Results 121 to 130 of about 16,709 (213)
DDX21 Promotes Breast Cancer Growth and Metastasis via Stimulating RNAPII Elongation During Hypoxia
DDX21 triggers CDK9 release from the 7SK RNP complex. DDX21‐CDK9 binding to HIFs drives transcriptional reprogramming during hypoxia. DDX21 enhances breast cancer progression and metastasis. Elevated DDX21 expression correlates with poor prognosis in breast cancer patients.
Guangqiang Li +11 more
wiley +1 more source
1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain
The BRPF (bromodomain and PHD finger-containing) protein family are important scaffolding proteins for assembly of MYST histone acetyltransferase complexes.
Emmanuel H. Demont (1343475) +16 more
core +1 more source
This review illustrates the key mechanisms of osimertinib resistance in EGFR‑mutant NSCLC, including EGFR‑dependent mutations, bypass pathway activation, and SMARCA4‑mediated epigenetic regulation. We also summarize emerging targeted therapies and future perspectives to overcome EGFR‑TKI resistance.
Junfeng Guo, Qiuyuan Wen, Songqing Fan
wiley +1 more source
The transcription factor signal STAT5 is constitutively activated in a wide range of leukemias and lymphomas, and drives the expression of genes necessary for proliferation, survival, and self-renewal.
Wadleigh, Martha +10 more
core +1 more source
Multicellular organisms have evolved specialized mechanisms to control transcription in a spatial and temporal manner. Gene activation is tightly linked to histone acetylation on lysine residues that can be recognized by bromodomains.
Ina Theofel +9 more
doaj +1 more source
AlphaFold2‐Guided Cyclic Peptide Stabilizer Design to Target Protein–Protein Interactions
ABSTRACT The control and modulation of protein–protein interactions (PPIs) is of central importance for the majority of biological processes and most biomedical applications. Stabilization of PPIs, besides inhibition, is of growing pharmaceutical interest.
Niklas Halbwedl, Martin Zacharias
wiley +1 more source
Unusual backfolded binding poses of BAZ2A bromodomain binders
We identified BAZ2A‐binding compounds assuming a peculiar, almost enclosed, conformation. These molecules pose a basis for the development of potent BAZ2A macrocyclic inhibitors, as performed for other bromodomains.BAZ2A is a large multidomain protein overexpressed in aggressive prostate cancer, where it potentiates migration and invasion of other ...
Andrea Dalle Vedove +5 more
wiley +1 more source
While CAFs are produced as a result of education by cancer cells in non‐scirrhous gastric cancer, normal fibroblasts of scirrhous gastric cancer patients are already pre‐conditioned, forming a stromal field for scirrhous gastric cancer. ABSTRACT Scirrhous gastric cancer has aggressive clinical courses and is characterized by dominating cancer ...
Yoshimi Yasukawa +12 more
wiley +1 more source
The transcriptional adapter ADA2 interacts with the histone acetyltransferase GCN5 to regulate starch and storage protein content in wheat grains through histone acetylation. ADA2 undergoes phase separation and is modulated by GCN5, affecting histone acetyltransferase activity and gene transcription.
Xiaobang Zhang +15 more
wiley +1 more source
Bromodomain inhibitor treatment leads to overexpression of multiple kinases in cancer cells
The bromodomain and extraterminal (BET) family of proteins show altered expression across various cancers. The members of the bromodomain (BRD) family contain epigenetic reader domains that bind to acetylated lysine residues in both histone and non ...
Darshan S. Chandrashekar +7 more
doaj +1 more source

