Evidence map›Paper›PMID 24269123›Full record

ArticleBioorganic & medicinal chemistry letters2014

Evaluation of benzoic acid derivatives as sirtuin inhibitors.

Yi-Pei Chen, Chad C Catbagan, Jeannette T Bowler, Trevor Gokey, Natalie D M Goodwin, Anton B Guliaev, Weiming Wu, Taro Amagata

Open access · greenAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing papers in PubMed
0.2field-weighted citation impact, top 42% 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

3 citing papers in PubMed, 8 citations in OpenAlex.

  1. Article
  2. Article
  3. Engineering trypsin for inhibitor resistance.Protein science : a publication of the Protein Society · 2015
    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

8 authors at 1 institution in 1 country.

Yi-Pei ChenDepartment of Chemistry and Biochemistry, San Francisco State University, San Francisco, CA 94132, USA.
Chad C CatbaganDepartment of Chemistry and Biochemistry, San Francisco State University, San Francisco, CA 94132, USA.
Jeannette T BowlerDepartment of Chemistry and Biochemistry, San Francisco State University, San Francisco, CA 94132, USA.
Trevor GokeyDepartment of Chemistry and Biochemistry, San Francisco State University, San Francisco, CA 94132, USA.
Natalie D M GoodwinDepartment of Chemistry and Biochemistry, San Francisco State University, San Francisco, CA 94132, USA.
Anton B GuliaevDepartment of Chemistry and Biochemistry, San Francisco State University, San Francisco, CA 94132, USA.
Weiming WuDepartment of Chemistry and Biochemistry, San Francisco State University, San Francisco, CA 94132, USA.
Taro AmagataDepartment of Chemistry and Biochemistry, San Francisco State University, San Francisco, CA 94132, USA. Electronic address: amagata@sfsu.edu.
San Francisco State University · US

Funding

Student EnrichmentP20MD000544 · NIMHD · SAN FRANCISCO STATE UNIVERSITY · PI BAIRD, TEASTER T · 2003 to 2012
$9.4M
Design and Synthesis of Inhibitors for Orotidine-5'-Monophosphate DecarboxylaseSC1GM095419 · NIGMS · SAN FRANCISCO STATE UNIVERSITY · PI WU, WEIMING · 2012 to 2014
$685k
A Chemical Biology Approach for Discovery of HDAC InhibitorsSC2GM088057 · NIGMS · SAN FRANCISCO STATE UNIVERSITY · PI AMAGATA, TARO · 2010 to 2012
$449k
Metal inhibition of the base excision repair enzymesSC2GM095448 · NIGMS · SAN FRANCISCO STATE UNIVERSITY · PI GULIAEV, ANTON · 2011 to 2013
$440k
NIGMS NIH HHS SC1 GM095419NIGMS NIH HHS SC1GM095419NIGMS NIH HHS SC2 GM088057NIGMS NIH HHS SC2GM088057NIGMS NIH HHS SC2 GM095448NIGMS NIH HHS SC2GM095448NIMHD NIH HHS P20 MD000544NIMHD NIH HHS P20MD000544
6 · The paper itself

Abstract

Employing a genetically modified yeast strain as a screening tool, 4-dimethylaminobenzoic acid (5) was isolated from the marine sediment-derived Streptomyces sp. CP27-53 as a weak yeast sirtuin (Sir2p) inhibitor. Using this compound as a scaffold, a series of disubstituted benzene derivatives were evaluated to elucidate the structure activity relationships for Sir2p inhibition. The results suggested that 4-alkyl or 4-alkylaminobenzoic acid is the key structure motif for Sir2p inhibitory activity. The most potent Sir2p inhibitor, 4-tert-butylbenzoic acid (20), among the tested compounds in this study turned out to be a weak but selective SIRT1 inhibitor. The calculated binding free energies between the selected compounds and the catalytic domain of SIRT1 were well correlated to their measured SIRT1 inhibitory activities.

Indexed as

BenzoatesDose-Response Relationship, DrugHistone Deacetylase InhibitorsMolecular StructureSilent Information Regulator Proteins, Saccharomyces cerevisiaeSirtuin 2StreptomycesStructure-Activity RelationshipBenzoatesHistone Deacetylase InhibitorsSilent Information Regulator Proteins, Saccharomyces cerevisiaeSIR2 protein, S cerevisiaeSirtuin 24-Dimethylaminobenzoic acid4-tert-Butylbenzoic acidClass III HDAC inhibitorMarine-derived Streptomyces sp.Sirtuin

Identifiers

PMID24269123
PMCPMC3909564
OpenAlexW1969914408

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.