Display options
Cite
Steinsapir J, Mora G, Muldoon TG, et al. Androgenic Activity of Antiandrogens Predicted by Fit into DNA. Am J Ther. 1994;1(3):236-244doi: 10.1097/00045391-199410000-00011.
Steinsapir, J., Mora, G., Muldoon, T. G., Mahesh, V. B., & Hendry, L. B. (1994). Androgenic Activity of Antiandrogens Predicted by Fit into DNA. American journal of therapeutics, 1(3), 236-244. https://doi.org/10.1097/00045391-199410000-00011
Steinsapir, Jaime, et al. "Androgenic Activity of Antiandrogens Predicted by Fit into DNA." American journal of therapeutics vol. 1,3 (1994): 236-244. doi: https://doi.org/10.1097/00045391-199410000-00011
Steinsapir J, Mora G, Muldoon TG, Mahesh VB, Hendry LB. Androgenic Activity of Antiandrogens Predicted by Fit into DNA. Am J Ther. 1994 Oct;1(3):236-244. doi: 10.1097/00045391-199410000-00011. PMID: 11835093.
Copy Download .nbib Format: NLM
Share it on

Am J Ther. 1994 Oct;1(3):236-244. doi: 10.1097/00045391-199410000-00011.

Androgenic Activity of Antiandrogens Predicted by Fit into DNA.

American journal of therapeutics

Jaime Steinsapir, Gloria Mora, Thomas G. Muldoon, Virendra B. Mahesh, Lawrence B. Hendry

Affiliations

  1. Drug Design and Development Laboratory, Department of Physiology and Endocrinology CLW 3134, Medical College of Georgia, Augusta, USA.

PMID: 11835093 DOI: 10.1097/00045391-199410000-00011

Abstract

Computer modeling including graphics and energy calculations were employed for the first time to examine the stereochemical fit of antiandrogens into double-stranded DNA. In this study, we assessed the relative fit of antiandrogens in the cavity between base pairs known to accommodate androgens. When compared to testosterone which was given a normalized value of 100%, the antiandrogens manifested the following order of fit: RU23908 (88%) > hydroxyflutamide (71%) > cyproterone acetate (41%). A correlation was observed between the relative fit of the antiandrogens and reported agonistic properties as assessed by the ability to increase nuclear androgen receptor levels in the rat ventral prostate. These findings may be useful in the design and development of androgen antagonists without agonistic activity.

Publication Types