Evidence map›Paper›PMID 27135651›Full record

ArticleChemMedChem2016

Cyclic Ketoximes as Estrogen Receptor β Selective Agonists.

Carlotta Granchi, Margherita Lapillo, Concetta Russo Spena, Flavio Rizzolio, Tiziano Tuccinardi, Teresa A Martin, Kathryn E Carlson, John A Katzenellenbogen, Filippo Minutolo

Open access · greenAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in ChemMedChem, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

0numbers the graph read from it
0cells of the map it votes in
0citing papers in PubMed
–field-weighted citation impact, top 97% 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

0 citing papers in PubMed, 2 citations in OpenAlex.

No citing paper in PubMed yet.

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

9 authors at 5 institutions in 3 countries.

Carlotta GranchiDipartimento di Farmacia, Università di Pisa, Via Bonanno 33, 56126, Pisa, Italy. carlotta.granchi@farm.unipi.it.
Margherita LapilloDipartimento di Farmacia, Università di Pisa, Via Bonanno 33, 56126, Pisa, Italy.
Concetta Russo SpenaGraduate School in Chemistry, University of Trieste, Italy.
Flavio RizzolioDivision of Experimental and Clinical Pharmacology, Department of Molecular Biology and Translational Research, CRO National Cancer Institute and Center for Molecular Biomedicine, IRCCS, 33081, Aviano, Pordenone, Italy.
Tiziano TuccinardiDipartimento di Farmacia, Università di Pisa, Via Bonanno 33, 56126, Pisa, Italy.
Teresa A MartinDepartment of Chemistry, University of Illinois, 600 S. Mathews Avenue, Urbana, IL, 61801, USA.
Kathryn E CarlsonDepartment of Chemistry, University of Illinois, 600 S. Mathews Avenue, Urbana, IL, 61801, USA.
John A KatzenellenbogenDepartment of Chemistry, University of Illinois, 600 S. Mathews Avenue, Urbana, IL, 61801, USA.
Filippo MinutoloDipartimento di Farmacia, Università di Pisa, Via Bonanno 33, 56126, Pisa, Italy.
University of Pisa · ITUniversity of Illinois Urbana-Champaign · USNational Cancer Institute · UAUniversity of Trieste · ITUrbana University · US

Funding

Novel Ligands and Mechanisms to Achieve Selective Nuclear Receptor ActivityR01DK015556 · NIDDK · UNIVERSITY OF ILLINOIS URBANA-CHAMPAIGN · PI KATZENELLENBOGEN, JOHN A. · 1986 to 2016
$1.6M
NIDDK NIH HHS R01 DK015556
6 · The paper itself

Abstract

The development of estrogen receptor β (ERβ)-selective agonists represents a therapeutic strategy against several kinds of cancers, but the high homology between the two receptor subtypes, ERα and ERβ, makes the achievement of this goal very challenging. In the past, we developed salicylaldoxime- and salicylketoxime-based molecules that proved to bind well to ERβ. In this paper, further structural evolution of the salicylketoximes is presented: two of the newly synthesized five-membered cyclic ketoximes bind with nanomolar affinities to ERβ, and they show selectivity for this subtype over ERα. Their agonist character was confirmed by cell-free coactivator recruitment assays, in which we demonstrated the ability of these compounds to form an active complex with ERβ capable of recruiting coactivator proteins; this indicated their efficacy as agonists. Finally, their potency and selectivity for ERβ binding were rationalized by molecular-modeling studies.

Indexed as

Cell Line, TumorCell ProliferationCell SurvivalCyclizationDose-Response Relationship, DrugEstrogen Receptor betaHumansModels, MolecularMolecular StructureOximesStructure-Activity RelationshipEstrogen Receptor betaOximescancerestrogenligand bindingoximesreceptors

Identifiers

PMID27135651
PMCPMC4993649
OpenAlexW2345941202

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.