Health Research, Inc.

University of Kentucky Research Foundation

James L Mohler

Vitaliy M Sviripa

Yun Li

Mark Titus

Olga Kozyreva

O Harris Ford, Iii

Elsbieta Kawinski

Michael V Fiandalo

David Watt

Provided are androstane and dihydrotestosterone compounds functionalized with carbocyclic groups or heterocyclic groups that may be saturated or unsaturated. The compounds may be used in methods of inhibiting cell growth of malignant cells and/or hyperplastic cells and/or treating individuals having diseases associated with malignant cell growth (e.g., cancer, such as, for example, prostate cancer) and/or hyperplastic cell growth and/or molecular imaging of malignant cells and/or hyperplastic cells and/or inducing degradation of a target protein. Also provided are compositions.

Coumarin-modified androgens for the treatment of prostate cancer

The invention provides an isolated, novel steroid 5&#x3b1;-reductase enzyme termed SRD5AIII. The protein has an estimated molecular weight of 37 kDa and is capable of converting testosterone to dihydrotestosterone at a pH of about 7.0. Also provided is a method for identifying inhibitors of SRD5AIII by contacting SRD5AIII with a test compound and measuring the activity of the enzyme. A reduced activity relative to a control indicates that the test compound is an inhibitor of SRD5AIII. A method is also provided for detecting androgen stimulated prostate cancer or recurrent prostate cancer in an individual. The method comprises obtaining a prostate biopsy from an individual and determining the level of expression of SRD5AIII gene or protein relative to a normal control. An increased expression of SRD5AIII relative to the control is indicative of androgen stimulated prostate cancer or recurrent prostate cancer.

Steroid 5&#x3b1;-reductase

Growing community of inventors

Buffalo, NY, United States of America

James L Mohler