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Exploring the role of the α-carboxyphosphonate moiety in the HIV-RT activity of α-carboxy nucleoside phosphonates.

Overview of attention for article published in Organic and Biomolecular Chemistry, January 2016
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Title
Exploring the role of the α-carboxyphosphonate moiety in the HIV-RT activity of α-carboxy nucleoside phosphonates.
Published in
Organic and Biomolecular Chemistry, January 2016
DOI 10.1039/c5ob02507a
Pubmed ID
Authors

Mullins, Nicholas D, Maguire, Nuala M, Ford, Alan, Das, Kalyan, Arnold, Eddy, Balzarini, Jan, Maguire, Anita R

Abstract

As α-carboxy nucleoside phosphonates (α-CNPs) have demonstrated a novel mode of action of HIV-1 reverse transcriptase inhibition, structurally related derivatives were synthesized, namely the malonate , the unsaturated and saturated bisphosphonates and , respectively and the amide . These compounds were evaluated for inhibition of HIV-1 reverse transcriptase in cell-free assays. The importance of the α-carboxy phosphonoacetic acid moiety for achieving reverse transcriptase inhibition, without the need for prior phosphorylation, was confirmed. The malonate derivative was less active by two orders of magnitude than the original α-CNPs, while displaying the same pattern of kinetic behavior; interestingly the activity resides in the "L"-enantiomer of , as seen with the earlier series of α-CNPs. A crystal structure with an RT/DNA complex at 2.95 Å resolution revealed the binding of the "L"-enantiomer of , at the polymerase active site with a weaker metal ion chelation environment compared to (T-α-CNP) which may explain the lower inhibitory activity of .

Twitter Demographics

The data shown below were collected from the profile of 1 tweeter who shared this research output. Click here to find out more about how the information was compiled.

Mendeley readers

The data shown below were compiled from readership statistics for 14 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Russia 1 7%
Unknown 13 93%

Demographic breakdown

Readers by professional status Count As %
Researcher 4 29%
Student > Bachelor 3 21%
Professor 2 14%
Other 1 7%
Student > Ph. D. Student 1 7%
Other 3 21%
Readers by discipline Count As %
Chemistry 7 50%
Medicine and Dentistry 3 21%
Agricultural and Biological Sciences 1 7%
Unspecified 1 7%
Unknown 2 14%

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 29 January 2016.
All research outputs
#5,289,866
of 7,060,796 outputs
Outputs from Organic and Biomolecular Chemistry
#1,124
of 1,653 outputs
Outputs of similar age
#220,329
of 319,809 outputs
Outputs of similar age from Organic and Biomolecular Chemistry
#76
of 112 outputs
Altmetric has tracked 7,060,796 research outputs across all sources so far. This one is in the 14th percentile – i.e., 14% of other outputs scored the same or lower than it.
So far Altmetric has tracked 1,653 research outputs from this source. They receive a mean Attention Score of 2.9. This one is in the 16th percentile – i.e., 16% 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 319,809 tracked outputs that were published within six weeks on either side of this one in any source. This one is in the 17th percentile – i.e., 17% of its contemporaries scored the same or lower than it.
We're also able to compare this research output to 112 others from the same source and published within six weeks on either side of this one. This one is in the 24th percentile – i.e., 24% of its contemporaries scored the same or lower than it.