Evidence map›Paper›PMID 37440686›Full record

ArticleJournal of medicinal chemistry2023

Innovative Strategy toward Mutant CFTR Rescue in Cystic Fibrosis: Design and Synthesis of Thiadiazole Inhibitors of the E3 Ligase RNF5.

Irene Brusa, Elvira Sondo, Emanuela Pesce, Valeria Tomati, Dario Gioia, Federico Falchi, Beatrice Balboni, Jose Antonio Ortega Martínez, Marina Veronesi, Elisa Romeo and 6 more

Open access · hybridAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.

0numbers the graph read from it
0cells of the map it votes in
7citing papers in PubMed
4.4field-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

7 citing papers in PubMed, 17 citations in OpenAlex.

  1. Review
  2. Article
  3. Article
  4. Targeting ubiquitination machinery in cystic fibrosis: Where do we stand?Cellular and molecular life sciences : CMLS · 2024
    Review
  5. The cross talk of ubiquitination and chemotherapy tolerance in colorectal cancer.Journal of cancer research and clinical oncology · 2024
    Review
  6. Article
  7. Review
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

16 authors at 3 institutions in 2 countries.

Irene BrusaDepartment of Pharmacy and Biotechnology, University of Bologna, 40126 Bologna, Italy.
Elvira SondoUOC Genetica Medica, IRCCS Istituto Giannina Gaslini, 16147 Genova, Italy.
Emanuela PesceUOC Genetica Medica, IRCCS Istituto Giannina Gaslini, 16147 Genova, Italy.
Valeria TomatiUOC Genetica Medica, IRCCS Istituto Giannina Gaslini, 16147 Genova, Italy.
Dario GioiaComputational & Chemical Biology, Istituto Italiano di Tecnologia, 16163 Genova, Italy.
Federico FalchiDepartment of Pharmacy and Biotechnology, University of Bologna, 40126 Bologna, Italy.ORCID 0000-0001-7385-649X
Beatrice BalboniDepartment of Pharmacy and Biotechnology, University of Bologna, 40126 Bologna, Italy.
Jose Antonio Ortega MartínezComputational & Chemical Biology, Istituto Italiano di Tecnologia, 16163 Genova, Italy.
Marina VeronesiStructural Biophysics and Translational Pharmacology Facility, Istituto Italiano di Tecnologia, 16163 Genova, Italy.
Elisa RomeoStructural Biophysics and Translational Pharmacology Facility, Istituto Italiano di Tecnologia, 16163 Genova, Italy.
Natasha MargaroliStructural Biophysics and Translational Pharmacology Facility, Istituto Italiano di Tecnologia, 16163 Genova, Italy.
Maurizio RecanatiniDepartment of Pharmacy and Biotechnology, University of Bologna, 40126 Bologna, Italy.ORCID 0000-0002-0039-0518
Stefania GirottoStructural Biophysics and Translational Pharmacology Facility, Istituto Italiano di Tecnologia, 16163 Genova, Italy.ORCID 0000-0002-0339-6675
Nicoletta PedemonteUOC Genetica Medica, IRCCS Istituto Giannina Gaslini, 16147 Genova, Italy.
Marinella RobertiDepartment of Pharmacy and Biotechnology, University of Bologna, 40126 Bologna, Italy.ORCID 0000-0001-9807-2886
Andrea CavalliDepartment of Pharmacy and Biotechnology, University of Bologna, 40126 Bologna, Italy.ORCID 0000-0002-6370-1176
Italian Institute of Technology · ITIstituto Giannina Gaslini · ITUniversity of Bologna · IT

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

In cystic fibrosis (CF), deletion of phenylalanine 508 (F508del) in the CF transmembrane conductance regulator (CFTR) is associated to misfolding and defective gating of the mutant channel. One of the most promising CF drug targets is the ubiquitin ligase RNF5, which promotes F508del-CFTR degradation. Recently, the first ever reported inhibitor of RNF5 was discovered, i.e., the 1,2,4-thiadiazol-5-ylidene

Indexed as

Cystic FibrosisThiadiazolesAminophenolsBenzodioxolesCystic Fibrosis Transmembrane Conductance RegulatorDNA-Binding ProteinsHumansMutationStructure-Activity RelationshipUbiquitin-Protein LigasesAminophenolsBenzodioxolesCFTR protein, humanCystic Fibrosis Transmembrane Conductance RegulatorDNA-Binding ProteinsRNF5 protein, humanThiadiazolesUbiquitin-Protein Ligases

Identifiers

PMID37440686
PMCPMC10388311
OpenAlexW4384155005

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.