Evidence map›Paper›PMID 30657666›Full record

ArticleJournal of medicinal chemistry2019

Structure-Based Design of Inhibitors Selective for Human Proteasome β2c or β2i Subunits.

Bo-Tao Xin, Eva M Huber, Gerjan de Bruin, Wolfgang Heinemeyer, Elmer Maurits, Christofer Espinal, Yimeng Du, Marissa Janssens, Emily S Weyburne, Alexei F Kisselev and 5 more

Open access · hybridAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.

0numbers the graph read from it
0cells of the map it votes in
18citing papers in PubMed
1.9field-weighted citation impact, top 14% 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

18 citing papers in PubMed, 36 citations in OpenAlex.

  1. Article
  2. Article
  3. Review
  4. Article
  5. Review
  6. Article
  7. Review
  8. Article
  9. Article
  10. Review
  11. Review
  12. Review
  13. Article
  14. Structure-Based Design of Fluorogenic Substrates Selective for Human Proteasome Subunits.Chembiochem : a European journal of chemical biology · 2020
    Article
  15. Article
  16. Article
  17. Preparative Method for Asymmetric Synthesis of (Molecules (Basel, Switzerland) · 2019
    Article
  18. 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

15 authors at 3 institutions in 3 countries.

Bo-Tao XinGorlaeus Laboratories , Leiden Institute of Chemistry and Netherlands Proteomics Centre , Einsteinweg 55 , 2333 CC Leiden , Netherlands.
Eva M HuberCenter for Integrated Protein Science at the Department Chemie, Lehrstuhl für Biochemie , Technische Universität München , 85748 Garching , Germany.
Gerjan de BruinGorlaeus Laboratories , Leiden Institute of Chemistry and Netherlands Proteomics Centre , Einsteinweg 55 , 2333 CC Leiden , Netherlands.
Wolfgang HeinemeyerCenter for Integrated Protein Science at the Department Chemie, Lehrstuhl für Biochemie , Technische Universität München , 85748 Garching , Germany.
Elmer MauritsGorlaeus Laboratories , Leiden Institute of Chemistry and Netherlands Proteomics Centre , Einsteinweg 55 , 2333 CC Leiden , Netherlands.
Christofer EspinalGorlaeus Laboratories , Leiden Institute of Chemistry and Netherlands Proteomics Centre , Einsteinweg 55 , 2333 CC Leiden , Netherlands.
Yimeng DuGorlaeus Laboratories , Leiden Institute of Chemistry and Netherlands Proteomics Centre , Einsteinweg 55 , 2333 CC Leiden , Netherlands.
Marissa JanssensGorlaeus Laboratories , Leiden Institute of Chemistry and Netherlands Proteomics Centre , Einsteinweg 55 , 2333 CC Leiden , Netherlands.
Emily S WeyburneDepartment of Molecular and Systems Biology and Norris Cotton Cancer Center , Geisel School of Medicine at Dartmouth , 1 Medical Centre Drive HB7936 , Lebanon , New Hampshire 03756 , United States.
Alexei F KisselevDepartment of Molecular and Systems Biology and Norris Cotton Cancer Center , Geisel School of Medicine at Dartmouth , 1 Medical Centre Drive HB7936 , Lebanon , New Hampshire 03756 , United States.
Bogdan I FloreaGorlaeus Laboratories , Leiden Institute of Chemistry and Netherlands Proteomics Centre , Einsteinweg 55 , 2333 CC Leiden , Netherlands.
Christoph DriessenDepartment of Hematology and Oncology , Kantonsspital St. Gallen , 9007 St. Gallen , Switzerland.
Gijsbert A van der MarelGorlaeus Laboratories , Leiden Institute of Chemistry and Netherlands Proteomics Centre , Einsteinweg 55 , 2333 CC Leiden , Netherlands.
Michael GrollCenter for Integrated Protein Science at the Department Chemie, Lehrstuhl für Biochemie , Technische Universität München , 85748 Garching , Germany.ORCID 0000-0002-1660-340X
Herman S OverkleeftGorlaeus Laboratories , Leiden Institute of Chemistry and Netherlands Proteomics Centre , Einsteinweg 55 , 2333 CC Leiden , Netherlands.ORCID 0000-0001-6976-7005
Center for Integrated Protein Science Munich · DEDartmouth College · USKantonsspital St. Gallen · CH

Funding

Proteasome inhibitors for the treatment of solid tumorsR01CA213223 · NCI · AUBURN UNIVERSITY AT AUBURN · PI KISSELEV, ALEXEI · 2017 to 2021
$1.8M
NCI NIH HHS R01 CA213223
6 · The paper itself

Abstract

Subunit-selective proteasome inhibitors are valuable tools to assess the biological and medicinal relevance of individual proteasome active sites. Whereas the inhibitors for the β1c, β1i, β5c, and β5i subunits exploit the differences in the substrate-binding channels identified by X-ray crystallography, compounds selectively targeting β2c or β2i could not yet be rationally designed because of the high structural similarity of these two subunits. Here, we report the development, chemical synthesis, and biological screening of a compound library that led to the identification of the β2c- and β2i-selective compounds LU-002c (4; IC

Indexed as

AnimalsCatalytic DomainCell Line, TumorCrystallography, X-RayDrug DesignHumansMiceMutationOligopeptidesPeptide LibraryProteasome Endopeptidase ComplexProteasome InhibitorsProtein BindingProtein EngineeringProtein SubunitsRecombinant Fusion ProteinsOligopeptidesPeptide LibraryProteasome Endopeptidase ComplexProteasome InhibitorsProtein SubunitsPSMB2 protein, humanRecombinant Fusion ProteinsSaccharomyces cerevisiae ProteinsSmall Molecule Libraries

Identifiers

PMID30657666
PMCPMC6378654
OpenAlexW2908586769

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.