The DOI matches its Crossref record; 3 of the 3 references it cites were found in a registry or an index.
Targeting Wide-Range Oncogenic Transformation via PU24FCl, a Specific Inhibitor of Tumor Hsp90
Open accessAbstract
Agents that inhibit Hsp90 function hold significant promise in cancer therapy. Here we present PU24FCl, a representative of the first class of designed Hsp90 inhibitors. By specifically and potently inhibiting tumor Hsp90, PU24FCl exhibits wide-ranging anti-cancer activities that occur at similar doses in all tested tumor types. Normal cells are 10- to 50-fold more resistant to these effects. Its Hsp90 inhibition results in multiple anti-tumor-specific effects, such as degradation of Hsp90-client proteins involved in cell growth, survival, and specific transformation, inhibition of cancer cell growth, delay of cell cycle progression, induction of morphological and functional changes, and apoptosis. In concordance with its higher affinity for tumor Hsp90, in vivo PU24FCl accumulates in tumors while being rapidly cleared from normal tissue. Concentrations achieved in vivo in tumors lead to single-agent anti-tumor activity at non-toxic doses.
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Cites
Lipinski, C. A., Lombardo, F., Dominy, B. W., & Feeney, P. J. (2001) · Advanced Drug Delivery Reviews · doi:10.1016/s0169-409x(00)00129-0 · Cited by 18,139
Molecular properties that influence the oral bioavailability of drug candidates
Veber, D. F., Johnson, S. R., Cheng, H.-Y., Smith, B. R., Ward, K. W., & Kopple, K. D. (2002) · Journal of Medicinal Chemistry · doi:10.1021/jm020017n · Cited by 8,420
Chang, F., Lee, J. T., Navolanic, P. M., Steelman, L. S., Shelton, J. G., Blalock, W. L., Franklin, R. A., & McCubrey, J. A. (2003) · Leukemia · doi:10.1038/sj.leu.2402824 · Cited by 1,176
Cited by
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
- Vilenchik, M., Solit, D., Basso, A., Huezo, H., Lucas, B., He, H., Rosen, N., Spampinato, C., Modrich, P., & Chiosis, G.
- Venue
- Chemistry & Biology
- Publisher
- Elsevier BV
- Published
- 2004-06
- Volume
- 11
- Issue
- 6
- Pages
- 787-797
- ISSN
- 1074-5521 (ISSN-L)
- OpenAlex
- W1980282046
- Cited by
- 171
- References
- 3
- FWCI
- 6.45
- Type
- journal article
- Language
- en
- Open access
- bronze
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- Vilenchik, M., Solit, D., Basso, A., Huezo, H., Lucas, B., He, H., Rosen, N., Spampinato, C., Modrich, P., & Chiosis, G. (2004). Targeting Wide-Range Oncogenic Transformation via PU24FCl, a Specific Inhibitor of Tumor Hsp90. Chemistry & Biology. https://doi.org/10.1016/j.chembiol.2004.04.008
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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