Transcription regulation by biomolecular condensates

G Pei, H Lyons, P Li, BR Sabari - Nature Reviews Molecular Cell …, 2024 - nature.com
Biomolecular condensates regulate transcription by dynamically compartmentalizing the
transcription machinery. Classic models of transcription regulation focus on the recruitment …

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 …

Fixation can change the appearance of phase separation in living cells

S Irgen-Gioro, S Yoshida, V Walling, S Chong - elife, 2022 - elifesciences.org
Fixing cells with paraformaldehyde (PFA) is an essential step in numerous biological
techniques as it is thought to preserve a snapshot of biomolecular transactions in living cells …

Remodeling oncogenic transcriptomes by small molecules targeting NONO

SG Kathman, SJ Koo, GL Lindsey, HL Her… - Nature chemical …, 2023 - nature.com
Much of the human proteome is involved in mRNA homeostasis, but most RNA-binding
proteins lack chemical probes. Here we identify electrophilic small molecules that rapidly …

Discovery of BWA-522, a first-in-class and orally bioavailable PROTAC degrader of the androgen receptor targeting N-terminal domain for the treatment of prostate …

B Zhang, C Liu, Z Yang, S Zhang, X Hu… - Journal of medicinal …, 2023 - ACS Publications
We report small molecular PROTAC compounds targeting the androgen receptor N-terminal
domain (AR-NTD), which were obtained by tethering AR-NTD antagonists and different …

Liquid–liquid phase separation in plants: Advances and perspectives from model species to crops

Q Liu, W Liu, Y Niu, T Wang, J Dong - Plant Communications, 2024 - cell.com
Membraneless biomolecular condensates play important roles in both normal biological
activities and responses to environmental stimuli in living organisms. Liquid‒liquid phase …

Rational optimization of a transcription factor activation domain inhibitor

S Basu, P Martínez-Cristóbal, M Frigolé-Vivas… - Nature structural & …, 2023 - nature.com
Transcription factors are among the most attractive therapeutic targets but are considered
largely 'undruggable'in part due to the intrinsically disordered nature of their activation …

Dynamic phase separation of the androgen receptor and its coactivators key to regulate gene expression

F Zhang, M Biswas, S Massah, J Lee… - Nucleic Acids …, 2023 - academic.oup.com
Numerous cancers, including prostate cancer (PCa), are addicted to transcription programs
driven by specific genomic regions known as super-enhancers (SEs). The robust …

Phase separation of phospho-HDAC6 drives aberrant chromatin architecture in triple-negative breast cancer

B Lu, R Qiu, J Wei, L Wang, Q Zhang, M Li, X Zhan… - Nature Cancer, 2024 - nature.com
How dysregulated liquid–liquid phase separation (LLPS) contributes to the oncogenesis of
female triple-negative breast cancer (TNBC) remains unknown. Here we demonstrate that …

Rational drug design targeting intrinsically disordered proteins

H Wang, R Xiong, L Lai - Wiley Interdisciplinary Reviews …, 2023 - Wiley Online Library
Intrinsically disordered proteins (IDPs) are proteins that perform important biological
functions without well‐defined structures under physiological conditions. IDPs can form …