Evidence map›Paper›PMID 27014922›Full record

ArticleJournal of medicinal chemistry2016

Repurposing the Clinically Efficacious Antifungal Agent Itraconazole as an Anticancer Chemotherapeutic.

Jennifer R Pace, Albert M DeBerardinis, Vibhavari Sail, Silvia K Tacheva-Grigorova, Kelly A Chan, Raymond Tran, Daniel S Raccuia, Robert J Wechsler-Reya, M Kyle Hadden

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.

0numbers the graph read from it
0cells of the map it votes in
29citing papers in PubMed
5.2field-weighted citation impact, top 4% 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

29 citing papers in PubMed, 55 citations in OpenAlex.

  1. Review
  2. Review
  3. Review
  4. Repurposing antifungal drugs for cancer therapy.Journal of advanced research · 2023
    Review
  5. Molecules (Basel, Switzerland) · 2022
    Article
  6. Review
  7. Itraconazole as a new pharmacotherapy method in haemangiomas.Postepy dermatologii i alergologii · 2021
    Article
  8. Review
  9. Review
  10. Article
  11. Article
  12. Article
  13. "Hedgehog pathway": a potential target of itraconazole in the treatment of cancer.Journal of cancer research and clinical oncology · 2020
    Review
  14. Article
  15. Review
  16. Article
  17. Article
  18. Article
  19. Review
  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 at 3 institutions in 1 country.

Jennifer R PaceDepartment of Pharmaceutical Sciences, University of Connecticut , 69 North Eagleville Road, Unit 3092, Storrs, Connecticut 06269-3092, United States.
Albert M DeBerardinisDepartment of Pharmaceutical Sciences, University of Connecticut , 69 North Eagleville Road, Unit 3092, Storrs, Connecticut 06269-3092, United States.
Vibhavari SailDepartment of Pharmaceutical Sciences, University of Connecticut , 69 North Eagleville Road, Unit 3092, Storrs, Connecticut 06269-3092, United States.
Silvia K Tacheva-GrigorovaTumor Initiation and Maintenance Program, NCI-Designated Cancer Center, Sanford Burnham Prebys Medical Discovery Institute , 2880 Torrey Pines Scenic Drive, La Jolla, California 92037, United States.
Kelly A ChanDepartment of Pharmaceutical Sciences, University of Connecticut , 69 North Eagleville Road, Unit 3092, Storrs, Connecticut 06269-3092, United States.
Raymond TranDepartment of Pharmaceutical Sciences, University of Connecticut , 69 North Eagleville Road, Unit 3092, Storrs, Connecticut 06269-3092, United States.
Daniel S RaccuiaDepartment of Pharmaceutical Sciences, University of Connecticut , 69 North Eagleville Road, Unit 3092, Storrs, Connecticut 06269-3092, United States.
Robert J Wechsler-ReyaTumor Initiation and Maintenance Program, NCI-Designated Cancer Center, Sanford Burnham Prebys Medical Discovery Institute , 2880 Torrey Pines Scenic Drive, La Jolla, California 92037, United States.
M Kyle HaddenDepartment of Pharmaceutical Sciences, University of Connecticut , 69 North Eagleville Road, Unit 3092, Storrs, Connecticut 06269-3092, United States.
University of Connecticut · USDiscovery Institute · USSanford Burnham Prebys Medical Discovery Institute · US

Funding

Itraconazole Analogues to Treat MedulloblastomaR01CA190617 · NCI · UNIVERSITY OF CONNECTICUT STORRS · PI HADDEN, MATTHEW KYLE · 2015 to 2019
$1.9M
NCI NIH HHS R01 CA190617
6 · The paper itself

Abstract

Itraconazole (ITZ) is an FDA-approved member of the triazole class of antifungal agents. Two recent drug repurposing screens identified ITZ as a promising anticancer chemotherapeutic that inhibits both the angiogenesis and hedgehog (Hh) signaling pathways. We have synthesized and evaluated first- and second-generation ITZ analogues for their anti-Hh and antiangiogenic activities to probe more fully the structural requirements for these anticancer properties. Our overall results suggest that the triazole functionality is required for ITZ-mediated inhibition of angiogenesis but that it is not essential for inhibition of Hh signaling. The synthesis and evaluation of stereochemically defined des-triazole ITZ analogues also provides key information as to the optimal configuration around the dioxolane ring of the ITZ scaffold. Finally, the results from our studies suggest that two distinct cellular mechanisms of action govern the anticancer properties of the ITZ scaffold.

Indexed as

AnimalsAntifungal AgentsAntineoplastic AgentsCell LineInhibitory Concentration 50ItraconazoleMiceMice, Inbred C3HRNA, MessengerZinc Finger Protein GLI1Antifungal AgentsAntineoplastic AgentsGli1 protein, mouseItraconazoleRNA, MessengerZinc Finger Protein GLI1

Identifiers

PMID27014922
PMCPMC5061146
OpenAlexW2336358768

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.