Rational optimization of a transcription factor activation domain inhibitor
S. Basu, P. Martinez-Cristobal, M. Pesarrodona, M. Frigole-Vivas, E. Szulc, M. Lewis, A. Banuelos, C. Sanchez-Zarzalejo, S. Bielskute, J. Zhu, K. Pombo-Garcia, C. Garcia-Cabau, C. Batlle, B. Mateos, M. Biesaga, , X. Salvatella
This study optimizes a small molecule inhibitor targeting the aromatic-rich activation domain of the androgen receptor, showing improved affinity and antitumorigenic effects in prostate cancer models.
bioRxiv · Aug 18, 2022Biochemistry