Evidence map›Paper›PMID 29137866›Full record

ArticleEuropean journal of medicinal chemistry2018

Development of noviomimetics that modulate molecular chaperones and manifest neuroprotective effects.

Leah K Forsberg, Mercy Anyika, Zhenyuan You, Sean Emery, Mason McMullen, Rick T Dobrowsky, Brian S J Blagg

Open access · greenAbstract read
In one paragraph

Article in European journal of medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
0.4field-weighted citation impact, top 36% 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

4 citing papers in PubMed, 10 citations in OpenAlex.

  1. Article
  2. Review
  3. Article
  4. Review
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

7 authors at 2 institutions in 1 country.

Leah K ForsbergDepartment of Medicinal Chemistry, 1251 Wescoe Hall Drive, Malott 4070, The University of Kansas, Lawrence, KS 66045-7563, United States.
Mercy AnyikaDepartment of Medicinal Chemistry, 1251 Wescoe Hall Drive, Malott 4070, The University of Kansas, Lawrence, KS 66045-7563, United States.
Zhenyuan YouDepartment of Pharmacology and Toxicology Department, The University of Kansas, Lawrence, KS 66045, United States.
Sean EmeryDepartment of Pharmacology and Toxicology Department, The University of Kansas, Lawrence, KS 66045, United States.
Mason McMullenDepartment of Pharmacology and Toxicology Department, The University of Kansas, Lawrence, KS 66045, United States.
Rick T DobrowskyDepartment of Pharmacology and Toxicology Department, The University of Kansas, Lawrence, KS 66045, United States.
Brian S J BlaggDepartment of Chemistry and Biochemistry, 305 McCourtney Hall, The University of Notre Dame, Notre Dame, IN 46556, United States. Electronic address: bblagg@nd.edu.
University of Kansas · USUniversity of Notre Dame · US

Funding

Chaperone therapeutics for the treatment of DPNR01NS075311 · NINDS · UNIVERSITY OF NOTRE DAME · PI BLAGG, BRIAN S J, DOBROWSKY, RICK T · 2012 to 2020
$2.8M
HSP90 InhibitorsU01CA109265 · NCI · UNIVERSITY OF KANSAS LAWRENCE · PI BLAGG, BRIAN S J · 2006 to 2014
$2.2M
Chaperones in Diabetic Peripheral NeuropathyR01DK095911 · NIDDK · UNIVERSITY OF KANSAS LAWRENCE · PI DOBROWSKY, RICK T · 2013 to 2016
$1.3M
NCI NIH HHS U01 CA109265NIDDK NIH HHS R01 DK095911NINDS NIH HHS R01 NS075311
6 · The paper itself

Abstract

Heat shock protein 90 (Hsp90) is a chaperone under investigation for the treatment of cancer and neurodegenerative diseases. Neuroprotective Hsp90 C-terminal inhibitors derived from novobiocin (novologues) include KU-32 and KU-596. These novologues modulate molecular chaperones and result in an induction of Heat Shock Protein 70 (Hsp70). "Noviomimetics" replace the synthetically complex noviose sugar with a simple cyclohexyl moiety to maintain biological efficacy as compared to novologues KU-596 and KU-32. In this study, we further explore the development of noviomimetics and evaluate their efficacy using a luciferase refolding assay, immunoblot analysis, a c-jun assay, and an assay measuring mitochondrial bioenergetics. These new noviomimetics were designed and synthesized and found to induce Hsp70 and improve biological activity. Noviomimetics 39e and 40a were found to induce Hsp70 and exhibit promising effects in cellular assays.

Indexed as

Drug DiscoveryCell LineDose-Response Relationship, DrugHSP90 Heat-Shock ProteinsMitochondriaModels, MolecularNeuroprotective AgentsNovobiocinProtein ConformationHSP90 Heat-Shock ProteinsNeuroprotective AgentsNovobiocinHeat shock protein 70Heat shock protein 90Molecular chaperonesNeurodegenerationNoviomimeticsNovologues

Identifiers

PMID29137866
PMCPMC5736410
OpenAlexW2765469098

What OpenQuestion holds

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LicenceTDM
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.