Evidence map›Paper›PMID 34445078›Full record

ArticleInternational journal of molecular sciences2021

A New Smoothened Antagonist Bearing the Purine Scaffold Shows Antitumour Activity In Vitro and In Vivo.

Ana María Zárate, Christian Espinosa-Bustos, Simón Guerrero, Angélica Fierro, Felipe Oyarzún-Ampuero, Andrew F G Quest, Lucia Di Marcotullio, Elena Loricchio, Miriam Caimano, Andrea Calcaterra and 4 more

Open access · goldAbstract read
In one paragraph

Article in International journal of molecular sciences, 2021. 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
1.0field-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

7 citing papers in PubMed, 16 citations in OpenAlex.

  1. Article
  2. Article
  3. Article
  4. Molecular Target and Action Mechanism of Anti-Cancer Agents.International journal of molecular sciences · 2023
    Article
  5. Review
  6. Article
  7. Substituted Purines as High-Affinity Histamine HPharmaceuticals (Basel, Switzerland) · 2022
    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

14 authors at 8 institutions in 2 countries.

Ana María ZárateDepartamento de Química Orgánica, Facultad de Química y de Farmacia, Pontificia Universidad Católica de Chile, Vicuña Mackenna 4860, Macul, Santiago 702843, Chile.ORCID 0000-0002-2132-2143
Christian Espinosa-BustosDepartamento de Farmacia, Facultad de Química y de Farmacia, Pontificia Universidad Católica de Chile, Vicuña Mackenna 4860, Macul, Santiago 702843, Chile.
Simón GuerreroAdvanced Center for Chronic Diseases (ACCDiS), Universidad de Chile, Sergio Livingstone 1007, Independencia, Santiago 8380492, Chile.ORCID 0000-0002-3003-0337
Angélica FierroDepartamento de Química Orgánica, Facultad de Química y de Farmacia, Pontificia Universidad Católica de Chile, Vicuña Mackenna 4860, Macul, Santiago 702843, Chile.ORCID 0000-0002-6507-4188
Felipe Oyarzún-AmpueroAdvanced Center for Chronic Diseases (ACCDiS), Universidad de Chile, Sergio Livingstone 1007, Independencia, Santiago 8380492, Chile.
Andrew F G QuestAdvanced Center for Chronic Diseases (ACCDiS), Universidad de Chile, Sergio Livingstone 1007, Independencia, Santiago 8380492, Chile.ORCID 0000-0001-8755-1590
Lucia Di MarcotullioLaboratory Affiliated to Insituto Pasteur Italia, Fondazione Cenci Bognetti, Department of Molecular Medicine, Sapienza University of Rome, Viale Regina Elena 291, 00161 Rome, Italy.ORCID 0000-0003-0274-7178
Elena LoricchioCenter For Life Nano Science@Sapienza, Istituto Italiano di Tecnologia, Viale Regina Elena 291, 00161 Rome, Italy.
Miriam CaimanoDepartment of Molecular Medicine, Sapienza University of Rome, Viale Regina Elena 291, 00161 Rome, Italy.
Andrea CalcaterraDepartment of Chemistry and Technology of Drugs, Sapienza University of Rome, Piazzale Aldo Moro 5, 00185 Rome, Italy.ORCID 0000-0001-7036-6620
Matías González-QuirozProgram of Cellular and Molecular Biology, Institute of Biomedical Sciences, Universidad de Chile, Independencia 1027, Santiago 8380453, Chile.ORCID 0000-0002-3727-0771
Adam AguirreLaboratorio de Medicina Traslacional, Fundación Arturo López Pérez, Rancagua 878, Lower Fifth Floor, Providencia, Santiago 8320000, Chile.
Jaime MeléndezDepartamento de Farmacia, Facultad de Química y de Farmacia, Pontificia Universidad Católica de Chile, Vicuña Mackenna 4860, Macul, Santiago 702843, Chile.
Cristian O SalasDepartamento de Química Orgánica, Facultad de Química y de Farmacia, Pontificia Universidad Católica de Chile, Vicuña Mackenna 4860, Macul, Santiago 702843, Chile.ORCID 0000-0001-7620-2459
Pontificia Universidad Católica de Chile · CLAdvanced Center for Chronic Diseases · CLSapienza University of Rome · ITFundación Arturo López Pérez · CLIstituto Pasteur · ITItalian Institute of Technology · ITUniversidad SEK · CLUniversity of Chile · CL

Funding

Fondecyt 1161816, 1161375 and 1170925
6 · The paper itself

Abstract

The Smoothened (SMO) receptor is the most druggable target in the Hedgehog (HH) pathway for anticancer compounds. However, SMO antagonists such as vismodegib rapidly develop drug resistance. In this study, new SMO antagonists having the versatile purine ring as a scaffold were designed, synthesised, and biologically tested to provide an insight to their mechanism of action. Compound

Indexed as

AnimalsAntineoplastic AgentsApoptosisCell Line, TumorCell ProliferationHedgehog ProteinsHT29 CellsHumansMiceMice, Inbred C57BLNeoplasmsPurinesSignal TransductionSmoothened ReceptorAntineoplastic AgentsHedgehog ProteinsPurinesSmoothened Receptordocking studiesHedgehog signalling pathwayin vivo assayspurine derivativessmoothened receptor antagonists

Identifiers

PMID34445078
PMCPMC8395040
OpenAlexW3192341051

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.