Evidence map›Paper›PMID 39153203›Full record

ArticleChemMedChem2024

The Investigation of Hsp90C-Terminal Inhibitors Containing Amide Bioisosteres.

Eva Amatya, Chitra Subramanian, Reagan Long, Kelli McNamara, Mark S Cohen, Brian S J Blagg

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in ChemMedChem, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing papers in PubMed
–field-weighted citation impact
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

1 citing paper in PubMed.

  1. 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

6 authors.

Eva AmatyaDepartment of Chemistry and Biochemistry, Warren Family Research Center for Drug Discovery and Development, University of Notre Dame, Notre Dame, Indiana, 46556, USA.
Chitra SubramanianCancer Center at Illinois, University of Illinois Urbana-Champaign, Urbana, Illinois, 61801, United States.
Reagan LongDepartment of Chemistry and Biochemistry, Warren Family Research Center for Drug Discovery and Development, University of Notre Dame, Notre Dame, Indiana, 46556, USA.
Kelli McNamaraCancer Center at Illinois, University of Illinois Urbana-Champaign, Urbana, Illinois, 61801, United States.
Mark S CohenCancer Center at Illinois, University of Illinois Urbana-Champaign, Urbana, Illinois, 61801, United States.
Brian S J BlaggDepartment of Chemistry and Biochemistry, Warren Family Research Center for Drug Discovery and Development, University of Notre Dame, Notre Dame, Indiana, 46556, USA.ORCID 0000-0002-6200-3480

Funding

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
Optimization and Investigation of Cruentaren A analogsR01CA216919 · NCI · UNIVERSITY OF NOTRE DAME · PI BLAGG, BRIAN S J, COHEN, MARK STEVEN · 2017 to 2021
$1.4M
NCI NIH HHS CA270147NCI NIH HHS R01 CA216919NCI NIH HHS R01 CA270147
6 · The paper itself

Abstract

Heat Shock Protein 90 (Hsp90) is responsible for the proper folding and maturation of ~400 client protein substrates, many of which are directly associated with the ten hallmarks of cancer. Hsp90 is a great target for cancer therapy including melanoma, since Hsp90 inhibition can disrupt multiple oncogenic pathways simultaneously. In this study, we report the synthesis and anti-proliferative activity manifested by a series of Hsp90 C-terminal inhibitors against mutant BRAF and wild-type BRAF melanoma cells. Furthermore, we explored structure-activity relationships (SAR) for the amide moiety of 6 (B1), a novel Hsp90C-terminal inhibitor via introduction of amide bioisosteres. Compound 6 displayed an IC

Indexed as

AmidesAntineoplastic AgentsCell ProliferationHSP90 Heat-Shock ProteinsCell Line, TumorDose-Response Relationship, DrugDrug Screening Assays, AntitumorHumansMelanomaMolecular StructureProto-Oncogene Proteins B-rafStructure-Activity RelationshipAmidesAntineoplastic AgentsHSP90 Heat-Shock ProteinsProto-Oncogene Proteins B-rafAnti-cancerBRAF and MEK mutant resistantC-terminal inhibitorsHeat shock protein 90 (Hsp90)MelanomaNovobiocin derivative

Identifiers

PMID39153203
PMCPMC11649481

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Registered trials

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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.