The DOI matches its Crossref record; 1 of the 1 references it cites were found in a registry or an index.
Hsp90 Inhibitors Identified from a Library of Novobiocin Analogues
Abstract
Novobiocin is a C-terminal inhibitor of the Hsp90 protein folding machinery, which is responsible for the conformational maturation of numerous proteins involved in cancer growth and survival. Due to novobiocin's poor inhibitory activity ( approximately 700 muM), very little attention has been paid toward the development of novobiocin analogues for Hsp90 inhibition. In this study, a parallel library of 20 novobiocin derivatives was prepared and the biological activity of each evaluated by Western blot analysis of Hsp90 client proteins. A4 was found to be a potent inhibitor of Hsp90 as determined by its ability to cause the degradation of several Hsp90 client proteins in both breast and prostate cancer cell lines. In the presence of 1 muM A4, several Hsp90 client proteins were degraded, including AKT, Her2, Hif-1alpha, and the androgen receptor.
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Cites
Roe, S. M., Prodromou, C., O'Brien, R., Ladbury, J. E., Piper, P. W., & Pearl, L. H. (1999) · Journal of Medicinal Chemistry · doi:10.1021/jm980403y · Cited by 1,004
Cited by
WORKMAN, P., BURROWS, F., NECKERS, L., & ROSEN, N. (2007) · Annals of the New York Academy of Sciences · doi:10.1196/annals.1391.012 · Cited by 521
Self-citationCoumarins: Old Compounds with Novel Promising Therapeutic Perspectives
Riveiro, M., De Kimpe, N., Moglioni, A., Vazquez, R., Monczor, F., Shayo, C., & Davio, C. (2010) · Current Medicinal Chemistry · doi:10.2174/092986710790936284 · Cited by 448
Jackson, S. E. (2012) · Topics in Current Chemistry · doi:10.1007/128_2012_356 · Cited by 338
Heat shock transcription factor 1 as a therapeutic target in neurodegenerative diseases
Neef, D. W., Jaeger, A. M., & Thiele, D. J. (2011) · Nature Reviews Drug Discovery · doi:10.1038/nrd3453 · Cited by 307
Small molecule modulators of protein-protein interactions: selected case studies
Aeluri, M., Chamakuri, S., Dasari, B., Guduru, S. K. R., Jimmidi, R., Jogula, S., & Arya, P. (2014) · Chemical Reviews · doi:10.1021/cr4004049 · Cited by 79
Pan- and isoform-specific inhibition of Hsp90: Design strategy and recent advances
Yu, J., Zhang, C., & Song, C. (2022) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2022.114516 · Cited by 51
Metadata
- Authors
- Yu, X. M., Shen, G., Neckers, L., Blake, H., Holzbeierlein, J., Cronk, B., & Blagg, B. S. J.
- Venue
- Journal of the American Chemical Society
- Publisher
- American Chemical Society (ACS)
- Published
- 2005-08-25
- Volume
- 127
- Issue
- 37
- Pages
- 12778-12779
- ISSN
- 0002-7863 (ISSN-L)
- 1520-5126
- OpenAlex
- W2020742237
- Cited by
- 172
- References
- 1
- FWCI
- 3.46
- Type
- journal article
- Language
- en
- Open access
- closed
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
