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Related Experiment Videos

Receptor binding of STS 557.

G Kaufmann, J Schlegel, B Eychenne

    Experimental and Clinical Endocrinology
    |February 1, 1983
    PubMed
    Summary

    The new progestagen STS 557 shows strong binding to progesterone receptors in mammals, with lower affinity in chicks. It also binds to androgen receptors, suggesting potential dual activity.

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    Area of Science:

    • Endocrinology
    • Steroid chemistry
    • Pharmacology

    Background:

    • Progestagens are crucial for reproductive functions.
    • Understanding novel progestagen binding is key for therapeutic development.
    • STS 557 is a new synthetic progestagen with an unexplored receptor binding profile.

    Purpose of the Study:

    • To investigate the binding affinity of STS 557 to progesterone receptors across species.
    • To compare the binding of STS 557 derivatives to progesterone receptors.
    • To assess the binding of STS 557 to androgen receptors.

    Main Methods:

    • Competitive binding assays using cytosol preparations from chick oviduct, rat uterus, rabbit uterus, and human endometrium.
    • Evaluation of five STS 557 derivatives for progesterone receptor binding.
    • Measurement of binding to rat prostate cytosol androgen receptors.

    Main Results:

    • STS 557 demonstrated high competitive potency for mammalian progesterone receptors, with binding affinity approximately 20% of progesterone.
    • Binding to chick oviduct receptors was significantly lower (two orders of magnitude less).
    • Planar derivatives of STS 557 retained similar progesterone receptor affinities, while 5 beta-H compounds were inactive. STS 557 and its planar derivatives also competed effectively with 5 alpha-dihydrotestosterone (DHT) for androgen receptors, showing about one-fifth the binding affinity of DHT.

    Conclusions:

    • STS 557 exhibits potent binding to mammalian progesterone receptors and moderate binding to androgen receptors.
    • The structural planarity of the steroid ring system is important for both progesterone and androgen receptor binding.
    • These findings provide insights into the structure-activity relationship and potential dual action of STS 557.

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