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Mendeley readers
Attention Score in Context
| Title |
The Aurora Kinase Inhibitor CCT137690 Downregulates MYCN and Sensitizes MYCN-Amplified Neuroblastoma In Vivo
|
|---|---|
| Published in |
Molecular Cancer Therapeutics, November 2011
|
| DOI | 10.1158/1535-7163.mct-11-0333 |
| Pubmed ID | |
| Authors |
Amir Faisal, Lynsey Vaughan, Vassilios Bavetsias, Chongbo Sun, Butrus Atrash, Sian Avery, Yann Jamin, Simon P. Robinson, Paul Workman, Julian Blagg, Florence I. Raynaud, Suzanne A. Eccles, Louis Chesler, Spiros Linardopoulos |
| Abstract |
Aurora kinases regulate key stages of mitosis including centrosome maturation, spindle assembly, chromosome segregation, and cytokinesis. Aurora A and B kinase overexpression has also been associated with various human cancers, and as such, they have been extensively studied as novel antimitotic drug targets. Here, we characterize the Aurora kinase inhibitor CCT137690, a highly selective, orally bioavailable imidazo[4,5-b]pyridine derivative that inhibits Aurora A and B kinases with low nanomolar IC(50) values in both biochemical and cellular assays and exhibits antiproliferative activity against a wide range of human solid tumor cell lines. CCT137690 efficiently inhibits histone H3 and transforming acidic coiled-coil 3 phosphorylation (Aurora B and Aurora A substrates, respectively) in HCT116 and HeLa cells. Continuous exposure of tumor cells to the inhibitor causes multipolar spindle formation, chromosome misalignment, polyploidy, and apoptosis. This is accompanied by p53/p21/BAX induction, thymidine kinase 1 downregulation, and PARP cleavage. Furthermore, CCT137690 treatment of MYCN-amplified neuroblastoma cell lines inhibits cell proliferation and decreases MYCN protein expression. Importantly, in a transgenic mouse model of neuroblastoma that overexpresses MYCN protein and is predisposed to spontaneous neuroblastoma formation, this compound significantly inhibits tumor growth. The potent preclinical activity of CCT137690 suggests that this inhibitor may benefit patients with MYCN-amplified neuroblastoma. |
Mendeley readers
The data shown below were compiled from readership statistics for 83 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| United Kingdom | 1 | 1% |
| Unknown | 82 | 99% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Ph. D. Student | 19 | 23% |
| Student > Master | 12 | 14% |
| Student > Bachelor | 11 | 13% |
| Researcher | 9 | 11% |
| Student > Doctoral Student | 6 | 7% |
| Other | 9 | 11% |
| Unknown | 17 | 20% |
| Readers by discipline | Count | As % |
|---|---|---|
| Biochemistry, Genetics and Molecular Biology | 24 | 29% |
| Medicine and Dentistry | 13 | 16% |
| Agricultural and Biological Sciences | 11 | 13% |
| Chemistry | 5 | 6% |
| Pharmacology, Toxicology and Pharmaceutical Science | 2 | 2% |
| Other | 7 | 8% |
| Unknown | 21 | 25% |
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 02 February 2023.
All research outputs
#3,360,651
of 23,269,984 outputs
Outputs from Molecular Cancer Therapeutics
#515
of 3,898 outputs
Outputs of similar age
#18,953
of 144,292 outputs
Outputs of similar age from Molecular Cancer Therapeutics
#11
of 64 outputs
Altmetric has tracked 23,269,984 research outputs across all sources so far. Compared to these this one has done well and is in the 84th percentile: it's in the top 25% of all research outputs ever tracked by Altmetric.
So far Altmetric has tracked 3,898 research outputs from this source. They typically receive more attention than average, with a mean Attention Score of 8.2. This one has done well, scoring higher than 82% 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 144,292 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 85% of its contemporaries.
We're also able to compare this research output to 64 others from the same source and published within six weeks on either side of this one. This one has done well, scoring higher than 75% of its contemporaries.