The DOI matches its Crossref record; 42 of the 42 references it cites were found in a registry or an index.
Characterization of an Akt Kinase Inhibitor with Potent Pharmacodynamic and Antitumor Activity
Open accessAbstract
Akt kinases 1, 2, and 3 are important regulators of cell survival and have been shown to be constitutively active in a variety of human tumors. GSK690693 is a novel ATP-competitive, low-nanomolar pan-Akt kinase inhibitor. It is selective for the Akt isoforms versus the majority of kinases in other families; however, it does inhibit additional members of the AGC kinase family. It causes dose-dependent reductions in the phosphorylation state of multiple proteins downstream of Akt, including GSK3β, PRAS40, and Forkhead. GSK690693 inhibited proliferation and induced apoptosis in a subset of tumor cells with potency consistent with intracellular inhibition of Akt kinase activity. In immune-compromised mice implanted with human BT474 breast carcinoma xenografts, a single i.p. administration of GSK690693 inhibited GSK3β phosphorylation in a dose- and time-dependent manner. After a single dose of GSK690693, >3 μmol/L drug concentration in BT474 tumor xenografts correlated with a sustained decrease in GSK3β phosphorylation. Consistent with the role of Akt in insulin signaling, treatment with GSK690693 resulted in acute and transient increases in blood glucose level. Daily administration of GSK690693 produced significant antitumor activity in mice bearing established human SKOV-3 ovarian, LNCaP prostate, and BT474 and HCC-1954 breast carcinoma xenografts. Immunohistochemical analysis of tumor xenografts after repeat dosing with GSK690693 showed reductions in phosphorylated Akt substrates in vivo. These results support further evaluation of GSK690693 as an anticancer agent. [Cancer Res 2008;68(7):2366–74]
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Cites
mTOR Inhibition Induces Upstream Receptor Tyrosine Kinase Signaling and Activates Akt
O'Reilly, K. E., Rojo, F., She, Q.-B., Solit, D., Mills, G. B., Smith, D., Lane, H., Hofmann, F., Hicklin, D. J., Ludwig, D. L., et al. (2006) · Cancer Research · doi:10.1158/0008-5472.can-05-2925 · Cited by 2,561
Expression profiling reveals off-target gene regulation by RNAi
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Exploiting the PI3K/AKT Pathway for Cancer Drug Discovery
Hennessy, B. T., Smith, D. L., Ram, P. T., Lu, Y., & Mills, G. B. (2005) · Nature Reviews Drug Discovery · doi:10.1038/nrd1902 · Cited by 2,185
Ras, PI(3)K and mTOR signalling controls tumour cell growth
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Growth retardation and increased apoptosis in mice with homozygous disruption of the akt1 gene
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Phosphorylation and inactivation of glycogen synthase kinase 3 by protein kinase A
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Cited by
AKT/PKB Signaling: Navigating the Network
Manning, B. D., & Toker, A. (2017) · Cell · doi:10.1016/j.cell.2017.04.001 · Cited by 3,772
Targeting the phosphoinositide 3-kinase pathway in cancer
Liu, P., Cheng, H., Roberts, T. M., & Zhao, J. J. (2009) · Nature Reviews Drug Discovery · doi:10.1038/nrd2926 · Cited by 2,721
Targeting PI3K signalling in cancer: opportunities, challenges and limitations
Engelman, J. A. (2009) · Nature Reviews Cancer · doi:10.1038/nrc2664 · Cited by 2,445
Targeting PI3K/Akt signal transduction for cancer therapy
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Metadata
- Authors
- Rhodes, N., Heerding, D. A., Duckett, D. R., Eberwein, D. J., Knick, V. B., Lansing, T. J., McConnell, R. T., Gilmer, T. M., Zhang, S.-Y., Robell, K., Kahana, J. A., Geske, R. S., Kleymenova, E. V., Choudhry, A. E., Lai, Z., Leber, J. D., Minthorn, E. A., Strum, S. L., Wood, E. R., Huang, P. S., Copeland, R. A., & Kumar, R.
- Venue
- Cancer Research
- Published
- 2008-04-01
- Volume
- 68
- Issue
- 7
- Pages
- 2366-2374
- ISSN
- 0008-5472 (ISSN-L)
- 1538-7445
- OpenAlex
- W2093345318
- Cited by
- 295
- References
- 42
- FWCI
- 9.43
- Type
- journal article
- Language
- en
- Open access
- bronze
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- Rhodes, N., Heerding, D. A., Duckett, D. R., Eberwein, D. J., Knick, V. B., Lansing, T. J., McConnell, R. T., Gilmer, T. M., Zhang, S.-Y., Robell, K., Kahana, J. A., Geske, R. S., Kleymenova, E. V., Choudhry, A. E., Lai, Z., Leber, J. D., Minthorn, E. A., Strum, S. L., Wood, E. R., . . . Kumar, R. (2008). Characterization of an Akt Kinase Inhibitor with Potent Pharmacodynamic and Antitumor Activity. Cancer Research. https://doi.org/10.1158/0008-5472.can-07-5783
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Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
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.
