Evidence map›Paper›PMID 29269255›Full record

ArticleBioorganic & medicinal chemistry2018

Immunoproteasome inhibition and bioactivity of thiasyrbactins.

Nicole A Bakas, Chad R Schultz, Lisette P Yco, Christopher C Roberts, Chia-En A Chang, André S Bachmann, Michael C Pirrung

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing papers in PubMed
–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

2 citing papers in PubMed.

  1. Article
  2. 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

7 authors.

Nicole A BakasDepartment of Chemistry, University of California, Riverside, CA 92521, USA.
Chad R SchultzDepartment of Pediatrics and Human Development, College of Human Medicine, Michigan State University, Grand Rapids, MI 49503, USA.
Lisette P YcoDepartment of Pediatrics and Human Development, College of Human Medicine, Michigan State University, Grand Rapids, MI 49503, USA.
Christopher C RobertsDepartment of Chemistry, University of California, Riverside, CA 92521, USA.
Chia-En A ChangDepartment of Chemistry, University of California, Riverside, CA 92521, USA.
André S BachmannDepartment of Pediatrics and Human Development, College of Human Medicine, Michigan State University, Grand Rapids, MI 49503, USA. Electronic address: andre.bachmann@hc.msu.edu.
Michael C PirrungDepartment of Chemistry, University of California, Riverside, CA 92521, USA; Department of Pharmaceutical Sciences, University of California, Irvine, CA 92697, USA. Electronic address: Michael.pirrung@ucr.edu.

Funding

Next-Generation GPU Computing Resource for Simulating Ligand-Protein Binding Kinetics/MechanismR01GM109045 · NIGMS · UNIVERSITY OF CALIFORNIA RIVERSIDE · PI CHANG, CHIA-EN · 2014 to 2023
$2.8M
NIGMS NIH HHS R01 GM109045
6 · The paper itself

Abstract

A family of macrodilactam natural products, the syrbactins, are known proteasome inhibitors. A small group of syrbactin analogs was prepared with a sulfur-for-carbon substitution to enhance synthetic accessibility and facilitate modulation of their solubility. Two of these compounds surprisingly proved to be inhibitors of the trypsin-like catalytic site, including of the immunoproteasome. Their bound and free conformations suggest special properties of the thiasyrbactin ring are responsible for this unusual preference, which may be exploited to develop drug-like immunoproteasome inhibitors. These compounds show greater selectivity than earlier compounds used to infer phenotypes of immunoproteasome inhibition, like ONX-0914.

Indexed as

Biological ProductsCell Line, TumorCell SurvivalDose-Response Relationship, DrugHumansLactamsMolecular StructureProteasome Endopeptidase ComplexProteasome InhibitorsStructure-Activity RelationshipBiological ProductsLactamsProteasome Endopeptidase ComplexProteasome InhibitorsConformational analysisMacrolactamNeuroblastomaProteasomeTrypsin-like site

Identifiers

PMID29269255
PMCPMC5920785

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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.