期刊
AGING-US
卷 13, 期 5, 页码 6982-6998出版社
IMPACT JOURNALS LLC
DOI: 10.18632/aging.202554
关键词
androgen receptor; HDAC6; prostate cancer; dual inhibitor; Zeta55
资金
- National Natural Science Foundation of China [81570537, 81974074, 81703412]
- Science and Technology Planning Project of Hunan Province [2018TP1017]
Zeta55, a novel AR/HDAC6 dual inhibitor, demonstrated anticancer effects by inhibiting nuclear translocation of AR, degrading AR, and selectively inhibiting HDAC6 activity, showing promise as a therapeutic in prostate cancer treatment.
Androgen receptor (AR) and histone deacetylase 6 (HDAC6) are important targets for cancer therapy. Given that both AR antagonists and HDAC6 inhibitors modulate AR signaling, a novel AR/HDAC6 dual inhibitor is investigated for its anticancer effects in castration-resistant prostate cancer (CRPC). Zeta55 inhibits nuclear translocation of AR and suppresses androgen-induced PSA and TMPRSS2 expression. Meanwhile, Zeta55 selectively inhibits HDAC6 activity, leading to AR degradation. Zeta55 reduces the growth of AR-overexpressing VCaP prostate cancer cells both in vitro and in a CRPC xenograft model. These results provide preclinical proof of principle for Zeta55 as a promising therapeutic in prostate cancer treatment.
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