Evidence map›Paper›PMID 33081023›Full record

ArticleMarine drugs2020

Design, Synthesis and In Vitro Experimental Validation of Novel TRPV4 Antagonists Inspired by Labdane Diterpenes.

Sarah Mazzotta, Gabriele Carullo, Aniello Schiano Moriello, Pietro Amodeo, Vincenzo Di Marzo, Margarita Vega-Holm, Rosa Maria Vitale, Francesca Aiello, Antonella Brizzi, Luciano De Petrocellis

Open access · goldAbstract read
In one paragraph

Article in Marine drugs, 2020. 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
1.5field-weighted citation impact, top 20% 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, 15 citations in OpenAlex.

  1. Article
  2. Labdane-Type Diterpenoids fromInternational journal of molecular sciences · 2024
    Article
  3. Review
  4. Article
  5. Review
  6. Article
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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

10 authors at 4 institutions in 3 countries.

Sarah MazzottaDepartment of Pharmacy, Health and Nutritional Sciences, DoE 2018-2022, University of Calabria, Edificio Polifunzionale, 87036 Rende (CS), Italy.ORCID 0000-0003-0029-7003
Gabriele CarulloDepartment of Pharmacy, Health and Nutritional Sciences, DoE 2018-2022, University of Calabria, Edificio Polifunzionale, 87036 Rende (CS), Italy.ORCID 0000-0002-1619-3295
Aniello Schiano MorielloEndocannabinoid Research Group (ERG), Institute of Biomolecular Chemistry, National Research Council (ICB-CNR), Via Campi Flegrei 34, 80078 Pozzuoli (NA), Italy.
Pietro AmodeoInstitute of Biomolecular Chemistry, National Research Council (ICB-CNR), Via Campi Flegrei 34, 80078 Pozzuoli (NA), Italy.ORCID 0000-0002-6439-7575
Vincenzo Di MarzoEndocannabinoid Research Group (ERG), Institute of Biomolecular Chemistry, National Research Council (ICB-CNR), Via Campi Flegrei 34, 80078 Pozzuoli (NA), Italy.
Margarita Vega-HolmDepartment of Organic and Medicinal Chemistry, Faculty of Pharmacy, University of Seville, Profesor García González 2, 41071 Seville, Spain.ORCID 0000-0003-2197-2004
Rosa Maria VitaleInstitute of Biomolecular Chemistry, National Research Council (ICB-CNR), Via Campi Flegrei 34, 80078 Pozzuoli (NA), Italy.ORCID 0000-0001-9243-1307
Francesca AielloDepartment of Pharmacy, Health and Nutritional Sciences, DoE 2018-2022, University of Calabria, Edificio Polifunzionale, 87036 Rende (CS), Italy.ORCID 0000-0001-6846-5582
Antonella BrizziDepartment of Biotechnology, Chemistry and Pharmacy, DoE 2018-2022, University of Siena, Via Aldo Moro 2, 53100 Siena, Italy.
Luciano De PetrocellisEndocannabinoid Research Group (ERG), Institute of Biomolecular Chemistry, National Research Council (ICB-CNR), Via Campi Flegrei 34, 80078 Pozzuoli (NA), Italy.ORCID 0000-0002-6131-0470
Istituto di Chimica Biomolecolare · ITUniversity of Calabria · ITUniversity of Siena · ITUniversidad de Sevilla · ES

Funding

Ministero dell'Istruzione, dell'Università e della Ricerca (Rome) Dipartimento di Eccellenza grant 2018-2022
6 · The paper itself

Abstract

Labdane diterpenes are widespread classes of natural compounds present in variety of marine and terrestrial organisms and plants. Many of them represents "natural libraries" of compounds with interesting biological activities due to differently functionalized drimane nucleus exploitable for potential pharmacological applications. The transient receptor potential channel subfamily V member 4 (TRPV4) channel has recently emerged as a pharmacological target for several respiratory diseases, including the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection. Inspired by the labdane-like bicyclic core, a series of homodrimane-derived esters and amides was designed and synthesized by modifying the flexible tail in position 1 of (+)-sclareolide, an oxidized derivative of the bioactive labdane-type diterpene sclareol. The potency and selectivity towards rTRPV4 and hTRPV1 receptors were assessed by calcium influx cellular assays. Molecular determinants critical for eliciting TRPV4 antagonism were identified by structure-activity relationships. Among the selective TRPV4 antagonists identified, compound

Indexed as

Drug DesignBetacoronavirusCoronavirus InfectionsCOVID-19DiterpenesGene Expression RegulationHEK293 CellsHumansInhibitory Concentration 50Molecular StructurePandemicsPneumonia, ViralSARS-CoV-2Structure-Activity RelationshipTRPV Cation ChannelsDiterpenesTRPV4 protein, humanTRPV Cation Channelsamides/estersbioactive diterpenesCOVID-19labdane scaffoldSARS-CoV-2sclareolidestructure-activity relationshipsTRPV4 channel

Identifiers

PMID33081023
PMCPMC7594054
OpenAlexW3093258005

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.