ArticleBioorganic & medicinal chemistry letters2014
A heat shock protein 90 inhibitor that modulates the immunophilins and regulates hormone receptors without inducing the heat shock response.
Article in Bioorganic & medicinal chemistry letters, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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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
16 citing papers in PubMed, 52 citations in OpenAlex.
- Advances in the structures, mechanisms and targeting of molecular chaperones.Signal transduction and targeted therapy · 2025Review
- Anti-cancer properties of Sansalvamide A, its derivatives, and analogs: an updated review.Naunyn-Schmiedeberg's archives of pharmacology · 2024Review
- A silicon-containing aryl/penta-1,4-dien-3-one/amine hybrid exhibits antiproliferative effects on breast cancer cells by targeting the HSP90 C-terminus without inducing heat-shock response.RSC medicinal chemistry · 2023Article
- Development of a First-in-Class Small-Molecule Inhibitor of the C-Terminal Hsp90 Dimerization.ACS central science · 2022Article
- Review
- Using NMR to identify binding regions for N and C-terminal Hsp90 inhibitors using Hsp90 domains.RSC medicinal chemistry · 2021Article
- Differential expression of microRNAs associated with thermal stress in Frieswal (Bos taurus x Bos indicus) crossbred dairy cattle.Cell stress & chaperones · 2018Article
- The FKBP51 Glucocorticoid Receptor Co-Chaperone: Regulation, Function, and Implications in Health and Disease.International journal of molecular sciences · 2017Review
- Targeting the Hsp90 C-terminal domain to induce allosteric inhibition and selective client downregulation.Biochimica et biophysica acta. General subjects · 2017Article
- X66, a novel N-terminal heat shock protein 90 inhibitor, exerts antitumor effects without induction of heat shock response.Oncotarget · 2016Article
- Anticancer Inhibitors of Hsp90 Function: Beyond the Usual Suspects.Advances in cancer research · 2016Review
- Steroid Receptor-Associated Immunophilins: A Gateway to Steroid Signalling.The Clinical biochemist. Reviews · 2015Review
- Identification and bioinformatics analysis of microRNAs associated with stress and immune response in serum of heat-stressed and normal Holstein cows.Cell stress & chaperones · 2014Article
- Alternative approaches to Hsp90 modulation for the treatment of cancer.Future medicinal chemistry · 2014Article
- Triazole Containing Novobiocin and Biphenyl Amides as Hsp90 C-Terminal Inhibitors.MedChemComm · 2014Article
- Chemically accessible hsp90 inhibitor that does not induce a heat shock response.ACS medicinal chemistry letters · 2014Article
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Authors and funding
3 authors at 2 institutions in 2 countries.
Funding
Abstract
When a cell encounters external stressors, such as lack of nutrients, elevated temperatures, changes in pH or other stressful environments, a key set of evolutionarily conserved proteins, the heat shock proteins (hsps), become overexpressed. Hsps are classified into six major families with the hsp90 family being the best understood; an increase in cell stress leads to increased levels of hsp90, which leads to cellular protection. A hallmark of hsp90 inhibitors is that they induce a cell rescue mechanism, the heat shock response. We define the unique molecular profile of a compound (SM145) that regulates hormone receptor protein levels through hsp90 inhibition without inducing the heat shock response. Modulation of the binding event between heat shock protein 90 and the immunophilins/homologs using SM145, leads to a decrease in hormone receptor protein levels. Unlike N-terminal hsp90 inhibitors, this hsp90 inhibitor does not induce a heat shock response. This work is proof of principle that controlling hormone receptor expression can occur by inhibiting hsp90 without inducing pro-survival protein heat shock protein 70 (hsp70) or other proteins associated with the heat shock response. Innovatively, we show that blocking the heat shock response, in addition to hsp90, is key to regulating hsp90-associated pathways.
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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.