Evidence map›Paper›PMID 29867461›Full record

ReviewFrontiers in pharmacology2018

Small Molecule Modulators of RING-Type E3 Ligases: MDM and Cullin Families as Targets.

Emil Bulatov, Almaz Zagidullin, Aygul Valiullina, Regina Sayarova, Albert Rizvanov

Open access · goldAbstract readReview
In one paragraph

Review in Frontiers in pharmacology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.

0numbers the graph read from it
0cells of the map it votes in
21citing papers in PubMed
1.5field-weighted citation impact, top 18% 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

21 citing papers in PubMed, 30 citations in OpenAlex.

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  13. Emerging Strategies Targeting Catabolic Muscle Stress Relief.International journal of molecular sciences · 2020
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  17. Novel approaches for the rational design of PROTAC linkers.Exploration of targeted anti-tumor therapy · 2020
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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 2 institutions in 1 country.

Emil BulatovInstitute of Fundamental Medicine and Biology, Kazan Federal University, Kazan, Russia.
Almaz ZagidullinA.E. Arbuzov Institute of Organic and Physical Chemistry, Kazan Scientific Center, Russian Academy of Sciences, Kazan, Russia.
Aygul ValiullinaInstitute of Fundamental Medicine and Biology, Kazan Federal University, Kazan, Russia.
Regina SayarovaInstitute of Fundamental Medicine and Biology, Kazan Federal University, Kazan, Russia.
Albert RizvanovInstitute of Fundamental Medicine and Biology, Kazan Federal University, Kazan, Russia.
Kazan Federal University · RUA.E. Arbuzov Institute of Organic and Physical Chemistry · RU

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Ubiquitin-proteasome system (UPS) is a primary signaling pathway for regulation of intracellular protein levels. E3 ubiquitin ligases, substrate-specific members of the UPS, represent highly attractive protein targets for drug discovery. The importance of E3 ligases as prospective targets for small molecule modulation is reinforced by ever growing evidence of their role in cancer and other diseases. To date the number of potent compounds targeting E3 ligases remains rather low and their rational design constitutes a challenging task. To successfully address this problem one must take into consideration the multi-subunit nature of many E3 ligases that implies multiple druggable pockets and protein-protein interfaces. In this review, we briefly cover the current state of drug discovery in the field of RING-type E3 ligases with focus on MDM and Cullin families as targets. We also provide an overview of small molecule chimeras that induce RING-type E3-mediated proteasomal degradation of substrate proteins of interest.

Indexed as

Cullin familyinduced protein degradationMDM familyPROTACsRING-type E3 ligasessmall moleculesSNIPERsubiquitin–proteasome system

Identifiers

PMID29867461
PMCPMC5951978
OpenAlexW2799638258

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.