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HM71224, a novel Bruton’s tyrosine kinase inhibitor, suppresses B cell and monocyte activation and ameliorates arthritis in a mouse model: a potential drug for rheumatoid arthritis

Overview of attention for article published in Arthritis Research & Therapy, April 2016
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Mentioned by

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1 X user
peer_reviews
1 peer review site

Citations

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54 Dimensions

Readers on

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38 Mendeley
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2 CiteULike
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Title
HM71224, a novel Bruton’s tyrosine kinase inhibitor, suppresses B cell and monocyte activation and ameliorates arthritis in a mouse model: a potential drug for rheumatoid arthritis
Published in
Arthritis Research & Therapy, April 2016
DOI 10.1186/s13075-016-0988-z
Pubmed ID
Authors

Jin Kyun Park, Joo-Yun Byun, Ji Ah Park, Yu-Yon Kim, Ye Ji Lee, Jeong In Oh, Sun Young Jang, Young Hoon Kim, Yeong Wook Song, Jeewoong Son, Kwee Hyun Suh, Young-Mi Lee, Eun Bong Lee

Abstract

Bruton's tyrosine kinase (Btk) is critical for activation of B cells and myeloid cells. This study aimed to characterize the effects of HM71224, a novel Btk inhibitor, both in vitro and in a mouse model of experimental arthritis. The kinase inhibition profile of HM71224 was analyzed. The in vitro effects of HM71224 on B cells and monocytes were analyzed by examining phosphorylation of Btk and its downstream signaling molecules, along with cytokine production and osteoclast formation. The in vivo effects of HM71224 were investigated in a mouse model of collagen-induced arthritis (CIA). HM71224 irreversibly bound to and inhibited Btk (IC50 = 1.95 nM). The compound also inhibited the phosphorylation of Btk and its downstream molecules such as PLCγ2, in activated Ramos B lymphoma cells and primary human B cells in a dose-dependent manner. Furthermore, HM71224 effectively inhibited the production of tumor necrosis factor (TNF)-α, interleukin (IL)-6, and IL-1β by human monocytes, and osteoclast formation by human monocytes. Finally, HM71224 improved experimental arthritis and prevented joint destruction in a murine model of CIA. HM71224 inhibits Btk in B cells and monocytes and ameliorates experimental arthritis in a mouse model. Thus, HM71224 is a potential novel therapeutic agent for rheumatoid arthritis in humans.

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X Demographics

The data shown below were collected from the profile of 1 X user 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 38 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Netherlands 1 3%
Unknown 37 97%

Demographic breakdown

Readers by professional status Count As %
Researcher 11 29%
Other 4 11%
Student > Ph. D. Student 4 11%
Student > Bachelor 3 8%
Student > Doctoral Student 2 5%
Other 6 16%
Unknown 8 21%
Readers by discipline Count As %
Chemistry 8 21%
Medicine and Dentistry 6 16%
Biochemistry, Genetics and Molecular Biology 5 13%
Agricultural and Biological Sciences 4 11%
Pharmacology, Toxicology and Pharmaceutical Science 4 11%
Other 3 8%
Unknown 8 21%
Attention Score in Context

Attention Score in Context

This research output has an Altmetric Attention Score of 2. 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 06 June 2016.
All research outputs
#16,722,190
of 25,374,917 outputs
Outputs from Arthritis Research & Therapy
#2,443
of 3,381 outputs
Outputs of similar age
#182,537
of 313,520 outputs
Outputs of similar age from Arthritis Research & Therapy
#30
of 43 outputs
Altmetric has tracked 25,374,917 research outputs across all sources so far. This one is in the 32nd percentile – i.e., 32% of other outputs scored the same or lower than it.
So far Altmetric has tracked 3,381 research outputs from this source. They typically receive more attention than average, with a mean Attention Score of 9.2. This one is in the 25th percentile – i.e., 25% 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 313,520 tracked outputs that were published within six weeks on either side of this one in any source. This one is in the 38th percentile – i.e., 38% of its contemporaries scored the same or lower than it.
We're also able to compare this research output to 43 others from the same source and published within six weeks on either side of this one. This one is in the 23rd percentile – i.e., 23% of its contemporaries scored the same or lower than it.