Long-range gene regulation in hormone-dependent cancer
The human genome is organized into multiple structural layers, ranging from chromosome
territories to progressively smaller substructures, such as topologically associating domains …
territories to progressively smaller substructures, such as topologically associating domains …
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, 2023 - cell.com
Membraneless biomolecular condensates play important roles in both normal life activities
and responses to environmental stimuli in living organisms. Liquid‒liquid phase separation …
and responses to environmental stimuli in living organisms. Liquid‒liquid phase separation …
Fixation can change the appearance of phase separation in living cells
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 …
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 …
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 …
domain (AR-NTD), which were obtained by tethering AR-NTD antagonists and different …
[HTML][HTML] 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 …
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 …
driven by specific genomic regions known as super-enhancers (SEs). The robust …
Rational drug design targeting intrinsically disordered proteins
Intrinsically disordered proteins (IDPs) are proteins that perform important biological
functions without well‐defined structures under physiological conditions. IDPs can form …
functions without well‐defined structures under physiological conditions. IDPs can form …
Hormone-induced enhancer assembly requires an optimal level of hormone receptor multivalent interactions
Transcription factors (TFs) activate enhancers to drive cell-specific gene programs in
response to signals, but our understanding of enhancer assembly during signaling events is …
response to signals, but our understanding of enhancer assembly during signaling events is …
[HTML][HTML] Addressing the reciprocal crosstalk between the AR and the PI3K/AKT/mTOR signaling pathways for prostate cancer treatment
F Raith, DH O'Donovan, C Lemos, O Politz… - International Journal of …, 2023 - mdpi.com
The reduction in androgen synthesis and the blockade of the androgen receptor (AR)
function by chemical castration and AR signaling inhibitors represent the main treatment …
function by chemical castration and AR signaling inhibitors represent the main treatment …