Evidence map›Paper›PMID 29759728›Full record

ArticleBioorganic & medicinal chemistry letters2018

Synthesis and evaluation of a ring-constrained Hsp90 C-terminal inhibitor that exhibits neuroprotective activity.

Zheng Zhang, Zhenyuan You, Rick T Dobrowsky, Brian S J Blagg

Abstract read
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed
0.6field-weighted citation impact, top 32% 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

5 citing papers in PubMed, 13 citations in OpenAlex.

  1. Review
  2. Article
  3. Review
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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

4 authors at 2 institutions in 1 country.

Zheng ZhangDepartment of Chemistry and Biochemistry, The University of Notre Dame, 251 Nieuwland Science Hall, Notre Dame, IN 46556, United States.
Zhenyuan YouDepartment 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, The University of Notre Dame, 251 Nieuwland Science Hall, Notre Dame, IN 46556, United States. Electronic address: bblagg@nd.edu.
University of Kansas · USUniversity of Notre Dame · US

Funding

University of Kansas Alzheimer's Disease Research Center (KU ADRC)P30AG072973 · NIA · UNIVERSITY OF KANSAS MEDICAL CENTER · PI JEFFREY Murray BURNS, RUSSELL H. SWERDLOW · 2021 to 2026
$25.3M
University of Kansas Alzheimer's Disease Core CentersP30AG035982 · NIA · UNIVERSITY OF KANSAS MEDICAL CENTER · PI SWERDLOW, RUSSELL H. · 2011 to 2020
$16.6M
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
Development and Evaluation of Purine and Coumarin Based Hsp90 Inhibitors`U01CA120458 · NCI · UNIVERSITY OF KANSAS LAWRENCE · PI BLAGG, BRIAN S J · 2007 to 2014
$2.6M
Development and Evaluation of Purine and Coumarin Based Hsp90 Inhibitors`R01CA120458 · NCI · UNIVERSITY OF NOTRE DAME · PI BLAGG, BRIAN S J · 2006 to 2019
$1.9M
Chaperones in Diabetic Peripheral NeuropathyR01DK095911 · NIDDK · UNIVERSITY OF KANSAS LAWRENCE · PI DOBROWSKY, RICK T · 2013 to 2016
$1.3M
NCI NIH HHS R01 CA120458NCI NIH HHS U01 CA120458NIA NIH HHS P30 AG035982NIA NIH HHS P30 AG072973NIDDK NIH HHS R01 DK095911NINDS NIH HHS R01 NS075311
6 · The paper itself

Abstract

KU-596 is a second-generation C-terminal heat shock protein 90 KDa (Hsp90) modulator based on the natural product, novobiocin. KU-596 has been shown to induce Hsp70 levels and manifest neuroprotective activity through induction of the heat shock response. A ring-constrained analog of KU-596 was designed and synthesized to probe its binding orientation and ability to induce Hsp70 levels. Compound 2 was found to exhibit comparable or increased activity compared to KU-596, which is under clinical investigation for the treatment of neuropathy.

Indexed as

AnimalsBinding SitesCell Line, TransformedGlycosidesHSP70 Heat-Shock ProteinsHSP90 Heat-Shock ProteinsHydrogen BondingLactamsMitochondriaMolecular Docking SimulationNeuroprotective AgentsOxidative StressPhenanthridinesPhenethylaminesRatsTranscriptional ActivationGlycosidesHSP70 Heat-Shock ProteinsHSP90 Heat-Shock ProteinsKU-596LactamsNeuroprotective AgentsPhenanthridinesPhenethylaminesHsp90 C-terminal inhibitorNeuroprotectiveNovologueRing-constrained

Identifiers

PMID29759728
PMCPMC6119633
OpenAlexW2792875772

What OpenQuestion holds

Textmetadata
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.