Advances in targeting 'undruggable'transcription factors with small molecules

MJ Henley, AN Koehler - Nature Reviews Drug Discovery, 2021 - nature.com
Transcription factors (TFs) represent key biological players in diseases including cancer,
autoimmunity, diabetes and cardiovascular disease. However, outside nuclear receptors …

[HTML][HTML] AR and PI3K/AKT in prostate cancer: a tale of two interconnected pathways

E Tortorella, S Giantulli, A Sciarra, I Silvestri - International Journal of …, 2023 - mdpi.com
Prostate cancer (PCa) is the most common cancer in men. The androgen receptor (AR) has
a pivotal role in the pathogenesis and progression of PCa. Many therapies targeting AR …

[HTML][HTML] The MURAL collection of prostate cancer patient-derived xenografts enables discovery through preclinical models of uro-oncology

GP Risbridger, AK Clark, LH Porter, R Toivanen… - Nature …, 2021 - nature.com
Preclinical testing is a crucial step in evaluating cancer therapeutics. We aimed to establish
a significant resource of patient-derived xenografts (PDXs) of prostate cancer for rapid and …

[HTML][HTML] The catalytic subunit of DNA-PK regulates transcription and splicing of AR in advanced prostate cancer

B Adamson, N Brittain, L Walker… - The Journal of …, 2023 - Am Soc Clin Investig
Aberrant androgen receptor (AR) signaling drives prostate cancer (PC), and it is a key
therapeutic target. Although initially effective, the generation of alternatively spliced AR …

Characterization of HOXB13 expression patterns in localized and metastatic castration‐resistant prostate cancer

RA Patel, E Sayar, I Coleman… - The Journal of …, 2024 - Wiley Online Library
HOXB13 is a key lineage homeobox transcription factor that plays a critical role in the
differentiation of the prostate gland. Several studies have suggested that HOXB13 …

[HTML][HTML] Selective degradation of AR-V7 to overcome castration resistance of prostate cancer

Y Liu, C Yu, Z Shao, X Xia, T Hu, W Kong, X He… - Cell death & …, 2021 - nature.com
Androgen receptor splice variant 7 (AR-V7), a form of ligand-independent and constitutively
activating variant of androgen receptor (AR), is considered as the key driver to initiate …

Targeting key proteins involved in transcriptional regulation for cancer therapy: Current strategies and future prospective

H Pei, W Guo, Y Peng, H Xiong… - Medicinal Research …, 2022 - Wiley Online Library
The key proteins involved in transcriptional regulation play convergent roles in cellular
homeostasis, and their dysfunction mediates aberrant gene expressions that underline the …

[HTML][HTML] The crucial role of AR-V7 in enzalutamide-resistance of castration-resistant prostate cancer

Z Zheng, J Li, Y Liu, Z Shi, Z Xuan, K Yang, C Xu, Y Bai… - Cancers, 2022 - mdpi.com
Simple Summary Androgen receptor splice variant 7 (AR-V7) has always been considered a
key driver for triggering enzalutamide resistance of castration-resistant prostate cancer …

Two-in-one polymeric NO-donor prodrugs mediate precision and synergistic prostate cancer treatment

B Zhao, Y Wan, X Zhou, J Zhang, J Chen… - … Applied Materials & …, 2023 - ACS Publications
Chemotherapy predominates in clinical treatment of prostate cancer (PCa), while
irreversible resistance to chemotherapeutics and severe side effects hinder the therapeutic …

[HTML][HTML] From omics to multi-omics approaches for in-depth analysis of the molecular mechanisms of prostate cancer

E Nevedomskaya, B Haendler - International Journal of Molecular …, 2022 - mdpi.com
Cancer arises following alterations at different cellular levels, including genetic and
epigenetic modifications, transcription and translation dysregulation, as well as metabolic …