| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 8338622 | The Journal of Steroid Biochemistry and Molecular Biology | 2014 | 31 Pages |
Abstract
- Abiraterone analogs with modified A/B-rings retain nanomolar affinity for CYP17A1.
- CYP17A1 inhibition by abiraterone and analogs is mixed competitive/noncompetitive.
- Dissociation of abiraterone from CYP17A1 is slow (koff < 0.01 minâ1) and incomplete.
- The 3β-hydroxyl Î5-system of abiraterone is not required for high CYP17A1 affinity.
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Authors
Mariana Garrido, Hwei-Ming Peng, Francis K. Yoshimoto, Sunil K. Upadhyay, Eugene Bratoeff, Richard J. Auchus,