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The BTK Inhibitor ARQ 531 Targets Ibrutinib Resistant CLL and Richter's Transformation

Overview of attention for article published in Cancer Discovery, October 2018
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About this Attention Score

  • In the top 5% of all research outputs scored by Altmetric
  • High Attention Score compared to outputs of the same age (96th percentile)
  • High Attention Score compared to outputs of the same age and source (88th percentile)

Mentioned by

news
9 news outlets
twitter
23 X users
patent
2 patents
wikipedia
1 Wikipedia page

Citations

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112 Dimensions

Readers on

mendeley
78 Mendeley
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Title
The BTK Inhibitor ARQ 531 Targets Ibrutinib Resistant CLL and Richter's Transformation
Published in
Cancer Discovery, October 2018
DOI 10.1158/2159-8290.cd-17-1409
Pubmed ID
Authors

Sean David Reiff, Rose Mantel, Lisa L. Smith, Joseph T. Greene, Elizabeth M. Muhowski, Catherine A Fabian, Virginia M. Goettl, Minh Tran, Bonnie Harrington, Kerry A Rogers, Farrukh T Awan, Kami Maddocks, Leslie Andritsos, Amy M. Lehman, Deepa Sampath, Rosa Lapalombella, Sudharshan Eathiraj, Giovanni Abbadessa, Brian Schwartz, Amy Johnson, John C. Byrd, Jennifer A. Woyach

Abstract

Targeted inhibition of Bruton's tyrosine kinase (BTK) with the irreversible inhibitor ibrutinib has improved outcomes for patients with hematologic malignancies, including chronic lymphocytic leukemia (CLL). Here we describe preclinical investigations of ARQ 531, a potent, reversible inhibitor of BTK with additional activity against Src family kinases and kinases related to ERK signaling. We hypothesized that targeting additional kinases would improve global inhibition of signaling pathways, producing more robust responses. In vitro treatment of patient CLL cells with ARQ 531 decreases BTK-mediated functions including B cell receptor (BCR) signaling, viability, migration, CD40 and CD86 expression, and NF-κB gene transcription. In vivo, ARQ 531 was found to increase survival over ibrutinib in a murine Eμ-TCL1 engraftment model of CLL and a murine Eμ-MYC/TCL1 engraftment model resembling Richter's transformation. Additionally, ARQ 531 inhibits CLL cell survival and suppresses BCR-mediated activation of C481S BTK and PLCγ2 mutations which facilitate clinical resistance to ibrutinib.

X Demographics

X Demographics

The data shown below were collected from the profiles of 23 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 78 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 78 100%

Demographic breakdown

Readers by professional status Count As %
Student > Ph. D. Student 15 19%
Researcher 11 14%
Other 7 9%
Student > Bachelor 7 9%
Student > Master 4 5%
Other 8 10%
Unknown 26 33%
Readers by discipline Count As %
Biochemistry, Genetics and Molecular Biology 14 18%
Medicine and Dentistry 13 17%
Chemistry 9 12%
Pharmacology, Toxicology and Pharmaceutical Science 3 4%
Immunology and Microbiology 3 4%
Other 9 12%
Unknown 27 35%
Attention Score in Context

Attention Score in Context

This research output has an Altmetric Attention Score of 85. 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 20 November 2023.
All research outputs
#497,790
of 25,389,116 outputs
Outputs from Cancer Discovery
#253
of 4,054 outputs
Outputs of similar age
#10,804
of 351,193 outputs
Outputs of similar age from Cancer Discovery
#13
of 103 outputs
Altmetric has tracked 25,389,116 research outputs across all sources so far. Compared to these this one has done particularly well and is in the 98th percentile: it's in the top 5% of all research outputs ever tracked by Altmetric.
So far Altmetric has tracked 4,054 research outputs from this source. They typically receive a lot more attention than average, with a mean Attention Score of 21.5. This one has done particularly well, scoring higher than 93% of its peers.
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 351,193 tracked outputs that were published within six weeks on either side of this one in any source. This one has done particularly well, scoring higher than 96% of its contemporaries.
We're also able to compare this research output to 103 others from the same source and published within six weeks on either side of this one. This one has done well, scoring higher than 88% of its contemporaries.