A2 Vertaisarvioitu katsausartikkeli tieteellisessä lehdessä
Coumarins as Tool Compounds to Aid the Discovery of Selective Function Modulators of Steroid Hormone Binding Proteins
Tekijät: Niinivehmas Sanna, Pentikäinen Olli T.
Kustantaja: MDPI
Julkaisuvuosi: 2021
Journal: Molecules
Tietokannassa oleva lehden nimi: MOLECULES
Lehden akronyymi: MOLECULES
Artikkelin numero: ARTN 5142
Vuosikerta: 26
Numero: 17
Sivujen määrä: 17
DOI: https://doi.org/10.3390/molecules26175142
Rinnakkaistallenteen osoite: https://research.utu.fi/converis/portal/detail/Publication/67221940
Tiivistelmä
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.
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.
Ladattava julkaisu This is an electronic reprint of the original article. |  |
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