Figure 3.

Novel preclinical agents that suppress AR/AR-Vs by regulating gene expression, degradation, AR transcriptional activity, and downstream signaling. The following broad categories are summarized. Refer to Table I for details.

(1) Targeting AR/AR-Vs translation: 6BIO+PS-LNA-AR-ASO

(2) Novel AR antagonists: EPIs, 3E10-AR411, VPC-3022, SARDs, Ad-E1A12 variant,

(3) Enhancing AR or AR-Vs degradation: Niclosamide, ASC-J9, alisertib, PROTAC degrader, leelamine

(4) Targeting AR chaperones: C86, VER155008, onalespib

(5) Targeting molecules involved in epigenetic modification: BETi, HDACi, CUDC-101, EZH2i, astemizole

(6) Targeting AR/AR-Vs co-regulators or transcriptional activity: KCI807, triptolide/minnelide, clorgyline/phenelzine, IPI-9119, BETi

(7) Targeting AR/AR-Vs downstream signaling molecules: LY2090314, N9 + doxorubicin, G1T28/G1T38, alisertib, FrA