Evidence map›Paper›PMID 24900384›Full record

ArticleACS medicinal chemistry letters2012

Antifungal spectrum, in vivo efficacy, and structure-activity relationship of ilicicolin h.

Sheo B Singh, Weiguo Liu, Xiaohua Li, Tom Chen, Ali Shafiee, Deborah Card, George Abruzzo, Amy Flattery, Charles Gill, John R Thompson and 7 more

Abstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 32 papers, 1 of them a synthesis that pooled it.

0numbers the graph read from it
0cells of the map it votes in
32citing papers in PubMed, 1 pooled it
–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

32 citing papers in PubMed, 1 synthesis or guideline pooled it.

  1. BioprospectingFrontiers in fungal biology · 2021
    Pooled it
  2. Article
  3. Article
  4. Article
  5. Review
  6. Review
  7. Article
  8. Genome Characteristics of the Endophytic FungusJournal of fungi (Basel, Switzerland) · 2024
    Article
  9. Article
  10. Review
  11. Article
  12. Review
  13. Article
  14. Review
  15. Article
  16. Review
  17. Therapeutic Approaches for CombatingCurrent drug targets · 2022
    Review
  18. Journal of fungi (Basel, Switzerland) · 2021
    Article
  19. Article
  20. Review
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

17 authors.

Sheo B SinghDepartments Medicinal Chemistry and Infectious Diseases, Merck Research Laboratories , Rahway, New Jersey 07065, United States.
Weiguo LiuDepartments Medicinal Chemistry and Infectious Diseases, Merck Research Laboratories , Rahway, New Jersey 07065, United States.
Xiaohua LiDepartments Medicinal Chemistry and Infectious Diseases, Merck Research Laboratories , Rahway, New Jersey 07065, United States.
Tom ChenDepartments Medicinal Chemistry and Infectious Diseases, Merck Research Laboratories , Rahway, New Jersey 07065, United States.
Ali ShafieeDepartments Medicinal Chemistry and Infectious Diseases, Merck Research Laboratories , Rahway, New Jersey 07065, United States.
Deborah CardDepartments Medicinal Chemistry and Infectious Diseases, Merck Research Laboratories , Rahway, New Jersey 07065, United States.
George AbruzzoDepartments Medicinal Chemistry and Infectious Diseases, Merck Research Laboratories , Rahway, New Jersey 07065, United States.
Amy FlatteryDepartments Medicinal Chemistry and Infectious Diseases, Merck Research Laboratories , Rahway, New Jersey 07065, United States.
Charles GillDepartments Medicinal Chemistry and Infectious Diseases, Merck Research Laboratories , Rahway, New Jersey 07065, United States.
John R ThompsonDepartments Medicinal Chemistry and Infectious Diseases, Merck Research Laboratories , Rahway, New Jersey 07065, United States.
Mark RosenbachDepartments Medicinal Chemistry and Infectious Diseases, Merck Research Laboratories , Rahway, New Jersey 07065, United States.
Sarah DreikornDepartments Medicinal Chemistry and Infectious Diseases, Merck Research Laboratories , Rahway, New Jersey 07065, United States.
Viktor HornakDepartments Medicinal Chemistry and Infectious Diseases, Merck Research Laboratories , Rahway, New Jersey 07065, United States.
Maria MeinzDepartments Medicinal Chemistry and Infectious Diseases, Merck Research Laboratories , Rahway, New Jersey 07065, United States.
Myra KurtzDepartments Medicinal Chemistry and Infectious Diseases, Merck Research Laboratories , Rahway, New Jersey 07065, United States.
Rosemarie KellyDepartments Medicinal Chemistry and Infectious Diseases, Merck Research Laboratories , Rahway, New Jersey 07065, United States.
Janet C OnishiDepartments Medicinal Chemistry and Infectious Diseases, Merck Research Laboratories , Rahway, New Jersey 07065, United States.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Ilicicolin H is a polyketide-nonribosomal peptide synthase (NRPS)-natural product isolated from Gliocadium roseum, which exhibits potent and broad spectrum antifungal activity, with sub-μg/mL MICs against Candida spp., Aspergillus fumigatus, and Cryptococcus spp. It showed a novel mode of action, potent inhibition (IC50 = 2-3 ng/mL) of the mitochondrial cytochrome bc1 reductase, and over 1000-fold selectivity relative to rat liver cytochrome bc1 reductase. Ilicicolin H exhibited in vivo efficacy in murine models of Candida albicans and Cryptococcus neoformans infections, but efficacy may have been limited by high plasma protein binding. Systematic structural modification of ilicicolin H was undertaken to understand the structural requirement for the antifungal activity. The details of the biological activity of ilicicolin H and structural modification of some of the key parts of the molecule and resulting activity of the derivatives are discussed. These data suggest that the β-keto group is critical for the antifungal activity.

Indexed as

antifungal activitybroad spectrumcytochrome bc1 reductase inhibitorGliocadium roseumilicicolin Hin vivo efficacy

Identifiers

PMID24900384
PMCPMC4025731

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.