Search Results - "Obst, Jon K."

Inhibitors of the transactivation domain of androgen receptor as a therapy for prostate cancer by Obst, Jon K., Tien, Amy H., Setiawan, Josie C., Deneault, Lauren F., Sadar, Marianne D.

“…•The androgen receptor plays a key role in prostate cancer.•The androgen receptor is transactivated by androgens.•Castration is a critical component in the…”
Get full text

Rational optimization of a transcription factor activation domain inhibitor by Basu, Shaon, Martínez-Cristóbal, Paula, Frigolé-Vivas, Marta, Pesarrodona, Mireia, Lewis, Michael, Szulc, Elzbieta, Bañuelos, C. Adriana, Sánchez-Zarzalejo, Carolina, Bielskutė, Stasė, Zhu, Jiaqi, Pombo-García, Karina, Garcia-Cabau, Carla, Zodi, Levente, Dockx, Hannes, Smak, Jordann, Kaur, Harpreet, Batlle, Cristina, Mateos, Borja, Biesaga, Mateusz, Escobedo, Albert, Bardia, Lídia, Verdaguer, Xavier, Ruffoni, Alessandro, Mawji, Nasrin R., Wang, Jun, Obst, Jon K., Tam, Teresa, Brun-Heath, Isabelle, Ventura, Salvador, Meierhofer, David, García, Jesús, Robustelli, Paul, Stracker, Travis H., Sadar, Marianne D., Riera, Antoni, Hnisz, Denes, Salvatella, Xavier

“…Transcription factors are among the most attractive therapeutic targets but are considered largely ‘undruggable’ in part due to the intrinsically disordered…”
Get full text

Differential Gene Expression Profiles between N-Terminal Domain and Ligand-Binding Domain Inhibitors of Androgen Receptor Reveal Ralaniten Induction of Metallothionein by a Mechanism Dependent on MTF1 by Obst, Jon K, Mawji, Nasrin R, Teskey, Simon J L, Wang, Jun, Sadar, Marianne D

“…Hormonal therapies for prostate cancer target the androgen receptor (AR) ligand-binding domain (LBD). Clinical development for inhibitors that bind to the…”
Get full text

Ralaniten Sensitizes Enzalutamide-Resistant Prostate Cancer to Ionizing Radiation in Prostate Cancer Cells that Express Androgen Receptor Splice Variants by Banuelos, Carmen A., Ito, Yusuke, Obst, Jon K., Mawji, Nasrin R., Wang, Jun, Hirayama, Yukiyoshi, Leung, Jacky K., Tam, Teresa, Tien, Amy H., Andersen, Raymond J., Sadar, Marianne D.

“…Blocking androgen receptor (AR) transcriptional activity by androgen deprivation therapy (ADT) improves the response to radiotherapy for intermediate and high…”
Get full text

Lessons learned from the metastatic castration-resistant prostate cancer phase I trial of EPI-506, a first-generation androgen receptor N-terminal domain inhibitor by Le Moigne, Ronan, Zhou, Han-Jie, Obst, Jon K., Banuelos, C. Adriana, Jian, Kunzhong, Williams, David, Virsik, Peter, Andersen, Raymond J, Sadar, Marianne, Perabo, Frank, Chi, Kim N.

“…Abstract only 257 Background: Aniten compounds bind to the N-terminal domain (NTD) of the androgen receptor (AR) and inhibit AR dependent transcription…”
Get full text

Revealing Metabolic Liabilities of Ralaniten To Enhance Novel Androgen Receptor Targeted Therapies by Obst, Jon K, Wang, Jun, Jian, Kunzhong, Williams, David E, Tien, Amy H, Mawji, Nasrin, Tam, Teresa, Yang, Yu Chi, Andersen, Raymond J, Chi, Kim N, Montgomery, Bruce, Sadar, Marianne D

“…Inhibition of the androgen receptor (AR) is the mainstay treatment for advanced prostate cancer. Ralaniten (formally EPI-002) prevents AR transcriptional…”
Get full text

Directing abiraterone metabolism: balancing the scales between clinical relevance and experimental observation by Obst, Jon K., Sadar, Marianne D.

Get full text