Table | Restoration of AR signalling and GR overexpression in resistant CRPC Table | Restoration of AR signalling and GR overexpression in resistant CRPC Table | Restoration of AR signalling and GR overexpression in resistant CRPC Table | Restoration of AR signalling and GR overexpression in resistant CRPC Table | Restoration of AR signalling and GR overexpression in resistant CRPC
Mechanisms Signalling pathways/Targets Signalling pathways/Targets Solutions References
AR reactivation AR enhancer (650 kb centromeric) (Takeda, Spisák et al., 2018)
Galectin-3 (Dondoo, Fukumori et al., 2017)
BMI1 PTC209 (BMI1 inhibitor) PTC209 (BMI1 inhibitor) (Zhu, Zhao et al., 2018)
FOXA1/CREB5/AR (Hwang, Seo et al., 2019)
IKBKE/Hippo/c-Myc/AR (Bainbridge, Walker et al., 2020)
EphB4/c-Myc/AR EphB4 inhibitors EphB4 inhibitors (Li, Lanman et al., 2020)
eIF4F (Liu, Horn et al., 2019)
STAT3/AR GPA500 GPA500 (Thaper, Vahid et al., 2018)
AR/AR-Vs Triptolide Triptolide (Han, Huang et al., 2017)
AR Tetraaryl cyclobutane (CBs) Tetraaryl cyclobutane (CBs) (Pollock, Wardell et al., 2016)
AR ARCC-4/UT-34/IRF8 ARCC-4/UT-34/IRF8 (Salami, Alabi et al., 2018)
AR splice variants lncRNA Malat1 (Tummala, Lou et al., 2017; Stone, 2017; Zhao, Wang et al., 2018)
ACK1/pY88-H4/WDR5/MLL2/AR, AR-V7 (Mahajan, Malla et al., 2017)
AR-V7 SPT SPT (Lam, Nguyen et al., 2020)
AVPR1A (Zhao, Peacock et al., 2019)
NK cells/microRNA-34, microRNA-449/AR-V7, EZH2 (Lin, Chou et al., 2017)
HSP70/STUB1/AR-V7 (Liu, Lou et al., 2018)
AKR1C3/AR-V7 (Liu, Yang et al., 2019)
AR-V7 ABT263 (BCL2 protein inhibitor)/IPI-9119 (fatty acid synthase inhibitor)/Luteolin/CDDO-Me/Degarelix ABT263 (BCL2 protein inhibitor)/IPI-9119 (fatty acid synthase inhibitor)/Luteolin/CDDO-Me/Degarelix (Zadra, Ribeiro et al., 2019; Naiki-Ito, Naiki et al., 2019; Khurana, Chandra et al., 2020; Cucchiara, Yang et al., 2019)
c-Myc/AR-Vs, AR-FL Quiflapon (5-Lox inhibitor) Quiflapon (5-Lox inhibitor) (BaiCao et al., 2019; Monga, Subramani et al., 2020)
GATA2/AR-FL, AR-Vs (Chaytor, Simcock et al., 2019)
BRD4 JQI/I-BET762 (BET inhibitors) JQI/I-BET762 (BET inhibitors) (Asangani, Dommeti et al., 2014; Chan, Selth et al., 2015)
ZFX/AR-V7 (Cai, Tsai et al., 2018)
PARP/AR-V7 (Kounatidou, Nakjang et al., 2019)
AR mutations AR F876L mutation ASC-J9®/JJ-450 ASC-J9®/JJ-450 (Joseph, Lu et al., 2013; Korpal, Korn et al., 2013; Wang, Lin et al., 2016)
F877L, H875Y, T878A/D891H, and T878A/S889G ODM-201 ODM-201 (Prekovicvan Royen et al., 2016; Borgmann, Lallous et al., 2018; LallousVolik et al., 2016)
GR overexpression AMFR-11β-HSD2 (Li, Alyamani et al., 2017)
TLE3 (Palit, Vis et al., 2019)
PI3K/AKT/GR (Adelaiye-Ogala, Gryder et al., 2020)
GR/AR Z19 (GR/AR dual antagonist) Z19 (GR/AR dual antagonist) (Wu, Xie et al., 2019)