Evidence map›Paper›PMID 24478983›Full record

ReviewFrontiers in oncology2014

Small and Innovative Molecules as New Strategy to Revert MDR.

Laura Zinzi, Elena Capparelli, Mariangela Cantore, Marialessandra Contino, Marcello Leopoldo, Nicola Antonio Colabufo

Abstract readReview
In one paragraph

Review in Frontiers in oncology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.

0numbers the graph read from it
0cells of the map it votes in
25citing papers in PubMed
–field-weighted citation impact
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

25 citing papers in PubMed.

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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

6 authors.

Laura ZinziDipartimento di Farmacia - Scienze del Farmaco, Università degli Studi di Bari "A. Moro" , Bari , Italy.
Elena CapparelliDipartimento di Farmacia - Scienze del Farmaco, Università degli Studi di Bari "A. Moro" , Bari , Italy.
Mariangela CantoreDipartimento di Farmacia - Scienze del Farmaco, Università degli Studi di Bari "A. Moro" , Bari , Italy.
Marialessandra ContinoDipartimento di Farmacia - Scienze del Farmaco, Università degli Studi di Bari "A. Moro" , Bari , Italy.
Marcello LeopoldoDipartimento di Farmacia - Scienze del Farmaco, Università degli Studi di Bari "A. Moro" , Bari , Italy.
Nicola Antonio ColabufoDipartimento di Farmacia - Scienze del Farmaco, Università degli Studi di Bari "A. Moro" , Bari , Italy.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Multidrug resistance (MDR) is a complex phenomenon principally due to the overexpression of some transmembrane proteins belonging to the ATP binding cassette (ABC) transporter family. Among these transporters, P-glycoprotein (P-gp) is mostly involved in MDR and its overexpression is the major cause of cancer therapy failure. The classical approach used to overcome MDR is the co-administration of a P-gp inhibitor and the classic antineoplastic drugs, although the results were often unsatisfactory. Different classes of P-gp ligands have been developed and, among them, Tariquidar has been extensively studied both in vitro and in vivo. Although Tariquidar has been considered for several years as the lead compound for the development of P-gp inhibitors, recent studies demonstrated it to be a substrate and inhibitor, in a dose-dependent manner. Moreover, Tariquidar structure-activity relationship studies were difficult to carry out because of the complexity of the structure that does not allow establishing the role of each moiety for P-gp activity. For this purpose, SMALL molecules bearing different scaffolds such as tetralin, biphenyl, arylthiazole, furoxane, furazan have been developed. Many of these ligands have been tested both in in vitro assays and in in vivo PET studies. These preliminary evaluations lead to obtain a library of P-gp interacting agents useful to conjugate chemotherapeutic agents displaying reduced pharmacological activity and appropriate small molecules. These molecules could get over the limits due to the antineoplastic-P-gp inhibitor co-administration since pharmacokinetic and pharmacodynamic profiles are related to a dual innovative drug.

Indexed as

dual effectMDRMDR reverting activitymultitarget drugsP-gp

Identifiers

PMID24478983
PMCPMC3896858

What OpenQuestion holds

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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.