Evidence map›Paper›PMID 24900212›Full record

ArticleACS medicinal chemistry letters2010

Targeting the c-Kit Promoter G-quadruplexes with 6-Substituted Indenoisoquinolines.

Mallesham Bejugam, Mekala Gunaratnam, Sebastian Müller, Deborah A Sanders, Sven Sewitz, Jonathan A Fletcher, Stephen Neidle, Shankar Balasubramanian

Erratum issuedOpen access · greenAbstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 26 papers.

0numbers the graph read from it
0cells of the map it votes in
26citing papers in PubMed
2.0field-weighted citation impact, top 14% 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

26 citing papers in PubMed, 68 citations in OpenAlex.

  1. Selective Recognition ofACS medicinal chemistry letters · 2024
    Article
  2. Review
  3. Review
  4. Article
  5. Article
  6. Article
  7. Polarizable Molecular Dynamics Simulations of TwoJournal of chemical theory and computation · 2020
    Article
  8. Article
  9. Article
  10. Article
  11. Article
  12. ACS medicinal chemistry letters · 2018
    Article
  13. Carbazole Derivatives' Binding to c-KIT G-Quadruplex DNA.Molecules (Basel, Switzerland) · 2018
    Article
  14. Article
  15. Article
  16. Article
  17. Article
  18. Article
  19. Targeting DNA G-quadruplexes with helical small molecules.Chembiochem : a European journal of chemical biology · 2014
    Article
  20. Article
4 · The record

Corrections and comments

  • Erratum issued
5 · Who and what money

Authors and funding

8 authors at 4 institutions in 2 countries.

Mallesham BejugamThe University Chemical Laboratory, University of Cambridge, Lensfield Road, Cambridge, CB2 1EW, United Kingdom.
Mekala GunaratnamCancer Research UK Biomolecular Structure Group, School of Pharmacy, University of London, 29-39 Brunswick Square, London WC19 1AX, United Kingdom.
Sebastian MüllerThe University Chemical Laboratory, University of Cambridge, Lensfield Road, Cambridge, CB2 1EW, United Kingdom.
Deborah A SandersThe University Chemical Laboratory, University of Cambridge, Lensfield Road, Cambridge, CB2 1EW, United Kingdom.
Sven SewitzThe University Chemical Laboratory, University of Cambridge, Lensfield Road, Cambridge, CB2 1EW, United Kingdom.
Jonathan A FletcherBrigham and Women's Hospital, 75 Francis Street, Boston, Massachusetts 02115.
Stephen NeidleCancer Research UK Biomolecular Structure Group, School of Pharmacy, University of London, 29-39 Brunswick Square, London WC19 1AX, United Kingdom.
Shankar BalasubramanianThe University Chemical Laboratory, University of Cambridge, Lensfield Road, Cambridge, CB2 1EW, United Kingdom ; School of Clinical Medicine, University of Cambridge, Cambridge CB2 0SP, United Kingdom ; Cancer Research UK Cambridge Research Institute, Li Ka Shing Centre, Cambridge CB2 0RE, United Kingdom.
University of Cambridge · GBCancer Research UK · GBBrigham and Women's Hospital · USUniversity of London · GB

Funding

Biotechnology and Biological Sciences Research Council BB/E012752/1
6 · The paper itself

Abstract

Herein, we demonstrate the design, synthesis, biophysical properties, and preliminary biological evaluation of 6-substituted indenoisoquinolines as a new class of G-quadruplex stabilizing small molecule ligands. We have synthesized 6-substituted indenoisoquinolines 1a-e in two steps from commercially available starting materials with excellent yields. The G-quadruplex stabilization potential of indenoisoquinolines 1a-e was evaluated by fluorescence resonance energy transfer-melting analysis, which showed that indenoisoquinolines show a high level of stabilization of various G-quadruplex DNA structures. Indenoisoquinolines demonstrated potent inhibition of cell growth in the GIST882 patient-derived gastrointestinal stromal tumor cell line, accompanied by inhibition of both c-Kit transcription and KIT oncoprotein levels.

Indexed as

c-kit regulationDNAinhibitionligandquadruplex

Identifiers

PMID24900212
PMCPMC4017300
OpenAlexW2026290591

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.