Evidence map›Paper›PMID 31000626›Full record

ArticleThe Journal of biological chemistry2019

Fluorescent indomethacin-dansyl conjugates utilize the membrane-binding domain of cyclooxygenase-2 to block the opening to the active site.

Shu Xu, Md Jashim Uddin, Surajit Banerjee, Kelsey Duggan, Joel Musee, James R Kiefer, Kebreab Ghebreselasie, Carol A Rouzer, Lawrence J Marnett

Open access · hybridAbstract read
In one paragraph

Article in The Journal of biological chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.

0numbers the graph read from it
0cells of the map it votes in
8citing papers in PubMed
2.7field-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

8 citing papers in PubMed, 24 citations in OpenAlex.

  1. Article
  2. Synergistic Combination ofAntioxidants (Basel, Switzerland) · 2023
    Article
  3. Article
  4. Article
  5. Targeted Detection of Cyclooxygenase-1 in Ovarian Cancer.ACS medicinal chemistry letters · 2020
    Article
  6. Review
  7. Article
  8. 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 2 institutions in 1 country.

Shu XuFrom the A. B. Hancock Jr. Memorial Laboratory for Cancer Research, Departments of Biochemistry, Chemistry, and Pharmacology, Vanderbilt Institute of Chemical Biology, Center in Molecular Toxicology, Vanderbilt-Ingram Cancer Center, Vanderbilt University School of Medicine, Nashville, Tennessee 37232.ORCID 0000-0002-6876-7991
Md Jashim UddinFrom the A. B. Hancock Jr. Memorial Laboratory for Cancer Research, Departments of Biochemistry, Chemistry, and Pharmacology, Vanderbilt Institute of Chemical Biology, Center in Molecular Toxicology, Vanderbilt-Ingram Cancer Center, Vanderbilt University School of Medicine, Nashville, Tennessee 37232.
Surajit BanerjeeDepartment of Chemistry and Chemical Biology, Cornell University, Ithaca, New York 14853.
Kelsey DugganFrom the A. B. Hancock Jr. Memorial Laboratory for Cancer Research, Departments of Biochemistry, Chemistry, and Pharmacology, Vanderbilt Institute of Chemical Biology, Center in Molecular Toxicology, Vanderbilt-Ingram Cancer Center, Vanderbilt University School of Medicine, Nashville, Tennessee 37232.
Joel MuseeFrom the A. B. Hancock Jr. Memorial Laboratory for Cancer Research, Departments of Biochemistry, Chemistry, and Pharmacology, Vanderbilt Institute of Chemical Biology, Center in Molecular Toxicology, Vanderbilt-Ingram Cancer Center, Vanderbilt University School of Medicine, Nashville, Tennessee 37232.
James R KieferGenentech, Inc., South San Francisco, California 94080.
Kebreab GhebreselasieFrom the A. B. Hancock Jr. Memorial Laboratory for Cancer Research, Departments of Biochemistry, Chemistry, and Pharmacology, Vanderbilt Institute of Chemical Biology, Center in Molecular Toxicology, Vanderbilt-Ingram Cancer Center, Vanderbilt University School of Medicine, Nashville, Tennessee 37232.
Carol A RouzerFrom the A. B. Hancock Jr. Memorial Laboratory for Cancer Research, Departments of Biochemistry, Chemistry, and Pharmacology, Vanderbilt Institute of Chemical Biology, Center in Molecular Toxicology, Vanderbilt-Ingram Cancer Center, Vanderbilt University School of Medicine, Nashville, Tennessee 37232.
Lawrence J MarnettFrom the A. B. Hancock Jr. Memorial Laboratory for Cancer Research, Departments of Biochemistry, Chemistry, and Pharmacology, Vanderbilt Institute of Chemical Biology, Center in Molecular Toxicology, Vanderbilt-Ingram Cancer Center, Vanderbilt University School of Medicine, Nashville, Tennessee 37232, larry.marnett@vanderbilt.edu.
Vanderbilt University · USArgonne National Laboratory · US

Funding

User Training and OutreachP30GM124165 · NIGMS · CORNELL UNIVERSITY · PI Nozomi Ando, J Christopher Fromme · 2018 to 2026
$34.2M
THE PHARMACOLOGY OF INHIBITORS OF HEME PROTEIN-CATALYZED LIPID PEROXIDATIONP50GM015431 · NIGMS · VANDERBILT UNIVERSITY · PI ROBERTS, II, L JACKSON · 1985 to 2010
$15.0M
Overall EvaluationP41GM103403 · NIGMS · CORNELL UNIVERSITY · PI EALICK, STEVEN E · 2012 to 2017
$14.3M
Therapeutic Modulation of Endothelial Cell TetrahydrobiopterinP01GM015431 · NIGMS · VANDERBILT UNIVERSITY · PI ROBERTS, JACKSON L · 2011 to 2015
$9.5M
FUNCTIONAL ANALYSIS OF CYCLOOXYGENASE 2R01CA089450 · NCI · VANDERBILT UNIVERSITY · PI MARNETT, LAWRENCE J. · 2001 to 2016
$6.3M
Pixel Array Detector for X-ray CrystallographyS10RR029205 · NCRR · CORNELL UNIVERSITY · PI EALICK, STEVEN E · 2010 to 2010
$1.8M
NCI NIH HHS R01 CA089450NCRR NIH HHS S10 RR029205NIGMS NIH HHS P01 GM015431NIGMS NIH HHS P30 GM124165NIGMS NIH HHS P41 GM103403NIGMS NIH HHS P50 GM015431
6 · The paper itself

Abstract

Many indomethacin amides and esters are cyclooxygenase-2 (COX-2)-selective inhibitors, providing a framework for the design of COX-2-targeted imaging and cancer chemotherapeutic agents. Although previous studies have suggested that the amide or ester moiety of these inhibitors binds in the lobby region, a spacious alcove within the enzyme's membrane-binding domain, structural details have been lacking. Here, we present observations on the crystal complexes of COX-2 with two indomethacin-dansyl conjugates (compounds 1 and 2) at 2.22-Å resolution. Both compounds are COX-2-selective inhibitors with IC

Indexed as

Catalytic DomainAnimalsCell MembraneCyclooxygenase 2Cyclooxygenase 2 InhibitorsDansyl CompoundsFluorescenceIndomethacinInhibitory Concentration 50KineticsMiceModels, MolecularTime FactorsCyclooxygenase 2Cyclooxygenase 2 InhibitorsDansyl CompoundsIndomethacinanticancer drugchemotherapycyclooxygenase (COX)enzyme kineticsenzyme structureinflammationprostaglandin endoperoxide synthaseprotein drug interactionX-ray crystallography

Identifiers

PMID31000626
PMCPMC6552414
OpenAlexW2936541063

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.