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Sex and Gender Differences in Pharmacology pp 543–587Cite as

Pharmacology and Clinical Use of Sex Steroid Hormone Receptor Modulators

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Part of the book series: Handbook of Experimental Pharmacology ((HEP,volume 214))

Abstract

Sex steroid receptors are ligand-triggered transcription factors. Oestrogen, progesterone and androgen receptors form, together with the glucocorticoid and mineralocorticoid receptors, a subgroup of the superfamily of nuclear receptors. They share a common mode of action, namely translating a hormone—i.e. a small-molecule signal—from outside to changes in gene expression and cell fate, and thereby represent “natural” pharmacological targets.

For pharmacological therapy, these receptors have originally been addressed by hormones and synthetic hormone analogues in order to overcome pathologies related to deficiencies in the natural ligands. Another major use for female sex hormone receptor modulators is oral contraception, i.e. birth control.

On the other side, blocking the activity of sex steroid receptors has become an established way to treat hormone-dependent malignancies, such as breast and prostate cancer.

In this review, we will discuss how the experience gained from the classical pharmacology of these receptors and their molecular similarities led to new options for the treatment of gender-specific diseases and highlight recent progress in medicinal chemistry of sex hormone-modulating drugs.

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Author notes

  1. T. Wintermantel

    Present address: A.T. Kearney GmbH, Kaistrasse 16A, 40221, Düsseldorf, Germany

Authors and Affiliations

  1. Global Drug Discovery, Medicinal Chemistry, Bayer Pharma AG, Muellerstr. 178, 13353, Berlin, Germany

    A. Cleve, N. Heinrich & W. Schwede

  2. Global Drug Discovery, Oncology/Gynecological Therapy, Bayer Pharma AG, Muellerstr. 178, 13353, Berlin, Germany

    K.-H. Fritzemeier & B. Haendler

  3. Global Market Access, Strategic Access and Operations, Bayer Pharma AG, Muellerstr. 178, 13353, Berlin, Germany

    C. Möller

  4. Corporate Development-Innovation, Bayer AG, Leverkusen, Germany

    T. Wintermantel

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  6. W. Schwede
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  7. T. Wintermantel
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Correspondence to T. Wintermantel .

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  1. Institute of Gender in Medicine (GiM), Center for Cardiovascular Research (CCR), Charité - Universitätsmedizin Berlin, Hessische Str. 3-4, Berlin, 10115, Germany

    Vera Regitz-Zagrosek

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Cleve, A. et al. (2013). Pharmacology and Clinical Use of Sex Steroid Hormone Receptor Modulators. In: Regitz-Zagrosek, V. (eds) Sex and Gender Differences in Pharmacology. Handbook of Experimental Pharmacology, vol 214. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-30726-3_24

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