Evidence map›Paper›PMID 31289333›Full record

ArticleScientific reports2019

Dual Kit/Aur Inhibitors as Chemosensitizing Agents for the Treatment of Melanoma: Design, Synthesis, Docking Studies and Functional Investigation.

Luca Quattrini, Vito Coviello, Stefania Sartini, Teresa Di Desidero, Paola Orlandi, Yi-Yu Ke, Kai-Lun Liu, Hsing-Pang Hsieh, Guido Bocci, Concettina La Motta

Abstract read
In one paragraph

Article in Scientific reports, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing 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

2 citing papers in PubMed.

  1. Review
  2. 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

10 authors.

Luca QuattriniDipartimento di Farmacia, Università di Pisa, Via Bonanno 6, 56126, Pisa, Italy.
Vito CovielloDipartimento di Farmacia, Università di Pisa, Via Bonanno 6, 56126, Pisa, Italy.
Stefania SartiniDipartimento di Farmacia, Università di Pisa, Via Bonanno 6, 56126, Pisa, Italy.ORCID http://orcid.org/0000-0002-7671-5243
Teresa Di DesideroDipartimento di Medicina Clinica e Sperimentale, Università di Pisa, Via Roma 55, 56126, Pisa, Italy.
Paola OrlandiDipartimento di Medicina Clinica e Sperimentale, Università di Pisa, Via Roma 55, 56126, Pisa, Italy.
Yi-Yu KeInstitute of Biotechnology and Pharmaceutical Research, National Health Research Institutes, 35, Keyan Road, Zhunan Town, Miaoli County, 350, Taiwan.
Kai-Lun LiuInstitute of Biotechnology and Pharmaceutical Research, National Health Research Institutes, 35, Keyan Road, Zhunan Town, Miaoli County, 350, Taiwan.
Hsing-Pang HsiehInstitute of Biotechnology and Pharmaceutical Research, National Health Research Institutes, 35, Keyan Road, Zhunan Town, Miaoli County, 350, Taiwan.
Guido BocciDipartimento di Medicina Clinica e Sperimentale, Università di Pisa, Via Roma 55, 56126, Pisa, Italy.
Concettina La MottaDipartimento di Farmacia, Università di Pisa, Via Bonanno 6, 56126, Pisa, Italy. concettina.lamotta@unipi.it.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Melanoma is the most serious form of skin cancer but its medication is still far from being safe and thoroughly effective. The search of novel therapeutic approaches represents therefore a health emergency to push through eagerly. In this study, we describe a novel class of dual c-Kit/Aur inhibitors, characterized by a 1,2,4-triazole core and developed by a structure-based optimization of a previously developed hit, and report the evidence of their significance as drug candidates for the treatment of melanoma. Compound 6a, merging the best inhibitory profile against the target kinases, showed anti-proliferative efficacy against the human melanoma cell lines A2058, expressing the BRAF V600D mutation, and WM266-4, expressing BRAF V600E. Significantly, it displayed also a highly synergistic profile when tested in combination with vemurafenib, thus proving its efficacy not only per se but even in a combination therapy, which is nowadays acknowledged as the cornerstone approach of the forthcoming tumour management.

Indexed as

Drug DesignMolecular Docking SimulationAntineoplastic AgentsAurora KinasesCell ProliferationHumansMelanomaMutationProtein Kinase InhibitorsProto-Oncogene Proteins B-rafProto-Oncogene Proteins c-kitTumor Cells, CulturedAntineoplastic AgentsAurora KinasesBRAF protein, humanKIT protein, humanProtein Kinase InhibitorsProto-Oncogene Proteins B-rafProto-Oncogene Proteins c-kit

Identifiers

PMID31289333
PMCPMC6617451

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.