ArticleBioorganic & medicinal chemistry2014
Potential C-terminal-domain inhibitors of heat shock protein 90 derived from a C-terminal peptide helix.
Article in Bioorganic & medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.
What it found
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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.
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.
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Who cites it
4 citing papers in PubMed, 14 citations in OpenAlex.
- Synthesis and Biological Evaluation of Stilbene Analogues as Hsp90 C-Terminal Inhibitors.ChemMedChem · 2017Article
- Diversity-Oriented Stapling Yields Intrinsically Cell-Penetrant Inducers of Autophagy.Journal of the American Chemical Society · 2017Article
- Synthesis and Biological Evaluation of Novobiocin Core Analogues as Hsp90 Inhibitors.Chemistry (Weinheim an der Bergstrasse, Germany) · 2016Article
- Targeting Hsp90 in urothelial carcinoma.Oncotarget · 2015Review
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
Hsp90 is a molecular chaperone implicated in many diseases including cancer and neurodegenerative disease. Most inhibitors target the ATPase site in Hsp90's N-terminal domain, with relatively few inhibitors of other domains reported to date. Here, we show that peptides derived from a short helix at the C-terminus of Hsp90 show micromolar activity as Hsp90 inhibitors in vitro. These inhibitors do not block the N-terminal domain's ATP-binding site, and thus are likely to bind at the C-terminal domain. Substitutions and helix stapling were applied to demonstrate structure-activity relationships and improve activity. These helical peptides will help guide the design of a new class of inhibitors of Hsp90's C-terminal domain.
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Registered trials
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.