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A Novel Chemical Series for Inhibiting Bromodomain-containing Protein 4 (BRD4) for Treating Cancer
Case ID:
TAB-3575
Web Published:
12/6/2022
Description:
This technology includes the design, synthesis, and use of a novel chemical series for multiple treatments, including for treating cancer. A series of substituted bicyclic heteroaryl small molecules were found to be a potent inhibitor of bromodomain-containing protein 4 (BRD4) for multiple uses, including cancer. A BRD4 inhibitor is in a class of drugs known as BET inhibitors that are used broadly as anti-inflammatories and as anti-cancer agents. The chemical series exhibited less hepatocyte toxicity compared to existing treatments. For example, the series also identified N-methyl 2-pyridone 1s as a great replacement for dimethylisoxazole, an existing BET inhibitor.
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Direct Link:
https://nih.technologypublisher.com/tech/A_Novel_Chemical_Series_for_Inhibiti ng_Bromodomain-containing_Protein_4_(BRD4)_for_Treating_Cancer
Category(s):
Oncology
Therapeutics
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For Information, Contact:
Suryanarayana Vepa
Technology Licensing Specialist
NIH Technology Transfer
301-827-7181
sury.vepa@nih.gov
Inventors:
David Maloney
Shyh-Ming Yang
Ajit Jadhav
Daniel Urban
Makoto Yoshioka
Jeffrey Strovel
Keywords:
BICYCLIC
Brd4
Bromodomain-containing
Heteroaryl
Inhibitors
Protein
Substituted
VCXXXX
WKXXXX
XEXXXX
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