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Discovery of PG545: A Highly Potent and Simultaneous Inhibitor of Angiogenesis, Tumor Growth, and Metastasis

Overview of attention for article published in Journal of Medicinal Chemistry, April 2012
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About this Attention Score

  • In the top 25% of all research outputs scored by Altmetric
  • High Attention Score compared to outputs of the same age (90th percentile)
  • High Attention Score compared to outputs of the same age and source (90th percentile)

Mentioned by

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1 X user
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9 patents

Citations

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109 Dimensions

Readers on

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67 Mendeley
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Title
Discovery of PG545: A Highly Potent and Simultaneous Inhibitor of Angiogenesis, Tumor Growth, and Metastasis
Published in
Journal of Medicinal Chemistry, April 2012
DOI 10.1021/jm201708h
Pubmed ID
Authors

Vito Ferro, Ligong Liu, Ken D. Johnstone, Norbert Wimmer, Tomislav Karoli, Paul Handley, Jessica Rowley, Keith Dredge, Cai Ping Li, Edward Hammond, Kat Davis, Laura Sarimaa, Job Harenberg, Ian Bytheway

Abstract

Increasing the aglycone lipophilicity of a series of polysulfated oligosaccharide glycoside heparan sulfate (HS) mimetics via attachment of a steroid or long chain alkyl group resulted in compounds with significantly improved in vitro and ex vivo antiangiogenic activity. The compounds potently inhibited heparanase and HS-binding angiogenic growth factors and displayed improved antitumor and antimetastatic activity in vivo compared with the earlier series. Preliminary pharmacokinetic analyses also revealed significant increases in half-life following iv dosing, ultimately supporting less frequent dosing regimens in preclinical tumor models compared with other HS mimetics. The compounds also displayed only mild anticoagulant activity, a common side effect usually associated with HS mimetics. These efforts led to the identification of 3β-cholestanyl 2,3,4,6-tetra-O-sulfo-α-d-glucopyranosyl-(1→4)-2,3,6-tri-O-sulfo-α-d-glucopyranosyl-(1→4)-2,3,6-tri-O-sulfo-α-d-glucopyranosyl-(1→4)-2,3,6-tri-O-sulfo-β-d-glucopyranoside, tridecasodium salt (PG545, 18) as a clinical candidate. Compound 18 was recently evaluated in a phase I clinical trial in cancer patients.

X Demographics

X Demographics

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

Mendeley readers

The data shown below were compiled from readership statistics for 67 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
United Kingdom 1 1%
Germany 1 1%
Australia 1 1%
Unknown 64 96%

Demographic breakdown

Readers by professional status Count As %
Student > Ph. D. Student 20 30%
Researcher 13 19%
Other 5 7%
Student > Master 5 7%
Student > Bachelor 4 6%
Other 10 15%
Unknown 10 15%
Readers by discipline Count As %
Chemistry 23 34%
Biochemistry, Genetics and Molecular Biology 11 16%
Agricultural and Biological Sciences 5 7%
Medicine and Dentistry 5 7%
Immunology and Microbiology 3 4%
Other 7 10%
Unknown 13 19%
Attention Score in Context

Attention Score in Context

This research output has an Altmetric Attention Score of 13. 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 13 November 2023.
All research outputs
#2,749,219
of 25,002,811 outputs
Outputs from Journal of Medicinal Chemistry
#1,871
of 23,009 outputs
Outputs of similar age
#16,475
of 166,164 outputs
Outputs of similar age from Journal of Medicinal Chemistry
#17
of 171 outputs
Altmetric has tracked 25,002,811 research outputs across all sources so far. Compared to these this one has done well and is in the 88th percentile: it's in the top 25% of all research outputs ever tracked by Altmetric.
So far Altmetric has tracked 23,009 research outputs from this source. They typically receive a little more attention than average, with a mean Attention Score of 6.9. This one has done particularly well, scoring higher than 91% 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 166,164 tracked outputs that were published within six weeks on either side of this one in any source. This one has done particularly well, scoring higher than 90% of its contemporaries.
We're also able to compare this research output to 171 others from the same source and published within six weeks on either side of this one. This one has done particularly well, scoring higher than 90% of its contemporaries.