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Identification of Novel Mycobacterial Inhibitors Against Mycobacterial Protein Kinase G

Overview of attention for article published in Frontiers in Microbiology, July 2018
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Title
Identification of Novel Mycobacterial Inhibitors Against Mycobacterial Protein Kinase G
Published in
Frontiers in Microbiology, July 2018
DOI 10.3389/fmicb.2018.01517
Pubmed ID
Authors

Yuichi Kanehiro, Haruaki Tomioka, Jean Pieters, Yutaka Tatano, Hyoji Kim, Hisashi Iizasa, Hironori Yoshiyama

Abstract

Protein kinase G (PknG) is a eukaryotic-like serine/threonine kinase that is expressed by Mycobacterium tuberculosis and promotes survival of mycobacteria in host macrophages by suppressing phagosome-lysosome fusion. Thus, compounds showing inhibitory activity against PknG are promising anti-mycobacterial agents. We therefore aimed to develop anti-mycobacterial agents by identifying new PknG inhibitors. A luciferase-based PknG kinase assay was used to screen potential inhibitors of PknG. We found that four compounds, namely AZD7762, R406, R406-free base, and CYC116, inhibited PknG activities. AZD7762, R406, and R406-free base promoted transfer of mycobacteria to lysosomes. These compounds also inhibited survival of M. bovis Bacillus Calmette-Guérin (BCG) inside human macrophages. Furthermore, R406 and R406-free base showed bactericidal activity against BCG in infected human macrophages without cytotoxicity. The PknG inhibitors identified in this study by the luciferase-based PknG kinase assay may be promising leads for the development of anti-mycobacterial agents.

X Demographics

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The data shown below were collected from the profiles of 4 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 42 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 42 100%

Demographic breakdown

Readers by professional status Count As %
Student > Master 7 17%
Student > Bachelor 7 17%
Student > Ph. D. Student 7 17%
Student > Doctoral Student 4 10%
Student > Postgraduate 2 5%
Other 4 10%
Unknown 11 26%
Readers by discipline Count As %
Biochemistry, Genetics and Molecular Biology 9 21%
Medicine and Dentistry 4 10%
Immunology and Microbiology 4 10%
Pharmacology, Toxicology and Pharmaceutical Science 2 5%
Business, Management and Accounting 2 5%
Other 8 19%
Unknown 13 31%
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 28 July 2018.
All research outputs
#13,621,195
of 23,094,276 outputs
Outputs from Frontiers in Microbiology
#10,682
of 25,264 outputs
Outputs of similar age
#169,214
of 326,948 outputs
Outputs of similar age from Frontiers in Microbiology
#362
of 746 outputs
Altmetric has tracked 23,094,276 research outputs across all sources so far. This one is in the 39th percentile – i.e., 39% of other outputs scored the same or lower than it.
So far Altmetric has tracked 25,264 research outputs from this source. They typically receive a little more attention than average, with a mean Attention Score of 6.4. This one has gotten more attention than average, scoring higher than 55% 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 326,948 tracked outputs that were published within six weeks on either side of this one in any source. This one is in the 46th percentile – i.e., 46% of its contemporaries scored the same or lower than it.
We're also able to compare this research output to 746 others from the same source and published within six weeks on either side of this one. This one is in the 49th percentile – i.e., 49% of its contemporaries scored the same or lower than it.