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Antitumor efficacy of intermittent treatment schedules with the rapamycin derivative RAD001 correlates with prolonged inactivation of ribosomal protein S6 kinase 1 in peripheral blood mononuclear cells.

Boulay A, Zumstein-Mecker S, Stephan C, Beuvink I, Zilbermann F, Haller R, Tobler S, Heusser C, O'Reilly T, Stolz B, Marti A, Thomas G, Lane HA.

Cancer Res. 2004 Jan 1;64(1):252-61.


Identifying optimal biologic doses of everolimus (RAD001) in patients with cancer based on the modeling of preclinical and clinical pharmacokinetic and pharmacodynamic data.

Tanaka C, O'Reilly T, Kovarik JM, Shand N, Hazell K, Judson I, Raymond E, Zumstein-Mecker S, Stephan C, Boulay A, Hattenberger M, Thomas G, Lane HA.

J Clin Oncol. 2008 Apr 1;26(10):1596-602. doi: 10.1200/JCO.2007.14.1127. Epub 2008 Mar 10.


Phase I/II study of the mammalian target of rapamycin inhibitor everolimus (RAD001) in patients with relapsed or refractory hematologic malignancies.

Yee KW, Zeng Z, Konopleva M, Verstovsek S, Ravandi F, Ferrajoli A, Thomas D, Wierda W, Apostolidou E, Albitar M, O'Brien S, Andreeff M, Giles FJ.

Clin Cancer Res. 2006 Sep 1;12(17):5165-73.


Pharmacodynamic Evaluation of CCI-779, an Inhibitor of mTOR, in Cancer Patients.

Peralba JM, DeGraffenried L, Friedrichs W, Fulcher L, Gr├╝nwald V, Weiss G, Hidalgo M.

Clin Cancer Res. 2003 Aug 1;9(8):2887-92.


Comparative pharmacokinetics of RAD001 (everolimus) in normal and tumor-bearing rodents.

O'Reilly T, McSheehy PM, Kawai R, Kretz O, McMahon L, Brueggen J, Bruelisauer A, Gschwind HP, Allegrini PR, Lane HA.

Cancer Chemother Pharmacol. 2010 Mar;65(4):625-39. doi: 10.1007/s00280-009-1068-8. Epub 2009 Sep 27.


Mammalian target of rapamycin inhibitors rapamycin and RAD001 (everolimus) induce anti-proliferative effects in GH-secreting pituitary tumor cells in vitro.

Gorshtein A, Rubinfeld H, Kendler E, Theodoropoulou M, Cerovac V, Stalla GK, Cohen ZR, Hadani M, Shimon I.

Endocr Relat Cancer. 2009 Sep;16(3):1017-27. doi: 10.1677/ERC-08-0269. Epub 2009 Jun 9.


The rapamycin-derivative RAD001 (everolimus) inhibits cell viability and interacts with the Akt-mTOR-p70S6K pathway in human medullary thyroid carcinoma cells.

Grozinsky-Glasberg S, Rubinfeld H, Nordenberg Y, Gorshtein A, Praiss M, Kendler E, Feinmesser R, Grossman AB, Shimon I.

Mol Cell Endocrinol. 2010 Feb 5;315(1-2):87-94. doi: 10.1016/j.mce.2009.09.027. Epub 2009 Oct 6.


mTOR inhibitor RAD001 (everolimus) has antiangiogenic/vascular properties distinct from a VEGFR tyrosine kinase inhibitor.

Lane HA, Wood JM, McSheehy PM, Allegrini PR, Boulay A, Brueggen J, Littlewood-Evans A, Maira SM, Martiny-Baron G, Schnell CR, Sini P, O'Reilly T.

Clin Cancer Res. 2009 Mar 1;15(5):1612-22. doi: 10.1158/1078-0432.CCR-08-2057. Epub 2009 Feb 17.


Antiangiogenic therapy with mammalian target of rapamycin inhibitor RAD001 (Everolimus) increases radiosensitivity in solid cancer.

Manegold PC, Paringer C, Kulka U, Krimmel K, Eichhorn ME, Wilkowski R, Jauch KW, Guba M, Bruns CJ.

Clin Cancer Res. 2008 Feb 1;14(3):892-900. doi: 10.1158/1078-0432.CCR-07-0955.


The combination of novel low molecular weight inhibitors of RAF (LBT613) and target of rapamycin (RAD001) decreases glioma proliferation and invasion.

Hjelmeland AB, Lattimore KP, Fee BE, Shi Q, Wickman S, Keir ST, Hjelmeland MD, Batt D, Bigner DD, Friedman HS, Rich JN.

Mol Cancer Ther. 2007 Sep;6(9):2449-57. Epub 2007 Aug 31.


Phase I pharmacokinetic and pharmacodynamic study of the oral mammalian target of rapamycin inhibitor everolimus in patients with advanced solid tumors.

O'Donnell A, Faivre S, Burris HA 3rd, Rea D, Papadimitrakopoulou V, Shand N, Lane HA, Hazell K, Zoellner U, Kovarik JM, Brock C, Jones S, Raymond E, Judson I.

J Clin Oncol. 2008 Apr 1;26(10):1588-95. doi: 10.1200/JCO.2007.14.0988. Epub 2008 Mar 10.


Analysis of the pharmacodynamic activity of the mTOR inhibitor ridaforolimus (AP23573, MK-8669) in a phase 1 clinical trial.

Berk L, Mita MM, Kreisberg J, Bedrosian CL, Tolcher AW, Clackson T, Rivera VM.

Cancer Chemother Pharmacol. 2012 May;69(5):1369-77. doi: 10.1007/s00280-011-1813-7. Epub 2012 Jan 10.


S6K1 plays a key role in glial transformation.

Nakamura JL, Garcia E, Pieper RO.

Cancer Res. 2008 Aug 15;68(16):6516-23. doi: 10.1158/0008-5472.CAN-07-6188.


Monitoring antitumor efficacy of rapamycin in Kaposi sarcoma.

Di Paolo S, Teutonico A, Ranieri E, Gesualdo L, Schena PF.

Am J Kidney Dis. 2007 Mar;49(3):462-70.


Ribosomal protein S6 phosphorylation and function during late gestation liver development in the rat.

Boylan JM, Anand P, Gruppuso PA.

J Biol Chem. 2001 Nov 30;276(48):44457-63. Epub 2001 Sep 26.


A spectrophotometric assay for routine measurement of mammalian target of rapamycin activity in cell lysates.

Dekter HE, Romijn FP, Temmink WP, van Pelt J, de Fijter JW, Smit NP.

Anal Biochem. 2010 Aug;403(1-2):79-87. doi: 10.1016/j.ab.2010.04.022. Epub 2010 Apr 24.


Mammalian target of rapamycin, a molecular target in squamous cell carcinomas of the head and neck.

Amornphimoltham P, Patel V, Sodhi A, Nikitakis NG, Sauk JJ, Sausville EA, Molinolo AA, Gutkind JS.

Cancer Res. 2005 Nov 1;65(21):9953-61.

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