Modulating biomolecular condensates: a novel approach to drug discovery

DM Mitrea, M Mittasch, BF Gomes, IA Klein… - Nature Reviews Drug …, 2022 - nature.com
In the past decade, membraneless assemblies known as biomolecular condensates have
been reported to play key roles in many cellular functions by compartmentalizing specific …

Liquid–liquid phase separation in tumor biology

X Tong, R Tang, J Xu, W Wang, Y Zhao, X Yu… - Signal Transduction and …, 2022 - nature.com
Liquid–liquid phase separation (LLPS) is a novel principle for explaining the precise spatial
and temporal regulation in living cells. LLPS compartmentalizes proteins and nucleic acids …

Targeting androgen receptor phase separation to overcome antiandrogen resistance

J Xie, H He, W Kong, Z Li, Z Gao, D Xie, L Sun… - Nature Chemical …, 2022 - nature.com
Patients with castration-resistant prostate cancer inevitably acquire resistance to
antiandrogen therapies in part because of androgen receptor (AR) mutations or splice …

Molecular basis of small-molecule binding to α-synuclein

P Robustelli, A Ibanez-de-Opakua… - Journal of the …, 2022 - ACS Publications
Intrinsically disordered proteins (IDPs) are implicated in many human diseases. They have
generally not been amenable to conventional structure-based drug design, however …

Androgen receptor signaling in castration-resistant prostate cancer: a lesson in persistence

I Coutinho, TK Day, WD Tilley… - Endocrine-related …, 2016 - erc.bioscientifica.com
The androgen receptor (AR) signaling axis drives all stages of prostate cancer, including the
lethal, drug-resistant form of the disease termed castration-resistant prostate cancer (CRPC) …

Intrinsically disordered proteins and biomolecular condensates as drug targets

M Biesaga, M Frigolé-Vivas, X Salvatella - Current Opinion in Chemical …, 2021 - Elsevier
Intrinsically disordered domains represent attractive therapeutic targets because they play
key roles in cancer, as well as in neurodegenerative and infectious diseases. They are …

Long-range gene regulation in hormone-dependent cancer

TT Tettey, L Rinaldi, GL Hager - Nature Reviews Cancer, 2023 - nature.com
The human genome is organized into multiple structural layers, ranging from chromosome
territories to progressively smaller substructures, such as topologically associating domains …

Non-genomic actions of the androgen receptor in prostate cancer

JK Leung, MD Sadar - Frontiers in endocrinology, 2017 - frontiersin.org
Androgen receptor (AR) is a validated drug target for prostate cancer based on its role in
proliferation, survival, and metastases of prostate cancer cells. Unfortunately, despite recent …

[HTML][HTML] Androgen deprivation and immunotherapy for the treatment of prostate cancer

M Gamat, DG McNeel - Endocrine-related cancer, 2017 - erc.bioscientifica.com
Prostate cancer is the most common newly diagnosed malignancy in men, and the second
most common cause of cancer-related death in the United States. The primary treatment for …

Eukaryotic transcription factors: paradigms of protein intrinsic disorder

L Staby, C O'Shea, M Willemoës, F Theisen… - Biochemical …, 2017 - portlandpress.com
Gene-specific transcription factors (TFs) are key regulatory components of signaling
pathways, controlling, for example, cell growth, development, and stress responses. Their …