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Journal Highlights

DMD Highlight: Structural and Functional Evaluation of Clinically Relevant Inhibitors of Steroidogenic Cytochrome P450 17A1

Posted on 5/19/2017 10:20:08 AM

DMD Highlight June Petrunak et al
 

CYP17A1 is an important therapeutic target in the treatment of prostate cancer. CYP17A1 has both 17-hydroxylase and 17,20 lyase activities, of which selective inhibition of the 17, 20 lyase activity is desirable for cancer treatment. Through careful characterization of inhibitor selectivity and structural analysis of inhibitor-bound enzymes, Petrunak and colleagues uncover a potential strategy for the development of more selective inhibitors via targeting a peripheral binding site in the enzyme.

See the article by Petrunak et al. at Drug Metabolism and Disposition June 2017, 45 (6) 635-645; DOI: https://doi.org/10.1124/dmd.117.075317 

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