WNT signalling in prostate cancer

V Murillo-Garzón, R Kypta - Nature Reviews Urology, 2017 - nature.com
Genome sequencing and gene expression analyses of prostate tumours have highlighted
the potential importance of genetic and epigenetic changes observed in WNT signalling …

Towards precision oncology in advanced prostate cancer

SY Ku, ME Gleave, H Beltran - Nature Reviews Urology, 2019 - nature.com
Metastatic biopsy programmes combined with advances in genomic sequencing have
provided new insights into the molecular landscape of castration-resistant prostate cancer …

[HTML][HTML] SETD2 restricts prostate cancer metastasis by integrating EZH2 and AMPK signaling pathways

H Yuan, Y Han, X Wang, N Li, Q Liu, Y Yin, H Wang… - Cancer cell, 2020 - cell.com
The level of SETD2-mediated H3K36me3 is inversely correlated with that of EZH2-catalyzed
H3K27me3. Nevertheless, it remains unclear whether these two enzymatic activities are …

[HTML][HTML] Second generation androgen receptor antagonists and challenges in prostate cancer treatment

Y Chen, Q Zhou, W Hankey, X Fang, F Yuan - Cell Death & Disease, 2022 - nature.com
Prostate cancer is a hormone-dependent malignancy, whose onset and progression are
closely related to the activity of the androgen receptor (AR) signaling pathway. Due to this …

Transdifferentiation as a mechanism of treatment resistance in a mouse model of castration-resistant prostate cancer

M Zou, R Toivanen, A Mitrofanova, N Floch, S Hayati… - Cancer discovery, 2017 - AACR
Current treatments for castration-resistant prostate cancer (CRPC) that target androgen
receptor (AR) signaling improve patient survival, yet ultimately fail. Here, we provide novel …

Effective combinatorial immunotherapy for castration-resistant prostate cancer

X Lu, JW Horner, E Paul, X Shang, P Troncoso, P Deng… - Nature, 2017 - nature.com
A significant fraction of patients with advanced prostate cancer treated with androgen
deprivation therapy experience relapse with relentless progression to lethal metastatic …

Discovery of ARD-2051 as a potent and orally efficacious proteolysis targeting chimera (PROTAC) degrader of androgen receptor for the treatment of advanced …

X Han, L Zhao, W Xiang, B Miao, C Qin… - Journal of Medicinal …, 2023 - ACS Publications
We report the discovery of ARD-2051 as a potent and orally efficacious androgen receptor
(AR) proteolysis-targeting chimera degrader. ARD-2051 achieves DC50 values of 0.6 nM …

Pre-existing castration-resistant prostate cancer–like cells in primary prostate cancer promote resistance to hormonal therapy

Q Cheng, W Butler, Y Zhou, H Zhang, L Tang… - European urology, 2022 - Elsevier
Background Hormonal therapy targeting the androgen receptor inhibits prostate cancer
(PCa), but the tumor eventually recurs as castration-resistant prostate cancer (CRPC) …

[HTML][HTML] Targeted degradation of transcription factors by TRAFTACs: transcription factor targeting chimeras

KTG Samarasinghe, S Jaime-Figueroa, M Burgess… - Cell chemical …, 2021 - cell.com
Many diseases, including cancer, stem from aberrant activation or overexpression of
oncoproteins that are associated with multiple signaling pathways. Although proteins with …

A phase II trial of the aurora kinase a inhibitor alisertib for patients with castration-resistant and neuroendocrine prostate cancer: efficacy and biomarkers

H Beltran, C Oromendia, DC Danila… - Clinical Cancer …, 2019 - AACR
Purpose: Neuroendocrine prostate cancer (NEPC) is an aggressive variant of prostate
cancer that may develop de novo or as a mechanism of treatment resistance. N-myc is …