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Data from Combination of Farnesyltransferase and Akt Inhibitors Is Synergistic in Breast Cancer Cells and Causes Significant Breast Tumor Regression in ErbB2 Transgenic Mice

Autor: Saïd M. Sebti, Jin Q. Cheng, Andrew D. Hamilton, Domenico Coppola, William J. Fulp, Y. Ann Chen, Kara D. Forinash, Maria E. Balasis

The Akt activation inhibitor triciribine and the farnesyltransferase inhibitor tipifarnib have modest to little activity in clinical trials when used as single agents. In this article, preclinical data show that the combination is more effective than

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7e0895cd4b3d0ea341e7f26ac360ffdb
https://doi.org/10.1158/1078-0432.c.6519345

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Supplementary Figure 2 from RKI-1447 Is a Potent Inhibitor of the Rho-Associated ROCK Kinases with Anti-Invasive and Antitumor Activities in Breast Cancer

Autor: Saïd M. Sebti, Nicholas J. Lawrence, Ernst Schönbrunn, Mathew P. Martin, Nan Sun, Ying Sun, Roberta Pireddu, Kara D. Forinash, Ronil A. Patel

PDF file, 64K, Effect of RKI-1447 and RKI-1313 on anchorage dependent proliferation/survival of MDA-MB-231 cells. Cells were seeded in a 96-well plate and treated with increasing concentrations of RKI-1447 or RKI-1313. The effects of the compounds on

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::12283faddd80f040d4fcd387d6eda5d8
https://doi.org/10.1158/0008-5472.22395777

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Supplementary Table 2 from RKI-1447 Is a Potent Inhibitor of the Rho-Associated ROCK Kinases with Anti-Invasive and Antitumor Activities in Breast Cancer

Autor: Saïd M. Sebti, Nicholas J. Lawrence, Ernst Schönbrunn, Mathew P. Martin, Nan Sun, Ying Sun, Roberta Pireddu, Kara D. Forinash, Ronil A. Patel

PDF file, 58K, Percent tumor volume change after mouse treatment with vehicle. ErbB2 mammary tumor transgenic mice were treated with Vehicle (20% HPCD) as described under Materials and Methods. Percent change in tumor volume was calculated for each t

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::010cd8795a78124402a30c017fde77c6
https://doi.org/10.1158/0008-5472.22395765

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Supplementary Table 4 from RKI-1447 Is a Potent Inhibitor of the Rho-Associated ROCK Kinases with Anti-Invasive and Antitumor Activities in Breast Cancer

Autor: Saïd M. Sebti, Nicholas J. Lawrence, Ernst Schönbrunn, Mathew P. Martin, Nan Sun, Ying Sun, Roberta Pireddu, Kara D. Forinash, Ronil A. Patel

PDF file, 56K, Percent mouse weight change after vehicle treatment. ErbB2 mammary tumor transgenic mice were treated with Vehicle (20% HPCD) as described under Materials and Methods. Final percent change in weight was calculated for each mouse using

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::08b036d791eed5cc9092b87753bb1603
https://doi.org/10.1158/0008-5472.22395759.v1

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Supplementary Table 3 from RKI-1447 Is a Potent Inhibitor of the Rho-Associated ROCK Kinases with Anti-Invasive and Antitumor Activities in Breast Cancer

Autor: Saïd M. Sebti, Nicholas J. Lawrence, Ernst Schönbrunn, Mathew P. Martin, Nan Sun, Ying Sun, Roberta Pireddu, Kara D. Forinash, Ronil A. Patel

PDF file, 59K, Percent mouse weight change after RKI-1447 treatment. ErbB2 mammary tumor transgenic mice were treated with RKI-1447 as described under Materials and Methods. Final percent change in weight was calculated for each mouse using the follo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cc0b7387632b7e2eb8ac99e920405251
https://doi.org/10.1158/0008-5472.22395762.v1

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Supplementary Figure 4 from RKI-1447 Is a Potent Inhibitor of the Rho-Associated ROCK Kinases with Anti-Invasive and Antitumor Activities in Breast Cancer

Autor: Saïd M. Sebti, Nicholas J. Lawrence, Ernst Schönbrunn, Mathew P. Martin, Nan Sun, Ying Sun, Roberta Pireddu, Kara D. Forinash, Ronil A. Patel

PDF file, 131K, Molecular mode of action of RKI-1447. Interaction of the ATP site of Rock1 kinase in complex with RKI-1447 determined by X-ray crystallography at 2.9 � resolution. The hinge region is indicated in orange, the DFG motif in cyan, and

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8a41899a6a8e1f8c37629cfa88c9950c
https://doi.org/10.1158/0008-5472.22395771.v1

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Supplementary Figure 1 from RKI-1447 Is a Potent Inhibitor of the Rho-Associated ROCK Kinases with Anti-Invasive and Antitumor Activities in Breast Cancer

Autor: Saïd M. Sebti, Nicholas J. Lawrence, Ernst Schönbrunn, Mathew P. Martin, Nan Sun, Ying Sun, Roberta Pireddu, Kara D. Forinash, Ronil A. Patel

PDF file, 93K, RKI-1447 inhibits the phosphorylation of the ROCK substrates MLC-2 and MYPT-1 in human breast cancer cells. MDA-MB-231 and MDA-MB-468 breast cancer cells were treated with either vehicle or RKI-1447 for 1 hour and processed for western

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::12a25bebf05e5949478030065dfb71a8
https://doi.org/10.1158/0008-5472.22395780.v1

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Supplementary Table 1 from RKI-1447 Is a Potent Inhibitor of the Rho-Associated ROCK Kinases with Anti-Invasive and Antitumor Activities in Breast Cancer

Autor: Saïd M. Sebti, Nicholas J. Lawrence, Ernst Schönbrunn, Mathew P. Martin, Nan Sun, Ying Sun, Roberta Pireddu, Kara D. Forinash, Ronil A. Patel

PDF file, 64K, Percent tumor volume change after RKI-1447 treatment of ErbB2 mammary tumor transgenic mice. ErbB2 mammary tumor transgenic mice were treated with RKI-1447 as described under Materials and Methods. Percent change in tumor volume was ca

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6b8dbad2a8b3b4926ca43a3b91fd80fd
https://doi.org/10.1158/0008-5472.22395768.v1

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Data from RKI-1447 Is a Potent Inhibitor of the Rho-Associated ROCK Kinases with Anti-Invasive and Antitumor Activities in Breast Cancer

Autor: Saïd M. Sebti, Nicholas J. Lawrence, Ernst Schönbrunn, Mathew P. Martin, Nan Sun, Ying Sun, Roberta Pireddu, Kara D. Forinash, Ronil A. Patel

The Rho-associated kinases ROCK1 and ROCK2 are critical for cancer cell migration and invasion, suggesting they may be useful therapeutic targets. In this study, we describe the discovery and development of RKI-1447, a potent small molecule inhibitor

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6ef365ddb9c892a1d7f06100c828baad
https://doi.org/10.1158/0008-5472.c.6504393.v1

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