Evidence map›Paper›PMID 25419525›Full record

ArticleNuclear receptor research2014

IDENTIFICATION OF VDR ANTAGONISTS AMONG NUCLEAR RECEPTOR LIGANDS USING VIRTUAL SCREENING.

Kelly Teske, Premchendar Nandhikonda, Jonathan W Bogart, Belaynesh Feleke, Preetpal Sidhu, Nina Yuan, Joshua Preston, Robin Goy, Lanlan Han, Nicholas R Silvaggi and 4 more

Open access · diamondAbstract read
In one paragraph

Article in Nuclear receptor research, 2014. 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
1.8field-weighted citation impact, top 15% 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, 13 citations in OpenAlex.

  1. Article
  2. Article
  3. Novel VDR antagonists based on the GW0742 scaffold.Bioorganic & medicinal chemistry letters · 2018
    Article
  4. Article
  5. Review
  6. Review
  7. Anticancer activity of VDR-coregulator inhibitor PS121912.Cancer chemotherapy and pharmacology · 2014
    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 3 institutions in 1 country.

Kelly TeskeDepartment of Chemistry and Biochemistry, University of Wisconsin-Milwaukee, WI 53211, USA.
Premchendar NandhikondaDepartment of Chemistry and Biochemistry, University of Wisconsin-Milwaukee, WI 53211, USA.
Jonathan W BogartDepartment of Chemistry and Biochemistry, University of Wisconsin-Milwaukee, WI 53211, USA.
Belaynesh FelekeDepartment of Chemistry and Biochemistry, University of Wisconsin-Milwaukee, WI 53211, USA.
Preetpal SidhuDepartment of Chemistry and Biochemistry, University of Wisconsin-Milwaukee, WI 53211, USA.
Nina YuanDepartment of Chemistry and Biochemistry, University of Wisconsin-Milwaukee, WI 53211, USA.
Joshua PrestonDepartment of Chemistry and Biochemistry, University of Wisconsin-Milwaukee, WI 53211, USA.
Robin GoyDepartment of Chemistry and Biochemistry, University of Wisconsin-Milwaukee, WI 53211, USA.
Lanlan HanDepartment of Chemistry and Biochemistry, University of Wisconsin-Milwaukee, WI 53211, USA.
Nicholas R SilvaggiDepartment of Chemistry and Biochemistry, University of Wisconsin-Milwaukee, WI 53211, USA.
Rakesh K SinghMolecular Therapeutics Laboratory, Program in Women's Oncology, Department of Obstetrics and Gynecology, Woman and Infant's Hospital of Rhode Island, Alpert Medical School of, Brown University, Provence, RI 02903, USA.
Daniel D BikleEndocrine Research Unit, Department of Medicine, Veterans Affairs Medical Center, San Francisco, CA 94121, USA.
James M CookDepartment of Chemistry and Biochemistry, University of Wisconsin-Milwaukee, WI 53211, USA.
Leggy A ArnoldDepartment of Chemistry and Biochemistry, University of Wisconsin-Milwaukee, WI 53211, USA.
University of Wisconsin–Milwaukee · USBrown University · USSan Francisco VA Medical Center · US

Funding

Vitamin D Receptor Coactivators in KeratinocytesR01AR050023 · NIAMS · NORTHERN CALIFORNIA INSTITUTE RES &EDUC · PI BIKLE, DANIEL DAVID · 2004 to 2014
$3.4M
Development of new drugs for asthma by targeting GABA(A) receptors in the lungR01HL118561 · NHLBI · UNIVERSITY OF WISCONSIN MILWAUKEE · PI COOK, JAMES M · 2014 to 2017
$2.0M
Design of New Therapeutic Agents to Treat SchizophreniaR01MH096463 · NIMH · UNIVERSITY OF WISCONSIN MILWAUKEE · PI COOK, JAMES M · 2013 to 2017
$1.9M
Synthesis of Alpha2/Alpha3 GABA Agonists to Treat Neuropathic PainR01NS076517 · NINDS · UNIVERSITY OF WISCONSIN MILWAUKEE · PI COOK, JAMES M · 2012 to 2015
$1.3M
Small molecule inhibitors of the vitamin D receptor-coactivator interactionR03DA031090 · NIDA · UNIVERSITY OF WISCONSIN MILWAUKEE · PI ARNOLD, ALEXANDER · 2010 to 2011
$73k
NHLBI NIH HHS R01 HL118561NIAMS NIH HHS R01 AR050023NIDA NIH HHS R03 DA031090NIMH NIH HHS R01 MH096463NINDS NIH HHS R01 NS076517
6 · The paper itself

Abstract

Herein, we described the development of two virtual screens to identify new vitamin D receptor (VDR) antagonists among nuclear receptor (NR) ligands. Therefore, a database of 14330 nuclear receptor ligands and their NR affinities was assembled using the online available "Binding Database". Two different virtual screens were carried out in conjunction with a reported VDR crystal structure applying a stringent and less stringent pharmacophore model to filter docked NR ligand conformations. The pharmacophore models were based on the spatial orientation of the hydroxyl functionalities of VDR's natural ligands 1,25(OH

Indexed as

estrogen receptornuclear receptorthyroid receptorVirtual screeningvitamin D receptor

Identifiers

PMID25419525
PMCPMC4240308
OpenAlexW1999642768

What OpenQuestion holds

Textmetadata
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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.