[DOWNLOAD] "Structural Characterization of Androgen Receptor Interactions with Nonsteroidal Ligands" by Casey Edward Bohl # Book PDF Kindle ePub Free

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eBook details

• Title: Structural Characterization of Androgen Receptor Interactions with Nonsteroidal Ligands
• Author : Casey Edward Bohl
• Release Date : January 18, 2013
• Genre: Medical,Books,Professional & Technical,
• Pages : * pages
• Size : 11569 KB

Description

The following research was aimed at uncovering the binding interactions of nonsteroidal ligands with the androgen receptor (AR). Steroidal binding to the AR is well understood through x-ray crystallography and mutational analysis. The binding mechanism for the nonsteroidal antiandrogens used in prostate cancer treatment however was unknown despite prevalent clinical use for nearly 20 years. Our laboratory discovered selective androgen receptor modulators (SARMs) by structural modification of currently available nonsteroidal antiandrogens. Collaboration with a group of medicinal chemists led to a vast number of potential therapeutic agents that target the AR, but their binding mechanism could not be explained based on currently published crystal structures complexed to steroids. We investigated the interactions between nonsteroidal ligands and the AR using a variety of approaches including molecular modeling, mutational analysis, and x-ray crystallography. Nonsteroidal ligands induced structural changes in the AR binding pocket allowing for their accommodation. Furthermore, crystal structures of currently prescribed antiandrogens complexed to mutant AR associated with resistance provided information regarding their mechanism of action. Knowledge of AR interactions with nonsteroidal ligands will provide the basis for development of improved drugs that target the AR.

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