Between Dec 19, 2024 and Jan 2, 2025, datasets can be submitted to DRUM but will not be processed until after the break. Staff will not be available to answer email during this period, and will not be able to provide DOIs until after Jan 2. If you are in need of a DOI during this period, consider Dryad or OpenICPSR. Submission responses to the UDC may also be delayed during this time.
 

Use of N,N-dimethyl ethylamine groups to target D144 of BRD4

Ellingson, Mikael
2020
Thumbnail Image

View/Download File

Ellingson_UROP_FinalReport_II.pdf (658.66 KB)

Persistent link to this item

https://hdl.handle.net/11299/216282
Statistics
View Statistics

Journal Title

Journal ISSN

Volume Title

Title

Use of N,N-dimethyl ethylamine groups to target D144 of BRD4

Authors

Published Date

2020

Publisher

Type

Report

Abstract

Though bromodomain and extraterminal (BET) family proteins are important epigenetic regulating proteins, high sequence similarity makes selective binding challenging. Molecules selective to the N-terminal bromodomain of the human bromodomain-containing protein, BRD4, have only been characterized recently and have spurred on therapeutic applications of BET inhibition. Here, the affinity of a BRD4-selective 1,4,5-trisubstituted imidazole scaffold is improved ~14-fold with the addition of a N,N-dimethyl ethylamine moiety as measured by a fluorescence polarization assay. This improvement is hypothesized to be due to electrostatic interactions with a nearby aspartic acid residue. Limitations of this characterization and conclusion are discussed

Keywords

Description

Faculty Advisor: William C.K. Pomerantz

Related to

Replaces

License

Collections

UMTC Undergraduate Research Presentations and Papers (UROP)

Series/Report Number

Funding information

This research was supported by the Undergraduate Research Opportunities Program (UROP).

Isbn identifier

Doi identifier

Previously Published Citation

Other identifiers

Suggested citation

Ellingson, Mikael. (2020). Use of N,N-dimethyl ethylamine groups to target D144 of BRD4. Retrieved from the University Digital Conservancy, https://hdl.handle.net/11299/216282.

Content distributed via the University Digital Conservancy may be subject to additional license and use restrictions applied by the depositor. By using these files, users agree to the Terms of Use. Materials in the UDC may contain content that is disturbing and/or harmful. For more information, please see our statement on harmful content in digital repositories.