The Journal of clinical investigation, 130(4), 1782-1792 (2019-12-25)
Recent findings have shown that inhibitors targeting bromodomain and extraterminal domain (BET) proteins, such as the small molecule JQ1, are potent growth inhibitors of many cancers and hold promise for cancer therapy. However, some reports have also revealed that JQ1...
Targeting chromatin readers.
James LI and Frye SV
Clinical Pharmacology and Therapeutics, 93(4), 312-314 (2013)
Nature reviews. Drug discovery, 13(5), 337-356 (2014-04-23)
Lysine acetylation is a key mechanism that regulates chromatin structure; aberrant acetylation levels have been linked to the development of several diseases. Acetyl-lysine modifications create docking sites for bromodomains, which are small interaction modules found on diverse proteins, some of...
Epigenetic chemical probes.
Muller S and Brown PJ
Clinical Pharmacology and Therapeutics, 92(6), 689-693 (2012)
British journal of cancer, 123(4), 580-590 (2020-06-06)
Oral squamous cell carcinoma (OSCC) has increased morbidity, and its high metastatic potential affects patient survival. Bromodomain containing 4 (BRD4) is a chromatin protein that associates with acetylated histone lysines and facilitates transcription. BRD4 has been implicated in cell proliferation...
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