Evidence map›Paper›PMID 28419419›Full record

ArticleBritish journal of pharmacology2017

The isoprenoid derivative N

Elena Ciaglia, Manuela Grimaldi, Mario Abate, Mario Scrima, Manuela Rodriquez, Chiara Laezza, Roberta Ranieri, Simona Pisanti, Pierangela Ciuffreda, Clementina Manera and 3 more

Open access · bronzeAbstract read
In one paragraph

Article in British journal of pharmacology, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.

0numbers the graph read from it
0cells of the map it votes in
11citing papers in PubMed
1.0field-weighted citation impact, top 25% 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

11 citing papers in PubMed, 16 citations in OpenAlex.

  1. Mangostanin, a Xanthone Derived fromPharmaceuticals (Basel, Switzerland) · 2022
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  11. The isoprenoid derivative NBritish journal of pharmacology · 2017
    Article
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

13 authors at 4 institutions in 1 country.

Elena CiagliaDepartment of Medicine, Surgery and Dentistry "Scuola Medica Salernitana", University of Salerno, Baronissi, Salerno, Italy.
Manuela GrimaldiDepartment of Pharmacy, University of Salerno, Fisciano, Salerno, Italy.
Mario AbateDepartment of Medicine, Surgery and Dentistry "Scuola Medica Salernitana", University of Salerno, Baronissi, Salerno, Italy.
Mario ScrimaDepartment of Pharmacy, University of Salerno, Fisciano, Salerno, Italy.
Manuela RodriquezDepartment of Pharmacy, University of Salerno, Fisciano, Salerno, Italy.
Chiara LaezzaDepartment of Biology and Cellular and Molecular Pathology, University of Naples Federico II, Naples, Italy.
Roberta RanieriDepartment of Medicine, Surgery and Dentistry "Scuola Medica Salernitana", University of Salerno, Baronissi, Salerno, Italy.
Simona PisantiDepartment of Medicine, Surgery and Dentistry "Scuola Medica Salernitana", University of Salerno, Baronissi, Salerno, Italy.
Pierangela CiuffredaDipartimento di Scienze Biomediche e Cliniche "Luigi Sacco", Università degli Studi di Milano, Milan, Italy.
Clementina ManeraDepartment of Pharmacy, University of Pisa, Pisa, Italy.
Patrizia GazzerroDepartment of Pharmacy, University of Salerno, Fisciano, Salerno, Italy.
Anna Maria D'UrsiDepartment of Pharmacy, University of Salerno, Fisciano, Salerno, Italy.
Maurizio BifulcoDepartment of Medicine, Surgery and Dentistry "Scuola Medica Salernitana", University of Salerno, Baronissi, Salerno, Italy.ORCID http://orcid.org/0000-0002-1771-4531
University of Salerno · ITUniversity of Milan · ITUniversity of Naples Federico II · ITUniversity of Pisa · IT

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

background and purposeN EXPERIMENTAL APPROACH: We designed and synthesized i6A derivatives characterized by the introduction of diverse chemical moieties in the N6 position of adenosine and tested for their efficacy in U87 cells and in primary glioma cultures, derived from patients. NMR-based structural analysis, molecular docking calculations and siRNA mediated knockdown were used to clarify the molecular basis of their action, targeting FPPS protein. KEY

resultsCM223, the i6A derivative including a benzyl moiety in N6 position of adenine, showed marked activity in selectively targeting glioma cells, but not normal human astrocytes. This was due to induction of intrinsic pathways of apoptosis and inhibition of proliferation, along with blockade of FPPS-dependent protein prenylation, which counteracted oncogenic signalling mediated by EGF receptors. CONCLUSION AND IMPLICATIONS: The biological effects together with structural data on interaction of CM223 with FPPS, provided additional evidence for the correlation of the i6A/CM223 antitumor activity with FPPS modulation. Because the MVA pathway is an important promising target, CM223 and its derivatives should be considered interesting active molecules in antiglioma research.

Indexed as

AdenosineAntineoplastic AgentsApoptosisBrain NeoplasmsCell ProliferationCells, CulturedDose-Response Relationship, DrugDrug Screening Assays, AntitumorGliomaHumansMevalonic AcidModels, MolecularMolecular StructureStructure-Activity RelationshipTerpenesAdenosineAntineoplastic AgentsMevalonic AcidTerpenes

Identifiers

PMID28419419
PMCPMC5481646
OpenAlexW2606704603

What OpenQuestion holds

Textmetadata
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.