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An Amphotericin B Derivative Equally Potent to Amphotericin B and with Increased Safety

Overview of attention for article published in PLOS ONE, September 2016
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Title
An Amphotericin B Derivative Equally Potent to Amphotericin B and with Increased Safety
Published in
PLOS ONE, September 2016
DOI 10.1371/journal.pone.0162171
Pubmed ID
Authors

Armando Antillón, Alexander H. de Vries, Marcel Espinosa-Caballero, José Marcos Falcón-González, David Flores Romero, Javier González–Damián, Fabiola Eloísa Jiménez-Montejo, Angel León-Buitimea, Manuel López-Ortiz, Ricardo Magaña, Siewert J. Marrink, Rosmarbel Morales-Nava, Xavier Periole, Jorge Reyes-Esparza, Josué Rodríguez Lozada, Tania Minerva Santiago-Angelino, María Cristina Vargas González, Ignacio Regla, Mauricio Carrillo-Tripp, Mario Fernández-Zertuche, Lourdes Rodríguez-Fragoso, Iván Ortega-Blake

Abstract

Amphotericin B is the most potent antimycotic known to date. However due to its large collateral toxicity, its use, although long standing, had been limited. Many attempts have been made to produce derivatives with reduced collateral damage. The molecular mechanism of polyene has also been closely studied for this purpose and understanding it would contribute to the development of safe derivatives. Our study examined polyene action, including chemical synthesis, electrophysiology, pharmacology, toxicology and molecular dynamics. The results were used to support a novel Amphotericin B derivative with increased selectivity: L-histidine methyl ester of Amphotericin B. We found that this derivative has the same form of action as Amphotericin B, i.e. pore formation in the cell membrane. Its reduced dimerization in solution, when compared to Amphotericin B, is at least partially responsible for its increased selectivity. Here we also present the results of preclinical tests, which show that the derivative is just as potent as Amphotericin B and has increased safety.

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Mendeley readers

Mendeley readers

The data shown below were compiled from readership statistics for 41 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 41 100%

Demographic breakdown

Readers by professional status Count As %
Student > Ph. D. Student 9 22%
Student > Master 8 20%
Student > Bachelor 6 15%
Other 3 7%
Researcher 3 7%
Other 7 17%
Unknown 5 12%
Readers by discipline Count As %
Chemistry 12 29%
Pharmacology, Toxicology and Pharmaceutical Science 5 12%
Immunology and Microbiology 5 12%
Biochemistry, Genetics and Molecular Biology 4 10%
Agricultural and Biological Sciences 3 7%
Other 6 15%
Unknown 6 15%
Attention Score in Context

Attention Score in Context

This research output has an Altmetric Attention Score of 1. 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 10 October 2016.
All research outputs
#18,473,108
of 22,890,496 outputs
Outputs from PLOS ONE
#155,345
of 195,183 outputs
Outputs of similar age
#244,861
of 322,616 outputs
Outputs of similar age from PLOS ONE
#3,346
of 4,161 outputs
Altmetric has tracked 22,890,496 research outputs across all sources so far. This one is in the 11th percentile – i.e., 11% of other outputs scored the same or lower than it.
So far Altmetric has tracked 195,183 research outputs from this source. They typically receive a lot more attention than average, with a mean Attention Score of 15.1. This one is in the 10th percentile – i.e., 10% of its peers scored the same or lower than it.
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 322,616 tracked outputs that were published within six weeks on either side of this one in any source. This one is in the 13th percentile – i.e., 13% of its contemporaries scored the same or lower than it.
We're also able to compare this research output to 4,161 others from the same source and published within six weeks on either side of this one. This one is in the 10th percentile – i.e., 10% of its contemporaries scored the same or lower than it.