Evidence map›Paper›PMID 25237759›Full record

ReviewOncotarget2014

Screening for E3-ubiquitin ligase inhibitors: challenges and opportunities.

Vivien Landré, Barak Rotblat, Sonia Melino, Francesca Bernassola, Gerry Melino

Open access · diamondAbstract readReview
In one paragraph

Review in Oncotarget, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 64 papers, 1 of them a synthesis that pooled it.

0numbers the graph read from it
0cells of the map it votes in
64citing papers in PubMed, 1 pooled it
4.1field-weighted citation impact, top 5% 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

64 citing papers in PubMed, 1 synthesis or guideline pooled it, 100 citations in OpenAlex.

  1. Pooled it
  2. SMURF2 in Anticancer Therapy: Dual Role in Carcinogenesis and Theranostics.International journal of molecular sciences · 2026
    Review
  3. Review
  4. Review
  5. Review
  6. Review
  7. Review
  8. Article
  9. Article
  10. Review
  11. Article
  12. Article
  13. Structural and functional validation of a highly specific Smurf2 inhibitor.Protein science : a publication of the Protein Society · 2024
    Article
  14. Review
  15. Article
  16. Review
  17. Article
  18. Article
  19. Review
  20. Article

4 more citing papers are in PubMed but not listed here.

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

5 authors at 3 institutions in 2 countries.

Vivien LandréMedical Research Council, Toxicology Unit, Leicester, UK.
Barak RotblatMedical Research Council, Toxicology Unit, Leicester, UK.
Sonia MelinoBiochemistry Laboratory, IDI-IRCCS, c/o Department of Experimental Medicine and Surgery, University of Rome "Tor Vergata", Rome, Italy.
Francesca BernassolaBiochemistry Laboratory, IDI-IRCCS, c/o Department of Experimental Medicine and Surgery, University of Rome "Tor Vergata", Rome, Italy.
Gerry MelinoMedical Research Council, Toxicology Unit, Leicester, UK. Biochemistry Laboratory, IDI-IRCCS, c/o Department of Experimental Medicine and Surgery, University of Rome "Tor Vergata", Rome, Italy.
Istituti di Ricovero e Cura a Carattere Scientifico · ITMedical Research Council · GBUniversity of Rome Tor Vergata · IT

Funding

Medical Research Council MC_U132670600
6 · The paper itself

Abstract

The ubiquitin proteasome system (UPS) plays a role in the regulation of most cellular pathways, and its deregulation has been implicated in a wide range of human pathologies that include cancer, neurodegenerative and immunological disorders and viral infections. Targeting the UPS by small molecular regulators thus provides an opportunity for the development of therapeutics for the treatment of several diseases. The proteasome inhibitor Bortezomib was approved for treatment of hematologic malignancies by the FDA in 2003, becoming the first drug targeting the ubiquitin proteasome system in the clinic. Development of drugs targeting specific components of the ubiquitin proteasome system, however, has lagged behind, mainly due to the complexity of the ubiquitination reaction and its outcomes. However, significant advances have been made in recent years in understanding the molecular nature of the ubiquitination system and the vast variety of cellular signals that it produces. Additionally, improvement of screening methods, both in vitro and in silico, have led to the discovery of a number of compounds targeting components of the ubiquitin proteasome system, and some of these have now entered clinical trials. Here, we discuss the current state of drug discovery targeting E3 ligases and the opportunities and challenges that it provides.

Indexed as

Drug DiscoveryMolecular Targeted TherapyAnimalsHumansProteasome Endopeptidase ComplexProteasome InhibitorsSignal TransductionUbiquitinationUbiquitin-Protein LigasesProteasome Endopeptidase ComplexProteasome InhibitorsUbiquitin-Protein Ligases

Identifiers

PMID25237759
PMCPMC4226663
OpenAlexW1794063461

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.