Evidence map›Paper›PMID 37736193›Full record

ArticleACS medicinal chemistry letters2023

Synthesis and Validation of the First Cell-Impermeable Hsp90α-Selective Inhibitors.

Tyelor S Reynolds, Brian S J Blagg

Open access · greenAbstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.

0numbers the graph read from it
0cells of the map it votes in
6citing papers in PubMed
1.2field-weighted citation impact, top 20% 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

6 citing papers in PubMed, 8 citations in OpenAlex.

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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

2 authors at 1 institution in 1 country.

Tyelor S ReynoldsDepartment of Chemistry and Biochemistry, The University of Notre Dame, 305 McCourtney Hall, Notre Dame, Indiana 46556, United States.
Brian S J BlaggDepartment of Chemistry and Biochemistry, The University of Notre Dame, 305 McCourtney Hall, Notre Dame, Indiana 46556, United States.ORCID https://orcid.org/0000-0002-6200-3480
University of Notre Dame · US

Funding

Chemistry-Biochemistry-Biology Interface (CBBI) Program at Notre DameT32GM145773 · NIGMS · UNIVERSITY OF NOTRE DAME · PI Christian Corey Melander · 2022 to 2026
$1.5M
Development of Hsp90 inhibitors for the treatment of cancerR01CA167079 · NCI · UNIVERSITY OF NOTRE DAME · PI BLAGG, BRIAN S J · 2012 to 2016
$1.5M
NCI NIH HHS R01 CA167079NIGMS NIH HHS T32 GM145773
6 · The paper itself

Abstract

Hsp90α is an isoform of the heat shock protein 90 (Hsp90) family of molecular chaperones and mediates the folding and activation of ∼400 client proteins. However, inhibition of intracellular Hsp90α has caused detrimental side effects and significantly hindered the clinical development of Hsp90 inhibitors. As an alternative strategy, 14 Hsp90α-selective inhibitors were synthesized to introduce permanently charged moieties onto the solvent-exposed portion of the Hsp90α binding site to produce cell-impermeable extracellular Hsp90α-selective inhibitors. The resulting lead compounds were cell-permeable dimethylamine

Identifiers

PMID37736193
PMCPMC10510499
OpenAlexW4385655668

What Socratic 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 Socratic graph.