The DOI matches its Crossref record; 3 of the 3 references it cites were found in a registry or an index.
Novel Small Molecule Inhibitors of 3-Phosphoinositide-dependent Kinase-1
Open accessAbstract
The phosphoinositide 3-kinase/3-phosphoinositide-dependent kinase 1 (PDK1)/Akt signaling pathway plays a key role in cancer cell growth, survival, and tumor angiogenesis and represents a promising target for anticancer drugs. Here, we describe three potent PDK1 inhibitors, BX-795, BX-912, and BX-320 (IC(50) = 11-30 nm) and their initial biological characterization. The inhibitors blocked PDK1/Akt signaling in tumor cells and inhibited the anchorage-dependent growth of a variety of tumor cell lines in culture or induced apoptosis. A number of cancer cell lines with elevated Akt activity were >30-fold more sensitive to growth inhibition by PDK1 inhibitors in soft agar than on tissue culture plastic, consistent with the cell survival function of the PDK1/Akt signaling pathway, which is particularly important for unattached cells. BX-320 inhibited the growth of LOX melanoma tumors in the lungs of nude mice after injection of tumor cells into the tail vein. The effect of BX-320 on cancer cell growth in vitro and in vivo indicates that PDK1 inhibitors may have clinical utility as anticancer agents.
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Cites
Phosphorylation and regulation of Akt/PKB by the rictor-mTOR complex
Sarbassov, D. D., Guertin, D. A., Ali, S. M., & Sabatini, D. M. (2005) · Science · doi:10.1126/science.1106148 · Cited by 6,216
Phosphorylation and Activation of p70 s6k by PDK1
Pullen, N., Dennis, P. B., Andjelkovic, M., Dufner, A., Kozma, S. C., Hemmings, B. A., & Thomas, G. (1998) · Science · doi:10.1126/science.279.5351.707 · Cited by 826
Ribosomal S6 Kinase Signaling and the Control of Translation
Dufner, A., & Thomas, G. (1999) · Experimental Cell Research · doi:10.1006/excr.1999.4683 · Cited by 676
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Feldman, M. E., Apsel, B., Uotila, A., Loewith, R., Knight, Z. A., Ruggero, D., & Shokat, K. M. (2009) · PLoS Biology · doi:10.1371/journal.pbio.1000038 · Cited by 1,082
Chappell, W. H., Steelman, L. S., Long, J. M., Kempf, R. C., Abrams, S. L., Franklin, R. A., Bäsecke, J., Stivala, F., Donia, M., Fagone, P., et al. (2011) · Oncotarget · doi:10.18632/oncotarget.240 · Cited by 510
Drug discovery approaches targeting the PI3K/Akt pathway in cancer
Garcia-Echeverria, C., & Sellers, W. R. (2008) · Oncogene · doi:10.1038/onc.2008.246 · Cited by 473
Inhibitor hijacking of Akt activation
Okuzumi, T., Fiedler, D., Zhang, C., Gray, D. C., Aizenstein, B., Hoffman, R., & Shokat, K. M. (2009) · Nature Chemical Biology · doi:10.1038/nchembio.183 · Cited by 294
New Roles for the LKB1-NUAK Pathway in Controlling Myosin Phosphatase Complexes and Cell Adhesion
Zagórska, A., Deak, M., Campbell, D. G., Banerjee, S., Hirano, M., Aizawa, S., Prescott, A. R., & Alessi, D. R. (2010) · Science Signaling · doi:10.1126/scisignal.2000616 · Cited by 193
Metadata
- Authors
- Feldman, R. I., Wu, J. M., Polokoff, M. A., Kochanny, M. J., Dinter, H., Zhu, D., Biroc, S. L., Alicke, B., Bryant, J., Yuan, S., Buckman, B. O., Lentz, D., Ferrer, M., Whitlow, M., Adler, M., Finster, S., Chang, Z., & Arnaiz, D. O.
- Venue
- Journal of Biological Chemistry
- Publisher
- Elsevier BV
- Published
- 2005-05
- Volume
- 280
- Issue
- 20
- Pages
- 19867-19874
- ISSN
- 0021-9258 (ISSN-L)
- OpenAlex
- W2106293966
- Cited by
- 228
- References
- 3
- FWCI
- 3.11
- Type
- journal article
- Language
- en
- Open access
- hybrid
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- Feldman, R. I., Wu, J. M., Polokoff, M. A., Kochanny, M. J., Dinter, H., Zhu, D., Biroc, S. L., Alicke, B., Bryant, J., Yuan, S., Buckman, B. O., Lentz, D., Ferrer, M., Whitlow, M., Adler, M., Finster, S., Chang, Z., & Arnaiz, D. O. (2005). Novel Small Molecule Inhibitors of 3-Phosphoinositide-dependent Kinase-1. Journal of Biological Chemistry. https://doi.org/10.1074/jbc.m501367200
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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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