Evidence map›Paper›PMID 19877647›Full record

ArticleJournal of medicinal chemistry2009

Synthetic mRNA splicing modulator compounds with in vivo antitumor activity.

Chandraiah Lagisetti, Alan Pourpak, Tinopiwa Goronga, Qin Jiang, Xiaoli Cui, Judith Hyle, Jill M Lahti, Stephan W Morris, Thomas R Webb

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 37 papers.

0numbers the graph read from it
0cells of the map it votes in
37citing papers in PubMed
–field-weighted citation impact
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

37 citing papers in PubMed.

  1. Review
  2. Article
  3. Review
  4. Article
  5. Review
  6. Review
  7. New approaches to target RNA binding proteins.Current opinion in chemical biology · 2021
    Review
  8. Total Synthesis of Meayamycin andOrganic letters · 2020
    Article
  9. Destabilization of the human RED-SMU1 splicing complex as a basis for host-directed antiinfluenza strategy.Proceedings of the National Academy of Sciences of the United States of America · 2019
    Article
  10. Alternative Splicing as a Target for Cancer Treatment.International journal of molecular sciences · 2018
    Review
  11. A Challenging Pie to Splice: Drugging the Spliceosome.Angewandte Chemie (International ed. in English) · 2017
    Review
  12. Review
  13. Article
  14. Review
  15. Article
  16. Article
  17. Article
  18. Expression levels of SF3B3 correlate with prognosis and endocrine resistance in estrogen receptor-positive breast cancer.Modern pathology : an official journal of the United States and Canadian Academy of Pathology, Inc · 2015
    Article
  19. Article
  20. 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

9 authors.

Chandraiah LagisettiDepartment of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, MS 1000, 262 Danny Thomas Place, Memphis, Tennessee 38105, USA.
Alan Pourpak
Tinopiwa Goronga
Qin Jiang
Xiaoli Cui
Judith Hyle
Jill M Lahti
Stephan W Morris
Thomas R Webb

Funding

Viral Vector Technology (VVTSR)P30CA021765 · NCI · ST. JUDE CHILDREN'S RESEARCH HOSPITAL · PI CHARLES ROBERTS · 1985 to 2026
$166.9M
STRUCTURE/FUNCTION OF PITSLRE KINASESR01GM044088 · NIGMS · UNIVERSITY OF ALABAMA AT BIRMINGHAM · PI LAHTI, JILL M · 1991 to 2010
$2.2M
NCI NIH HHS P30 CA021765NIGMS NIH HHS 5R01GM044088
6 · The paper itself

Abstract

We report our progress on the development of new synthetic anticancer lead compounds that modulate the splicing of mRNA. We also report the synthesis and evaluation of new biologically active ester and carbamate analogues. Further, we describe initial animal studies demonstrating the antitumor efficacy of compound 5 in vivo. Additionally, we report the enantioselective and diastereospecific synthesis of a new 1,3-dioxane series of active analogues. We confirm that compound 5 inhibits the splicing of mRNA in cell-free nuclear extracts and in a cell-based dual-reporter mRNA splicing assay. In summary, we have developed totally synthetic novel spliceosome modulators as therapeutic lead compounds for a number of highly aggressive cancers. Future efforts will be directed toward the more complete optimization of these compounds as potential human therapeutics.

Indexed as

AnimalsAntineoplastic AgentsCarbamatesCell Line, TumorCell ProliferationDrug DesignEstersFemaleHumansInhibitory Concentration 50MiceModels, MolecularMolecular ConformationRNA, MessengerRNA SplicingSolubilityAntineoplastic AgentsCarbamatesEstersRNA, Messenger

Identifiers

PMID19877647
PMCPMC2801547

What OpenQuestion holds

Textmetadata
LicenceTDM
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.