Evidence map›Paper›PMID 34500187›Full record

ArticleBioorganic & medicinal chemistry2021

Kinetic and structural investigations of novel inhibitors of human epithelial 15-lipoxygenase-2.

Wan-Chen Tsai, Nathan C Gilbert, Amanda Ohler, Michelle Armstrong, Steven Perry, Chakrapani Kalyanaraman, Adam Yasgar, Ganesha Rai, Anton Simeonov, Ajit Jadhav and 9 more

Open access · bronzeAbstract read
In one paragraph

Article in Bioorganic & medicinal chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.

0numbers the graph read from it
0cells of the map it votes in
21citing papers in PubMed
2.4field-weighted citation impact, top 11% 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

21 citing papers in PubMed, 26 citations in OpenAlex.

  1. Article
  2. Article
  3. Article
  4. Allosteric properties of mammalian ALOX15 orthologs.The Journal of biological chemistry · 2026
    Review
  5. Article
  6. Article
  7. Article
  8. Article
  9. Review
  10. Impact ofBiochemistry · 2024
    Article
  11. Article
  12. Article
  13. Article
  14. Article
  15. Article
  16. Discovering selective antiferroptotic inhibitors of the 15LOX/PEBP1 complex noninterfering with biosynthesis of lipid mediators.Proceedings of the National Academy of Sciences of the United States of America · 2023
    Article
  17. Biochemistry · 2023
    Article
  18. PROTACs in the Management of Prostate Cancer.Molecules (Basel, Switzerland) · 2023
    Review
  19. Interactions ofMembranes · 2023
    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

19 authors at 7 institutions in 1 country.

Wan-Chen TsaiDepartment of Chemistry and Biochemistry, University of California Santa Cruz, Santa Cruz, CA 95064, United States.
Nathan C GilbertDepartment of Biological Sciences, Louisiana State University, Baton Rouge, LA 70803, United States.
Amanda OhlerDepartment of Chemistry, East Carolina University, Greenville, NC 27858, United States.
Michelle ArmstrongDepartment of Chemistry and Biochemistry, University of California Santa Cruz, Santa Cruz, CA 95064, United States.
Steven PerryDepartment of Chemistry and Biochemistry, University of California Santa Cruz, Santa Cruz, CA 95064, United States.
Chakrapani KalyanaramanDepartment of Pharmaceutical Chemistry, School of Pharmacy, University of California San Francisco, San Francisco, CA 94158, United States.
Adam YasgarNational Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, MD 20850, United States.
Ganesha RaiNational Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, MD 20850, United States.
Anton SimeonovNational Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, MD 20850, United States.
Ajit JadhavNational Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, MD 20850, United States.
Melissa StandleyDepartment of Chemistry and Biochemistry, University of California Santa Cruz, Santa Cruz, CA 95064, United States.
Hsiau-Wei LeeDepartment of Chemistry and Biochemistry, University of California Santa Cruz, Santa Cruz, CA 95064, United States.
Phillip CrewsDepartment of Chemistry and Biochemistry, University of California Santa Cruz, Santa Cruz, CA 95064, United States.
Anthony T IavaroneDepartment of Chemistry and California Institute for Quantitative Biosciences (QB3), University of California Berkeley, Berkeley, CA 94720, United States.
Matthew P JacobsonDepartment of Pharmaceutical Chemistry, School of Pharmacy, University of California San Francisco, San Francisco, CA 94158, United States.
David B NeauCornell University, Northeastern Collaborative Access Team, Argonne National Laboratory, Argonne, IL, United States.
Adam R OffenbacherDepartment of Chemistry, East Carolina University, Greenville, NC 27858, United States.
Marcia NewcomerDepartment of Biological Sciences, Louisiana State University, Baton Rouge, LA 70803, United States.
Theodore R HolmanDepartment of Chemistry and Biochemistry, University of California Santa Cruz, Santa Cruz, CA 95064, United States. Electronic address: holman@ucsc.edu.
University of California, Santa Cruz · USNational Institutes of Health · USEast Carolina University · USLouisiana State University · USUniversity of California, San Francisco · USArgonne National Laboratory · USQB3 · US

Funding

User Training and OutreachP30GM124165 · NIGMS · CORNELL UNIVERSITY · PI Nozomi Ando, J Christopher Fromme · 2018 to 2026
$34.2M
Pregnane and Glycosides and Obesity/llya RaskinP50AT002776 · NCCIH · LSU PENNINGTON BIOMEDICAL RESEARCH CTR · PI RASKIN, ILYA · 2005 to 2019
$24.9M
Pixel Array Detector for Macromolecular CrystallographyS10OD021527 · OD · CORNELL UNIVERSITY · PI EALICK, STEVEN E · 2016 to 2016
$2.0M
12-HETrE regulation of plateletsR01GM105671 · NIGMS · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI HOLINSTAT, MICHAEL ALLAN · 2013 to 2017
$1.6M
The Structural Basis for Control of 5-Lipoxgenease ActivityR01HL107887 · NHLBI · LOUISIANA STATE UNIV A&M COL BATON ROUGE · PI NEWCOMER, MARCIA E. · 2011 to 2014
$1.4M
High Definition Ion Mobility SpectrometerS10OD020062 · OD · UNIVERSITY OF CALIFORNIA BERKELEY · PI WILLIAMS, EVAN R · 2015 to 2015
$590k
Conformational Flexibility of Lipoxygenases and its Role in Regulation and Substrate Acquisition.R15GM143724 · NIGMS · LOUISIANA STATE UNIV A&M COL BATON ROUGE · PI GILBERT, NATHANIEL · 2021 to 2021
$444k
High Throughput and Virtual Screening for Human 12-LO, 15-LO-1, and 15-LO-2 InhibR03MH081283 · NIMH · UNIVERSITY OF CALIFORNIA SANTA CRUZ · PI HOLMAN, THEODORE R · 2007 to 2007
$25k
NCCIH NIH HHS P50 AT002776NHLBI NIH HHS R01 HL107887NIGMS NIH HHS P30 GM124165NIGMS NIH HHS R01 GM105671NIGMS NIH HHS R15 GM143724NIH HHS S10 OD020062NIH HHS S10 OD021527NIMH NIH HHS R03 MH081283
6 · The paper itself

Abstract

Human epithelial 15-lipoxygenase-2 (h15-LOX-2, ALOX15B) is expressed in many tissues and has been implicated in atherosclerosis, cystic fibrosis and ferroptosis. However, there are few reported potent/selective inhibitors that are active ex vivo. In the current work, we report newly discovered molecules that are more potent and structurally distinct from our previous inhibitors, MLS000545091 and MLS000536924 (Jameson et al, PLoS One, 2014, 9, e104094), in that they contain a central imidazole ring, which is substituted at the 1-position with a phenyl moiety and with a benzylthio moiety at the 2-position. The initial three molecules were mixed-type, non-reductive inhibitors, with IC

Indexed as

Arachidonate 15-LipoxygenaseDose-Response Relationship, DrugHumansKineticsLipoxygenase InhibitorsMolecular StructureStructure-Activity RelationshipALOX15B protein, humanArachidonate 15-LipoxygenaseLipoxygenase InhibitorsCellular activityComputational dockingCrystallographyEnzymologyHydrogen-deuterium exchangeInhibitorlipoxygenaseMixed inhibition

Identifiers

PMID34500187
PMCPMC8785688
OpenAlexW3187494908

What OpenQuestion holds

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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.