Inhibitors of Androgen Receptor Activation Function-2 (AF2) Site Identified through Virtual Screening

Axerio-Cilies, P., et al., 54 (18), 6197-6205, Journal of Medicinal Chemistry, 2011

This study employs computer-aided design to identify small-molecule androgen receptor inhibitors that specifically target the receptor's activation function-2 (AF2) site. Interactions between the inhibitors and the androgen receptor were quantified using the Octet RED platform. Biotinylated androgen receptor LBD was immobilized on Super Streptavidin biosensors and used to characterize direct binding of the small-molecule inhibitors.

Read More