Evidence map›Paper›PMID 26819668›Full record

ArticleACS medicinal chemistry letters2016

Development of Noviomimetics as C-Terminal Hsp90 Inhibitors.

Mercy Anyika, Mason McMullen, Leah K Forsberg, Rick T Dobrowsky, Brian S J Blagg

Abstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers, 1 of them a synthesis that pooled it.

0numbers the graph read from it
0cells of the map it votes in
16citing papers in PubMed, 1 pooled it
2.3field-weighted citation impact, top 12% 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

16 citing papers in PubMed, 1 synthesis or guideline pooled it, 30 citations in OpenAlex.

  1. Pooled it
  2. Review
  3. Article
  4. Review
  5. Recent advances toward the development of Hsp90 C-terminal inhibitors.Bioorganic & medicinal chemistry letters · 2023
    Review
  6. Article
  7. Article
  8. Review
  9. Inhibitors and chemical probes for molecular chaperone networks.The Journal of biological chemistry · 2019
    Review
  10. Article
  11. Effects of Inhibitors on Hsp90's Conformational Dynamics, Cochaperone and Client Interactions.Chemphyschem : a European journal of chemical physics and physical chemistry · 2018
    Article
  12. Article
  13. Article
  14. Article
  15. Gambogic acid identifies an isoform-specific druggable pocket in the middle domain of Hsp90β.Proceedings of the National Academy of Sciences of the United States of America · 2016
    Article
  16. 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

5 authors at 1 institution in 1 country.

Mercy AnyikaDepartment of Medicinal Chemistry, The University of Kansas , 1251 Wescoe Hall Drive, Malott 4070, Lawrence, Kansas 66045-7563, United States.
Mason McMullenDepartment of Pharmacology and Toxicology Department, The University of Kansas , Lawrence, Kansas 66045, United States.
Leah K ForsbergDepartment of Medicinal Chemistry, The University of Kansas , 1251 Wescoe Hall Drive, Malott 4070, Lawrence, Kansas 66045-7563, United States.
Rick T DobrowskyDepartment of Pharmacology and Toxicology Department, The University of Kansas , Lawrence, Kansas 66045, United States.
Brian S J BlaggDepartment of Medicinal Chemistry, The University of Kansas , 1251 Wescoe Hall Drive, Malott 4070, Lawrence, Kansas 66045-7563, United States.
University of Kansas · 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
Engineering the Next Generation of Safer Hsp90 InhibitorsR01CA270147 · NCI · UNIVERSITY OF NOTRE DAME · PI Brian S J Blagg, Mark Steven Cohen · 2023 to 2026
$1.8M
Chaperones in Diabetic Peripheral NeuropathyR01DK095911 · NIDDK · UNIVERSITY OF KANSAS LAWRENCE · PI DOBROWSKY, RICK T · 2013 to 2016
$1.3M
NCI NIH HHS R01 CA270147NCI NIH HHS U01 CA109265NIDDK NIH HHS R01 DK095911NINDS NIH HHS R01 NS075311
6 · The paper itself

Abstract

KU-32 and KU-596 are novobiocin-derived, C-terminal heat shock protein 90 (Hsp90) modulators that induce Hsp70 levels and manifest neuroprotective activity. However, the synthetically complex noviose sugar requires 10 steps to prepare, which makes translational development difficult. In this study, we developed a series of "noviomimetic" analogues of KU-596, which contain noviose surrogates that can be easily prepared, while maintaining the ability to induce Hsp70 levels. Both sugar and sugar analogues were designed, synthesized, and evaluated in a luciferase reporter assay, which identified compound 37, a benzyl containing noviomimetic, as the most potent inducer of Hsp70.

Indexed as

C-terminal inhibitionHeat Shock Protein 70Heat Shock Protein 90neuroprotectionnoviomimetics

Identifiers

PMID26819668
PMCPMC4716602
OpenAlexW2263525143

What OpenQuestion holds

Textmetadata
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.