Coumarins as Tool Compounds to Aid the Discovery of Selective Function Modulators of Steroid Hormone Binding Proteins |
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Authors: | Sanna Niinivehmas Olli T Pentikinen |
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Institution: | 1.Faculty of Medicine, Institute of Biomedicine, University of Turku, FI-20520 Turku, Finland;2.InFLAMES Research Flagship Center, University of Turku, FI-20520 Turku, Finland;3.Aurlide Ltd., FI-20520 Turku, Finland |
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Abstract: | Steroid hormones play an essential role in a wide variety of actions in the body, such as in metabolism, inflammation, initiating and maintaining sexual differentiation and reproduction, immune functions, and stress response. Androgen, aromatase, and sulfatase pathway enzymes and nuclear receptors are responsible for steroid biosynthesis and sensing steroid hormones. Changes in steroid homeostasis are associated with many endocrine diseases. Thus, the discovery and development of novel drug candidates require a detailed understanding of the small molecule structure–activity relationship with enzymes and receptors participating in steroid hormone synthesis, signaling, and metabolism. Here, we show that simple coumarin derivatives can be employed to build cost-efficiently a set of molecules that derive essential features that enable easy discovery of selective and high-affinity molecules to target proteins. In addition, these compounds are also potent tool molecules to study the metabolism of any small molecule. |
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Keywords: | coumarin 3-phenylcoumarin estrogen receptor aromatase 17β -hydroxysteroid dehydrogenase |
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