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A small molecule modulates Jumonji histone demethylase activity and selectively inhibits cancer growth

Overview of attention for article published in Nature Communications, June 2013
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About this Attention Score

  • In the top 25% of all research outputs scored by Altmetric
  • High Attention Score compared to outputs of the same age (83rd percentile)
  • Average Attention Score compared to outputs of the same age and source

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3 X users
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2 patents
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4 Facebook pages

Citations

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255 Dimensions

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217 Mendeley
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Title
A small molecule modulates Jumonji histone demethylase activity and selectively inhibits cancer growth
Published in
Nature Communications, June 2013
DOI 10.1038/ncomms3035
Pubmed ID
Authors

Lei Wang, Jianjun Chang, Diana Varghese, Michael Dellinger, Subodh Kumar, Anne M. Best, Julio Ruiz, Richard Bruick, Samuel Peña-Llopis, Junjie Xu, David J. Babinski, Doug E. Frantz, Rolf A. Brekken, Amy M. Quinn, Anton Simeonov, Johnny Easmon, Elisabeth D. Martinez

Abstract

The pharmacological inhibition of general transcriptional regulators has the potential to block growth through targeting multiple tumorigenic signalling pathways simultaneously. Here, using an innovative cell-based screen, we identify a structurally unique small molecule (named JIB-04) that specifically inhibits the activity of the Jumonji family of histone demethylases in vitro, in cancer cells, and in tumours in vivo. Unlike known inhibitors, JIB-04 is not a competitive inhibitor of α-ketoglutarate. In cancer, but not in patient-matched normal cells, JIB-04 alters a subset of transcriptional pathways and blocks viability. In mice, JIB-04 reduces tumour burden and prolongs survival. Importantly, we find that patients with breast tumours that overexpress Jumonji demethylases have significantly lower survival. Thus, JIB-04, a novel inhibitor of Jumonji demethylases in vitro and in vivo, constitutes a unique potential therapeutic and research tool against cancer, and validates the use of unbiased cellular screens to discover chemical modulators with disease relevance.

X Demographics

X Demographics

The data shown below were collected from the profiles of 3 X users who shared this research output. Click here to find out more about how the information was compiled.
Mendeley readers

Mendeley readers

The data shown below were compiled from readership statistics for 217 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
United Kingdom 6 3%
Brazil 1 <1%
Germany 1 <1%
China 1 <1%
United States 1 <1%
Unknown 207 95%

Demographic breakdown

Readers by professional status Count As %
Researcher 54 25%
Student > Ph. D. Student 45 21%
Student > Master 24 11%
Student > Bachelor 23 11%
Student > Doctoral Student 15 7%
Other 36 17%
Unknown 20 9%
Readers by discipline Count As %
Agricultural and Biological Sciences 65 30%
Biochemistry, Genetics and Molecular Biology 60 28%
Chemistry 38 18%
Medicine and Dentistry 8 4%
Neuroscience 6 3%
Other 13 6%
Unknown 27 12%
Attention Score in Context

Attention Score in Context

This research output has an Altmetric Attention Score of 9. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 24 February 2021.
All research outputs
#4,143,499
of 25,220,525 outputs
Outputs from Nature Communications
#35,170
of 55,790 outputs
Outputs of similar age
#33,194
of 202,800 outputs
Outputs of similar age from Nature Communications
#191
of 364 outputs
Altmetric has tracked 25,220,525 research outputs across all sources so far. Compared to these this one has done well and is in the 83rd percentile: it's in the top 25% of all research outputs ever tracked by Altmetric.
So far Altmetric has tracked 55,790 research outputs from this source. They typically receive a lot more attention than average, with a mean Attention Score of 55.8. This one is in the 36th percentile – i.e., 36% of its peers scored the same or lower than it.
Older research outputs will score higher simply because they've had more time to accumulate mentions. To account for age we can compare this Altmetric Attention Score to the 202,800 tracked outputs that were published within six weeks on either side of this one in any source. This one has done well, scoring higher than 83% of its contemporaries.
We're also able to compare this research output to 364 others from the same source and published within six weeks on either side of this one. This one is in the 47th percentile – i.e., 47% of its contemporaries scored the same or lower than it.