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Stapled BIG3 helical peptide ERAP potentiates anti-tumour activity for breast cancer therapeutics

Overview of attention for article published in Scientific Reports, May 2017
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  • In the top 25% of all research outputs scored by Altmetric
  • High Attention Score compared to outputs of the same age (83rd percentile)
  • High Attention Score compared to outputs of the same age and source (80th percentile)

Mentioned by

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4 X users
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3 patents

Citations

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11 Dimensions

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33 Mendeley
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Title
Stapled BIG3 helical peptide ERAP potentiates anti-tumour activity for breast cancer therapeutics
Published in
Scientific Reports, May 2017
DOI 10.1038/s41598-017-01951-6
Pubmed ID
Authors

Tetsuro Yoshimaru, Keisuke Aihara, Masato Komatsu, Yosuke Matsushita, Yasumasa Okazaki, Shinya Toyokuni, Junko Honda, Mitsunori Sasa, Yasuo Miyoshi, Akira Otaka, Toyomasa Katagiri

Abstract

Estradiol (E2) and the oestrogen receptor-alpha (ERα) signalling pathway play pivotal roles in the proliferative activity of breast cancer cells. Recent findings show that the brefeldin A-inhibited guanine nucleotide-exchange protein 3-prohibitin 2 (BIG3-PHB2) complex plays a crucial role in E2/ERα signalling modulation in breast cancer cells. Moreover, specific inhibition of the BIG3-PHB2 interaction using the ERα activity-regulator synthetic peptide (ERAP: 165-177 amino acids), derived from α-helical BIG3 sequence, resulted in a significant anti-tumour effect. However, the duration of this effect was very short for viable clinical application. We developed the chemically modified ERAP using stapling methods (stapledERAP) to improve the duration of its antitumour effects. The stapledERAP specifically inhibited the BIG3-PHB2 interaction and exhibited long-lasting suppressive activity. Its intracellular localization without the membrane-permeable polyarginine sequence was possible via the formation of a stable α-helix structure by stapling. Tumour bearing-mice treated daily or weekly with stapledERAP effectively prevented the BIG3-PHB2 interaction, leading to complete regression of E2-dependent tumours in vivo. Most importantly, combination of stapledERAP with tamoxifen, fulvestrant, and everolimus caused synergistic inhibitory effects on growth of breast cancer cells. Our findings suggested that the stapled ERAP may be a promising anti-tumour drug to suppress luminal-type breast cancer growth.

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Mendeley readers

Mendeley readers

The data shown below were compiled from readership statistics for 33 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 33 100%

Demographic breakdown

Readers by professional status Count As %
Researcher 6 18%
Unspecified 2 6%
Other 2 6%
Student > Master 2 6%
Lecturer 2 6%
Other 7 21%
Unknown 12 36%
Readers by discipline Count As %
Chemistry 5 15%
Agricultural and Biological Sciences 5 15%
Pharmacology, Toxicology and Pharmaceutical Science 3 9%
Medicine and Dentistry 3 9%
Unspecified 2 6%
Other 5 15%
Unknown 10 30%
Attention Score in Context

Attention Score in Context

This research output has an Altmetric Attention Score of 11. 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 18 August 2022.
All research outputs
#2,956,624
of 24,285,692 outputs
Outputs from Scientific Reports
#25,033
of 131,992 outputs
Outputs of similar age
#52,675
of 313,909 outputs
Outputs of similar age from Scientific Reports
#776
of 4,008 outputs
Altmetric has tracked 24,285,692 research outputs across all sources so far. Compared to these this one has done well and is in the 87th percentile: it's in the top 25% of all research outputs ever tracked by Altmetric.
So far Altmetric has tracked 131,992 research outputs from this source. They typically receive a lot more attention than average, with a mean Attention Score of 18.6. This one has done well, scoring higher than 80% 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 313,909 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 83% of its contemporaries.
We're also able to compare this research output to 4,008 others from the same source and published within six weeks on either side of this one. This one has done well, scoring higher than 80% of its contemporaries.