Evidence map›Paper›PMID 34296619›Full record

ArticleJournal of medicinal chemistry2021

First-in-Class Cyclic Temporin L Analogue: Design, Synthesis, and Antimicrobial Assessment.

Rosa Bellavita, Bruno Casciaro, Salvatore Di Maro, Diego Brancaccio, Alfonso Carotenuto, Annarita Falanga, Floriana Cappiello, Elisabetta Buommino, Stefania Galdiero, Ettore Novellino and 4 more

Open access · hybridAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.

0numbers the graph read from it
0cells of the map it votes in
23citing papers in PubMed
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

23 citing papers in PubMed, 37 citations in OpenAlex.

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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

14 authors at 6 institutions in 2 countries.

Rosa BellavitaDepartment of Pharmacy, University of Naples "Federico II", Naples 80131, Italy.ORCID 0000-0003-2163-5163
Bruno CasciaroCenter for Life Nano- & Neuro-Science, Fondazione Istituto Italiano di Tecnologia (IIT), Rome 00161, Italy.
Salvatore Di MaroDiSTABiF, University of Campania "Luigi Vanvitelli", Caserta 81100, Italy.ORCID 0000-0002-9286-4433
Diego BrancaccioDepartment of Pharmacy, University of Naples "Federico II", Naples 80131, Italy.
Alfonso CarotenutoDepartment of Pharmacy, University of Naples "Federico II", Naples 80131, Italy.ORCID 0000-0001-7532-5449
Annarita FalangaDepartment of Agricultural Sciences, University of Naples "Federico II", Portici 80055, Italy.
Floriana CappielloDepartment of Biochemical Sciences, Laboratory affiliated to Istituto Pasteur Italia-Fondazione Cenci Bolognetti, Sapienza University of Rome, Rome 00185, Italy.
Elisabetta BuomminoDepartment of Pharmacy, University of Naples "Federico II", Naples 80131, Italy.
Stefania GaldieroDepartment of Pharmacy, University of Naples "Federico II", Naples 80131, Italy.
Ettore NovellinoDepartment of Pharmacy, University of Naples "Federico II", Naples 80131, Italy.ORCID 0000-0002-2181-2142
Tom N GrossmannDepartment of Chemistry & Pharmaceutical Sciences, VU University Amsterdam, Amsterdam 1081 HZ, The Netherlands.ORCID 0000-0003-0179-4116
Maria Luisa MangoniDepartment of Biochemical Sciences, Laboratory affiliated to Istituto Pasteur Italia-Fondazione Cenci Bolognetti, Sapienza University of Rome, Rome 00185, Italy.ORCID 0000-0002-5991-5868
Francesco MerlinoDepartment of Pharmacy, University of Naples "Federico II", Naples 80131, Italy.ORCID 0000-0002-9607-229X
Paolo GriecoDepartment of Pharmacy, University of Naples "Federico II", Naples 80131, Italy.ORCID 0000-0002-6854-8123
University of Naples Federico II · ITIstituto Pasteur · ITFederico II University Hospital · ITItalian Institute of Technology · ITUniversity of Campania "Luigi Vanvitelli" · ITVrije Universiteit Amsterdam · NL

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

The pharmacodynamic and pharmacokinetic properties of bioactive peptides can be modulated by introducing conformational constraints such as intramolecular macrocyclizations, which can involve either the backbone and/or side chains. Herein, we aimed at increasing the α-helicity content of temporin L, an isoform of an intriguing class of linear antimicrobial peptides (AMPs), endowed with a wide antimicrobial spectrum, by the employment of diverse side-chain tethering strategies, including lactam, 1,4-substituted [1,2,3]-triazole, hydrocarbon, and disulfide linkers. Our approach resulted in a library of cyclic temporin L analogues that were biologically assessed for their antimicrobial, cytotoxic, and antibiofilm activities, leading to the development of the first-in-class cyclic peptide related to this AMP family. Our results allowed us to expand the knowledge regarding the relationship between the α-helical character of temporin derivatives and their biological activity, paving the way for the development of improved antibiotic cyclic AMP analogues.

Indexed as

Drug DesignAnimalsAnti-Bacterial AgentsAntimicrobial Cationic PeptidesAntineoplastic AgentsBacteriaCell Line, TumorCell ProliferationCell SurvivalDose-Response Relationship, DrugDrug Screening Assays, AntitumorHumansMicrobial Sensitivity TestsMolecular StructureRana temporariaStructure-Activity RelationshipAnti-Bacterial AgentsAntimicrobial Cationic PeptidesAntineoplastic Agentstemporin

Identifiers

PMID34296619
PMCPMC8389922
OpenAlexW3185011025

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.