The structure and function of DNA G-quadruplexes
J Spiegel, S Adhikari, S Balasubramanian - Trends in Chemistry, 2020 - cell.com
Guanine-rich DNA sequences can fold into four-stranded, noncanonical secondary
structures called G-quadruplexes (G4s). G4s were initially considered a structural curiosity …
structures called G-quadruplexes (G4s). G4s were initially considered a structural curiosity …
The mechanisms behind the therapeutic activity of BET bromodomain inhibition
The bromodomain and extraterminal (BET) protein Brd4 recruits transcriptional regulatory
complexes to acetylated chromatin. While Brd4 is considered to be a general transcriptional …
complexes to acetylated chromatin. While Brd4 is considered to be a general transcriptional …
Phthalimide conjugation as a strategy for in vivo target protein degradation
The development of effective pharmacological inhibitors of multidomain scaffold proteins,
notably transcription factors, is a particularly challenging problem. In part, this is because …
notably transcription factors, is a particularly challenging problem. In part, this is because …
Selective small molecule induced degradation of the BET bromodomain protein BRD4
The Bromo-and Extra-Terminal (BET) proteins BRD2, BRD3, and BRD4 play important roles
in transcriptional regulation, epigenetics, and cancer and are the targets of pan-BET …
in transcriptional regulation, epigenetics, and cancer and are the targets of pan-BET …
BET bromodomain proteins function as master transcription elongation factors independent of CDK9 recruitment
Processive elongation of RNA Polymerase II from a proximal promoter paused state is a rate-
limiting event in human gene control. A small number of regulatory factors influence …
limiting event in human gene control. A small number of regulatory factors influence …
Response and resistance to BET bromodomain inhibitors in triple-negative breast cancer
Triple-negative breast cancer (TNBC) is a heterogeneous and clinically aggressive disease
for which there is no targeted therapy,,. BET bromodomain inhibitors, which have shown …
for which there is no targeted therapy,,. BET bromodomain inhibitors, which have shown …
NF-κB directs dynamic super enhancer formation in inflammation and atherogenesis
Proinflammatory stimuli elicit rapid transcriptional responses via transduced signals to
master regulatory transcription factors. To explore the role of chromatin-dependent signal …
master regulatory transcription factors. To explore the role of chromatin-dependent signal …
Gut bacterial isoamylamine promotes age-related cognitive dysfunction by promoting microglial cell death
Y Teng, J Mu, F Xu, X Zhang, MK Sriwastva, QM Liu… - Cell host & …, 2022 - cell.com
The intestinal microbiome releases a plethora of small molecules. Here, we show that the
Ruminococcaceae metabolite isoamylamine (IAA) is enriched in aged mice and elderly …
Ruminococcaceae metabolite isoamylamine (IAA) is enriched in aged mice and elderly …
Super-enhancer-driven transcriptional dependencies in cancer
S Sengupta, RE George - Trends in cancer, 2017 - cell.com
Transcriptional deregulation is one of the core tenets of cancer biology and is underpinned
by alterations in both protein-coding genes and noncoding regulatory elements. Large …
by alterations in both protein-coding genes and noncoding regulatory elements. Large …
Visualizing biologically active small molecules in cells using click chemistry
T Cañeque, S Müller, R Rodriguez - Nature Reviews Chemistry, 2018 - nature.com
Natural products and synthetic small molecules can be used to perturb, dissect and
manipulate biological processes, thereby providing the basis for drug development. Over the …
manipulate biological processes, thereby providing the basis for drug development. Over the …