Evidence map›Paper›PMID 34795861›Full record

ArticleACS medicinal chemistry letters2021

Influence of Linker Attachment Points on the Stability and Neosubstrate Degradation of Cereblon Ligands.

Aleša Bricelj, Yuen Lam Dora Ng, Dominic Ferber, Robert Kuchta, Sina Müller, Marius Monschke, Karl G Wagner, Jan Krönke, Izidor Sosič, Michael Gütschow and 1 more

Abstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.

0numbers the graph read from it
0cells of the map it votes in
25citing 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

25 citing papers in PubMed.

  1. Review
  2. Article
  3. First Generation Proteolysis Targeting Chimeras (PROTACs) for the Treatment of Progeria.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026
    Article
  4. Article
  5. A Facile Protocol for C(spChemMedChem · 2026
    Article
  6. Review
  7. FDA-approved kinase inhibitors in PROTAC design, development and synthesis.Journal of enzyme inhibition and medicinal chemistry · 2025
    Review
  8. Review
  9. Review
  10. Review
  11. Article
  12. Article
  13. Article
  14. Article
  15. Article
  16. Article
  17. Article
  18. Formation of C(spJournal of the American Chemical Society · 2023
    Article
  19. Review
  20. Beilstein journal of organic chemistry · 2023
    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

11 authors.

Aleša BriceljFaculty of Pharmacy, University of Ljubljana, Aškerčeva cesta 7, 1000 Ljubljana, Slovenia.
Yuen Lam Dora NgDepartment of Internal Medicine with Focus on Hematology, Oncology and Tumor Immunology, Charité, Hindenburgdamm 30, 12203 Berlin, Germany.
Dominic FerberPharmaceutical Institute, Department of Pharmaceutical & Medicinal Chemistry, University of Bonn, An der Immenburg 4, 53121 Bonn, Germany.
Robert KuchtaPharmaceutical Institute, Department of Pharmaceutical & Medicinal Chemistry, University of Bonn, An der Immenburg 4, 53121 Bonn, Germany.
Sina MüllerDepartment of Internal Medicine with Focus on Hematology, Oncology and Tumor Immunology, Charité, Hindenburgdamm 30, 12203 Berlin, Germany.
Marius MonschkePharmaceutical Institute, Pharmaceutical Technology, University of Bonn, Gerhard-Domagk-Straße 3, 53121 Bonn, Germany.
Karl G WagnerPharmaceutical Institute, Pharmaceutical Technology, University of Bonn, Gerhard-Domagk-Straße 3, 53121 Bonn, Germany.
Jan KrönkeDepartment of Internal Medicine with Focus on Hematology, Oncology and Tumor Immunology, Charité, Hindenburgdamm 30, 12203 Berlin, Germany.
Izidor SosičFaculty of Pharmacy, University of Ljubljana, Aškerčeva cesta 7, 1000 Ljubljana, Slovenia.ORCID https://orcid.org/0000-0002-3370-4587
Michael GütschowPharmaceutical Institute, Department of Pharmaceutical & Medicinal Chemistry, University of Bonn, An der Immenburg 4, 53121 Bonn, Germany.ORCID https://orcid.org/0000-0002-9376-7897
Christian SteinebachPharmaceutical Institute, Department of Pharmaceutical & Medicinal Chemistry, University of Bonn, An der Immenburg 4, 53121 Bonn, Germany.ORCID https://orcid.org/0000-0001-5638-1955

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Proteolysis targeting chimeras (PROTACs) hijacking the cereblon (CRBN) E3 ubiquitin ligase have emerged as a novel paradigm in drug development. Herein we found that linker attachment points of CRBN ligands highly affect their aqueous stability and neosubstrate degradation features. This work provides a blueprint for the assembly of future heterodimeric CRBN-based degraders with tailored properties.

Identifiers

PMID34795861
PMCPMC8591746

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.