Evidence map›Paper›PMID 22607187›Full record

ArticleJournal of medicinal chemistry2012

Characterization and solubilization of pyrrole-imidazole polyamide aggregates.

Amanda E Hargrove, Jevgenij A Raskatov, Jordan L Meier, David C Montgomery, Peter B Dervan

Open access · bronzeAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.

0numbers the graph read from it
0cells of the map it votes in
20citing papers in PubMed
3.4field-weighted citation impact, top 8% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

20 citing papers in PubMed, 42 citations in OpenAlex.

  1. Article
  2. Review
  3. Article
  4. Review
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  6. Review
  7. Article
  8. Article
  9. Article
  10. Article
  11. Article
  12. Article
  13. Article
  14. Article
  15. Programmable DNA-binding small molecules.Bioorganic & medicinal chemistry · 2013
    Review
  16. Article
  17. Article
  18. Synthesis of cyclic Py-Im polyamide libraries.The Journal of organic chemistry · 2013
    Article
  19. Article
  20. Gene expression changes in a tumor xenograft by a pyrrole-imidazole polyamide.Proceedings of the National Academy of Sciences of the United States of America · 2012
    Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

5 authors at 1 institution in 1 country.

Amanda E HargroveCalifornia Institute of Technology, Division of Chemistry and Chemical Engineering, 1200 East California Boulevard, Pasadena, California 91125, United States.
Jevgenij A Raskatov
Jordan L Meier
David C Montgomery
Peter B Dervan
California Institute of Technology · US

Funding

PREDOCTORAL TRAINING IN BIOLOGY AND CHEMISTRYT32GM007616 · NIGMS · CALIFORNIA INSTITUTE OF TECHNOLOGY · PI STERNBERG, PAUL WARREN · 1985 to 2019
$22.9M
SITE SPECIFIC CHEMICAL METHODS FOR CLEAVING GENOMIC DNAR01GM051747 · NIGMS · CALIFORNIA INSTITUTE OF TECHNOLOGY · PI DERVAN, PETER B · 1995 to 2014
$6.2M
SEQUENCE SPECIFIC RECOGNITION OF DOUBLE HELICAL DNAR01GM027681 · NIGMS · CALIFORNIA INSTITUTE OF TECHNOLOGY · PI DERVAN, PETER B · 1985 to 2017
$4.5M
SEQUENCE SPECIFIC RECOGNITION OF DNAR37GM027681 · NIGMS · CALIFORNIA INSTITUTE OF TECHNOLOGY · PI DERVAN, PETER B · 1996 to 2005
$1.9M
DNA-binding polyamides as Hedgehog inhibitors in human carcinomaF32CA156833 · NCI · CALIFORNIA INSTITUTE OF TECHNOLOGY · PI HARGROVE, AMANDA E · 2011 to 2012
$97k
NCI NIH HHS 1F32CA156833NCI NIH HHS F32 CA156833NIGMS NIH HHS 5T32GM007616NIGMS NIH HHS GM27681NIGMS NIH HHS GM51747NIGMS NIH HHS R01 GM027681NIGMS NIH HHS R01 GM051747NIGMS NIH HHS R37 GM027681NIGMS NIH HHS T32 GM007616
6 · The paper itself

Abstract

To optimize the biological activity of pyrrole-imidazole polyamide DNA-binding molecules, we characterized the aggregation propensity of these compounds through dynamic light scattering and fractional solubility analysis. Nearly all studied polyamides were found to form measurable particles 50-500 nm in size under biologically relevant conditions, while HPLC-based analyses revealed solubility trends in both core sequences and peripheral substituents that did not correlate with overall ionic charge. The solubility of both hairpin and cyclic polyamides was increased upon addition of carbohydrate solubilizing agents, in particular, 2-hydroxypropyl-β-cyclodextrin (HpβCD). In mice, the use of HpβCD allowed for improved injection conditions and subsequent investigations of the availability of polyamides in mouse plasma to human cells. The results of these studies will influence the further design of Py-Im polyamides and facilitate their study in animal models.

Indexed as

2-Hydroxypropyl-beta-cyclodextrinAnimalsbeta-CyclodextrinsBiological AvailabilityCell Line, TumorChromatography, High Pressure LiquidHumansImidazolesInjections, IntraperitonealLightMiceMice, Inbred C57BLMolecular ConformationNylonsPyrrolesScattering, Radiation2-Hydroxypropyl-beta-cyclodextrinbeta-CyclodextrinsImidazolesNylonsPyrroles

Identifiers

PMID22607187
PMCPMC3375050
OpenAlexW2072522264

What OpenQuestion holds

Textmetadata
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.