| Title |
KX2-361: a novel orally bioavailable small molecule dual Src/tubulin inhibitor that provides long term survival in a murine model of glioblastoma
|
|---|---|
| Published in |
Journal of Neuro-Oncology, September 2018
|
| DOI | 10.1007/s11060-018-2992-4 |
| Pubmed ID | |
| Authors |
Michael J. Ciesielski, Yahao Bu, Stephan A. Munich, Paola Teegarden, Michael P. Smolinski, James L. Clements, Johnson Y. N. Lau, David G. Hangauer, Robert A. Fenstermaker |
| Abstract |
A major challenge to developing new therapies for patients with malignant brain tumors is that relatively few small molecule anticancer drugs penetrate the blood-brain barrier (BBB) well enough to provide therapeutically effective concentrations in brain tissue before drug exposure in non-CNS tissues results in unacceptable toxicity. KX2-361, a member of a novel family of compounds with Src-kinase and tubulin polymerization inhibitory activity, demonstrates good oral bioavailability and readily crosses the BBB in mice. The objective of this study was to investigate the activity of KX2-361 against human and murine glioma cells and assess its therapeutic effect in a syngeneic orthotopic model of glioblastoma. In addition to reducing the level of Src autophosphorylation in the GL261 murine glioblastoma cell line, KX2-361 binds directly to tubulin and disrupts microtubule architecture in glioma cells maintained in culture. The drug is active in vivo against orthotopic GL261 gliomas in syngeneic C57BL/6 mice. Long term survival is not observed in mice lacking an adaptive immune system, indicating that KX2-361 works in concert with the host immune system to control tumor growth and promote long-term survival in the GL261 glioma model. |
X Demographics
The data shown below were collected from the profiles of 10 X users who shared this research output. Click here to find out more about how the information was compiled.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| United States | 4 | 40% |
| Portugal | 1 | 10% |
| Unknown | 5 | 50% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Members of the public | 6 | 60% |
| Science communicators (journalists, bloggers, editors) | 3 | 30% |
| Scientists | 1 | 10% |
Mendeley readers
The data shown below were compiled from readership statistics for 11 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 11 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Ph. D. Student | 3 | 27% |
| Student > Bachelor | 3 | 27% |
| Researcher | 1 | 9% |
| Student > Doctoral Student | 1 | 9% |
| Unknown | 3 | 27% |
| Readers by discipline | Count | As % |
|---|---|---|
| Medicine and Dentistry | 4 | 36% |
| Biochemistry, Genetics and Molecular Biology | 2 | 18% |
| Immunology and Microbiology | 1 | 9% |
| Pharmacology, Toxicology and Pharmaceutical Science | 1 | 9% |
| Unknown | 3 | 27% |
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 20 July 2023.
All research outputs
#4,089,209
of 24,769,082 outputs
Outputs from Journal of Neuro-Oncology
#374
of 3,171 outputs
Outputs of similar age
#75,564
of 347,238 outputs
Outputs of similar age from Journal of Neuro-Oncology
#7
of 57 outputs
Altmetric has tracked 24,769,082 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 3,171 research outputs from this source. They receive a mean Attention Score of 4.4. This one has done well, scoring higher than 88% 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 347,238 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 78% of its contemporaries.
We're also able to compare this research output to 57 others from the same source and published within six weeks on either side of this one. This one has done well, scoring higher than 89% of its contemporaries.