Approximately 80% of breast cancers overexpress the kinase BRK/PTK6, which has various oncogenic roles in breast cancer cell proliferation, survival and migration. However, BRK inhibitors have yet to be explored as possible therapeutic tools. In this study, we employed a parallel compound-centric approach to discover a new class of pharmaceutical agents, exemplified by XMU-MP-2, as potent and selective BRK inhibitors. XMU-MP-2 exhibited target-specific inhibition of BRK kinase activity and disrupted signaling pathways mediated by this activity, thereby reducing proliferation in BRK-positive breast cancer cells. In mouse xenograft models, XMU-MP-2 repressed the growth of tumors driven by oncogenic BRK, including BRK-transformed Ba/F3 cells and BRK-positive breast cancer cells. Notably, XMU-MP-2 cooperated strongly with HER2 inhibitor or ER blockade to block breast cancer cell proliferation in vitro and in vivo. Overall, our findings offer a preclinical proof of concept for therapeutic targeting of the BRK kinase in breast cancer.
Pharmacology, Toxicology and Pharmaceutical Science
2
6%
Medicine and Dentistry
2
6%
Agricultural and Biological Sciences
1
3%
Other
1
3%
Unknown
12
36%
Attention Score in Context
Attention Score in Context
This research output has an Altmetric Attention Score of 8. 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 14 July 2026.
All research outputs
#6,547,205
of 34,089,221 outputs
Outputs from Cancer Research
#10,212
of 35,577 outputs
Outputs of similar age
#91,795
of 463,487 outputs
Outputs of similar age from Cancer Research
#67
of 228 outputs
Altmetric has tracked 34,089,221 research outputs across all sources so far. Compared to these this one has done well and is in the 80th percentile: it's in the top 25% of all research outputs ever tracked by Altmetric.
So far Altmetric has tracked 35,577 research outputs from this source. They typically receive more attention than average, with a mean Attention Score of 8.6. This one has gotten more attention than average, scoring higher than 70% 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 463,487 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 79% of its contemporaries.
We're also able to compare this research output to 228 others from the same source and published within six weeks on either side of this one. This one has gotten more attention than average, scoring higher than 70% of its contemporaries.
