Kinetic Analysis of LY320236: Competitive Inhibitor of Type I and Non-Competitive Inhibitor of Type II Human Steroid 5α-Reductase

    January 2000 in “ The Journal of Steroid Biochemistry and Molecular Biology ”
    Ann M. McNulty, James E. Audia, Kerry G. Bemis, Robin L. Goode, Vincent P. Rocco, Blake Lee Neubauer
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    TLDR LY320236 is a strong blocker of two enzymes that change testosterone into dihydrotestosterone and might help treat conditions related to male hormones.
    The study analyzed LY320236, a benzoquinolinone compound, and found it to be a potent inhibitor of both type I and type II human steroid 5α-reductases, which are key in converting testosterone to dihydrotestosterone. LY320236 acted as a competitive inhibitor of type I 5α-reductase with a Ki value of 3.39±0.38 nM and a non-competitive inhibitor of type II with a Ki value of 29.7±3.4 nM. These results, obtained through various analytical methods including Lineweaver-Burk and Dixon analyses, suggest that LY320236 could be therapeutically useful for treating androgen-dependent disorders. The study was based on in vitro enzymatic assays and did not involve human subjects.
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