These are preliminary reports that have not been peer-reviewed. They should not be regarded as conclusive, guide clinical practice/health-related behavior, or be reported in news media as established information. For more information, please see our FAQs.
Preprints are manuscripts made publicly available before they have been submitted for formal peer review and publication. They might contain new research findings or data. Preprints can be a draft or final version of an author's research but must not have been accepted for publication at the time of submission.
submitted on 20.04.2020 and posted on 23.04.2020by Huarui Cui, Anand Divakaran, Anil K. Pandey, Jorden
A. Johnson, huda zahid, zachary hoell, mikael ellingson, ke shi, Hideki Aihara, Daniel A. Harki, william pomerantz
This manuscript focuses on the structure-based design of selective inhibitors of the first bromodomain of BRD4. This manuscript uses describes organic synthesis to make inhibitors, and biophysical analysis to evaluate their inhibitor potency in competive inhibition assays (fluorescence anisotropy assays and AlphaScreen). Binding mode is evaluate from protein co-crystal structures. Cell activity is evaluated in cell viability assays, target engagement CETSA assays analyzed via western blot, and inhibition of Myc via western blot analysis.