Evidence map›Paper›PMID 27876319›Full record

ArticleBioorganic & medicinal chemistry letters2016

Development of a triazole class of highly potent Porcn inhibitors.

Lin You, Chengwei Zhang, Nageswari Yarravarapu, Lorraine Morlock, Xiaolei Wang, Lishu Zhang, Noelle S Williams, Lawrence Lum, Chuo Chen

Open access · greenAbstract read
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.

0numbers the graph read from it
0cells of the map it votes in
16citing papers in PubMed
1.2field-weighted citation impact, top 19% 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

16 citing papers in PubMed, 28 citations in OpenAlex.

  1. Structural basis for Porcupine inhibition.Communications chemistry · 2025
    Article
  2. Article
  3. Article
  4. Article
  5. Article
  6. Article
  7. Article
  8. Review
  9. Targeting the Wnt/β-catenin signaling pathway in cancer.Journal of hematology & oncology · 2020
    Review
  10. Review
  11. Review
  12. Article
  13. Review
  14. Review
  15. Article
  16. 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.

Lin YouDepartment of Biochemistry, UT Southwestern Medical Center, Dallas, TX 75390, USA.
Chengwei ZhangDepartment of Biochemistry, UT Southwestern Medical Center, Dallas, TX 75390, USA.
Nageswari YarravarapuDepartment of Cell Biology, UT Southwestern Medical Center, Dallas, TX 75390, USA.
Lorraine MorlockDepartment of Biochemistry, UT Southwestern Medical Center, Dallas, TX 75390, USA.
Xiaolei WangDepartment of Biochemistry, UT Southwestern Medical Center, Dallas, TX 75390, USA.
Lishu ZhangDepartment of Cell Biology, UT Southwestern Medical Center, Dallas, TX 75390, USA.
Noelle S WilliamsDepartment of Biochemistry, UT Southwestern Medical Center, Dallas, TX 75390, USA.
Lawrence LumDepartment of Cell Biology, UT Southwestern Medical Center, Dallas, TX 75390, USA.
Chuo ChenDepartment of Biochemistry, UT Southwestern Medical Center, Dallas, TX 75390, USA. Electronic address: chuo.chen@utsouthwestern.edu.
Southwestern Medical Center · USThe University of Texas Southwestern Medical Center · USSouthwestern Medical Center

Funding

UNIVERSITY OF TEXAS--SPORE IN LUNG CANCERP50CA070907 · NCI · UT SOUTHWESTERN MEDICAL CENTER · PI GIBBONS, DON LYNN · 1996 to 2024
$57.4M
Chemical disruption of Wnt-mediated signal transductionR01CA168761 · NCI · UT SOUTHWESTERN MEDICAL CENTER · PI KIM, JAMES · 2013 to 2017
$2.3M
Targeting vismodegib-resistant tumors using BH3 mimeticsR01CA196851 · NCI · UT SOUTHWESTERN MEDICAL CENTER · PI KIM, JAMES · 2016 to 2020
$1.7M
NCI NIH HHS P50 CA070907NCI NIH HHS R01 CA168761NCI NIH HHS R01 CA196851
6 · The paper itself

Abstract

The acyltransferase Porcupine (Porcn) is essential for the secretion of Wnt proteins which contribute to embryonic development, tissue regeneration, and tumorigenesis. We have previously discovered four molecular scaffolds harboring Porcn-inhibitory activity. Comparison of their structures led to the identification of a general scaffold that can be readily assembled by modular synthesis. We report herein the development of a triazole version of this new class of Porcn inhibitors. This study yielded IWP-O1, a Porcn inhibitor with an EC

Indexed as

AcyltransferasesDose-Response Relationship, DrugHumansMembrane ProteinsMolecular StructureStructure-Activity RelationshipTriazolesAcyltransferasesMembrane ProteinsPORCN protein, humanTriazolesBiaryl amidePorcupineTriarylTriazoleWnt signaling

Identifiers

PMID27876319
PMCPMC5142825
OpenAlexW2556494636

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.