antisteroid to stabilize the hetero-oligomeric 8S-form of the glucocorticosteroid receptor, which involves the interaction of the 94,000-dalton receptor and the heat-shock protein MW 90,000 (hsp 90). It is proposed that hsp 90 caps the DNA-binding site of the receptor, and this prevents it from binding to the DNA of hormone regulatory elements and to increase transcription of regulated genes. This paper reviews other antiglucocorticosteroid and antiestrogen systems with reference to this hypothesis, and also describes a four-step analysis of the molecular mechanism of antisteroid hormone action at the receptor level.

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Metabolism and Protein Binding of Sex Steroids in Target Organs: An Approach to the Mechanism of Hormone Action

Cited by 48 publications

References 50 publications

An Oestradiol receptor in rat testis interstitial tissue

An Oestradiol receptor in rat testis interstitial tissue

Methods for Perfusing the Male Reproductive Tract: Models for Studying Drug and Hormone Metabolism

Antihormone-Steroid Hormonal Activity, Heat-Shock Protein hsp 90 and Receptors

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