Structural Characterization and Ligand-Specific Protein Interactions of Androgen Receptor

The study investigated the structural and biochemical differences between two selective androgen receptor modulators (SARMs), 007 and 014, when bound to the androgen receptor (AR). It was found that AR-007 degraded more quickly than AR-014 when exposed to heat, indicating it was less stable. Both AR-007 and AR-014 had similar trypsin degradation patterns, but they were more stable than the AR-DHT complex. Additionally, AR-007 showed a stronger association with heat shock protein 70 (hsp70) compared to AR-014. The research concluded that SARM-induced conformational changes in the AR are ligand-specific, affecting the receptor's stability and its interactions with intracellular proteins, which contributes to their distinct pharmacological profiles compared to steroidal androgens.