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Synthesis and Biological Investigation of (+)-JD1, an Organometallic BET Bromodomain Inhibitor

descriptionPublicationkeyboard_double_arrow_right Article 17 Dec 2019 United Kingdom English Publisher:American Chemical Society (ACS)Journal:Organometallics, volume 39, pages 408-416 (issn: 0276-7333, eissn: 1520-6041, Copyright policy )Funded by:WT | Institutional Strategic S..., UKRI | ZMYND8-regulation of MITF..., WT | A UK Hub to Catalyse Open... +4 projects
Authors: Storm Hassell-Hart; Andrew Runcie; Tobias Krojer; Jordan Doyle; Ella Lineham; Cory A. Ocasio; Brenno A. D. Neto; +16 Authors

doi: 10.1021/acs.organomet.9b00750

Synthesis and Biological Investigation of (+)-JD1, an Organometallic BET Bromodomain Inhibitor

Abstract

(+)-JD1, a rationally designed ferrocene analogue of the BET bromodomain (BRD) probe molecule (+)-JQ1, has been synthesized and evaluated in biophysical, cell-based assays as well as in pharmacokinetic studies. It displays nanomolar activity against BRD isoforms, and its cocrystal structure was determined in complex with the first bromodomain of BRD4 and compared with that of (+)-JQ1, a known BRD4 small-molecule probe. At 1 μM concentration, (+)-JD1 was able to inhibit c-Myc, a key driver in cancer and an indirect target of BRD4.

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Keywords

/dk/atira/pure/subjectarea/asjc/1600/1606, /dk/atira/pure/subjectarea/asjc/1600/1604, QD0901, /dk/atira/pure/subjectarea/asjc/1600/1605, name=Inorganic Chemistry, QD0411, 610, 540, name=Organic Chemistry, QD, name=Physical and Theoretical Chemistry, QD0241

  • BIP!
    Impact byBIP!
    citations
    This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
    		 8
    popularity
    This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
    		 Top 10%
    influence
    This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
    		 Average
    impulse
    This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
    		 Average
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citations
This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Citations provided by BIP!
popularity
This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
BIP!Popularity provided by BIP!
influence
This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Influence provided by BIP!
impulse
This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
BIP!Impulse provided by BIP!
8
Top 10%
Average
Average
Green
bronze
Related to Research communities
Knowmad Institut
UArctic
Cancer Research