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Items: 1 to 20 of 95

1.

Recent advances in the development of selective, ATP-competitive inhibitors of mTOR.

Richard DJ, Verheijen JC, Zask A.

Curr Opin Drug Discov Devel. 2010 Jul;13(4):428-40. Review.

PMID:
20597028
2.

Discovery of 3,6-dihydro-2H-pyran as a morpholine replacement in 6-aryl-1H-pyrazolo[3,4-d]pyrimidines and 2-arylthieno[3,2-d]pyrimidines: ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR).

Kaplan J, Verheijen JC, Brooijmans N, Toral-Barza L, Hollander I, Yu K, Zask A.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):640-3. doi: 10.1016/j.bmcl.2009.11.050. Epub 2009 Dec 4.

PMID:
19963384
3.

ATP-competitive inhibitors of the mammalian target of rapamycin: design and synthesis of highly potent and selective pyrazolopyrimidines.

Zask A, Verheijen JC, Curran K, Kaplan J, Richard DJ, Nowak P, Malwitz DJ, Brooijmans N, Bard J, Svenson K, Lucas J, Toral-Barza L, Zhang WG, Hollander I, Gibbons JJ, Abraham RT, Ayral-Kaloustian S, Mansour TS, Yu K.

J Med Chem. 2009 Aug 27;52(16):5013-6. doi: 10.1021/jm900851f.

PMID:
19645448
4.

Functional consequences of mTOR inhibition.

Sudarsanam S, Johnson DE.

Curr Opin Drug Discov Devel. 2010 Jan;13(1):31-40. Review.

PMID:
20047144
5.

Mammalian target of rapamycin: discovery of rapamycin reveals a signaling pathway important for normal and cancer cell growth.

Gibbons JJ, Abraham RT, Yu K.

Semin Oncol. 2009 Dec;36 Suppl 3:S3-S17. doi: 10.1053/j.seminoncol.2009.10.011. Review.

PMID:
19963098
6.

Beyond rapalog therapy: preclinical pharmacology and antitumor activity of WYE-125132, an ATP-competitive and specific inhibitor of mTORC1 and mTORC2.

Yu K, Shi C, Toral-Barza L, Lucas J, Shor B, Kim JE, Zhang WG, Mahoney R, Gaydos C, Tardio L, Kim SK, Conant R, Curran K, Kaplan J, Verheijen J, Ayral-Kaloustian S, Mansour TS, Abraham RT, Zask A, Gibbons JJ.

Cancer Res. 2010 Jan 15;70(2):621-31. doi: 10.1158/0008-5472.CAN-09-2340. Epub 2010 Jan 12.

7.

ATP-competitive inhibitors of mTOR: an update.

Schenone S, Brullo C, Musumeci F, Radi M, Botta M.

Curr Med Chem. 2011;18(20):2995-3014. Review.

PMID:
21651476
8.

Biochemical, cellular, and in vivo activity of novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin.

Yu K, Toral-Barza L, Shi C, Zhang WG, Lucas J, Shor B, Kim J, Verheijen J, Curran K, Malwitz DJ, Cole DC, Ellingboe J, Ayral-Kaloustian S, Mansour TS, Gibbons JJ, Abraham RT, Nowak P, Zask A.

Cancer Res. 2009 Aug 1;69(15):6232-40. doi: 10.1158/0008-5472.CAN-09-0299. Epub 2009 Jul 7.

9.

Novel imidazolopyrimidines as dual PI3-Kinase/mTOR inhibitors.

Venkatesan AM, Dehnhardt CM, Chen Z, Santos ED, Dos Santos O, Bursavich M, Gilbert AM, Ellingboe JW, Ayral-Kaloustian S, Khafizova G, Brooijmans N, Mallon R, Hollander I, Feldberg L, Lucas J, Yu K, Gibbons J, Abraham R, Mansour TS.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):653-6. doi: 10.1016/j.bmcl.2009.11.057. Epub 2009 Dec 1.

PMID:
19954970
10.

Novel purine and pyrazolo[3,4-d]pyrimidine inhibitors of PI3 kinase-alpha: Hit to lead studies.

Gilbert AM, Nowak P, Brooijmans N, Bursavich MG, Dehnhardt C, Santos ED, Feldberg LR, Hollander I, Kim S, Lombardi S, Park K, Venkatesan AM, Mallon R.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):636-9. doi: 10.1016/j.bmcl.2009.11.051. Epub 2009 Dec 5.

PMID:
19969455
11.

Inhibition of mammalian target of rapamycin induces phosphatidylinositol 3-kinase-dependent and Mnk-mediated eukaryotic translation initiation factor 4E phosphorylation.

Wang X, Yue P, Chan CB, Ye K, Ueda T, Watanabe-Fukunaga R, Fukunaga R, Fu H, Khuri FR, Sun SY.

Mol Cell Biol. 2007 Nov;27(21):7405-13. Epub 2007 Aug 27.

12.

Pyrazolopyrimidines as highly potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 1-substituent.

Curran KJ, Verheijen JC, Kaplan J, Richard DJ, Toral-Barza L, Hollander I, Lucas J, Ayral-Kaloustian S, Yu K, Zask A.

Bioorg Med Chem Lett. 2010 Feb 15;20(4):1440-4. doi: 10.1016/j.bmcl.2009.12.086. Epub 2010 Jan 4.

PMID:
20089401
13.

WJD008, a dual phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin inhibitor, prevents PI3K signaling and inhibits the proliferation of transformed cells with oncogenic PI3K mutant.

Li T, Wang J, Wang X, Yang N, Chen SM, Tong LJ, Yang CH, Meng LH, Ding J.

J Pharmacol Exp Ther. 2010 Sep 1;334(3):830-8. doi: 10.1124/jpet.110.167940. Epub 2010 Jun 3.

14.

The mTOR pathway: a new target in cancer therapy.

Ciuffreda L, Di Sanza C, Incani UC, Milella M.

Curr Cancer Drug Targets. 2010 Aug;10(5):484-95. Review.

PMID:
20384580
15.

Raptor-rictor axis in TGFbeta-induced protein synthesis.

Das F, Ghosh-Choudhury N, Mahimainathan L, Venkatesan B, Feliers D, Riley DJ, Kasinath BS, Choudhury GG.

Cell Signal. 2008 Feb;20(2):409-23. Epub 2007 Nov 7.

PMID:
18068336
16.

mTOR inhibitor/proliferation signal inhibitors: entering or leaving the field?

Rostaing L, Kamar N.

J Nephrol. 2010 Mar-Apr;23(2):133-42. Review.

PMID:
20155724
17.

Dissecting the role of mTOR: lessons from mTOR inhibitors.

Dowling RJ, Topisirovic I, Fonseca BD, Sonenberg N.

Biochim Biophys Acta. 2010 Mar;1804(3):433-9. doi: 10.1016/j.bbapap.2009.12.001. Epub 2009 Dec 11. Review.

PMID:
20005306
18.

Targeting the PI3K/AKT/mTOR signaling network in acute myelogenous leukemia.

Martelli AM, Evangelisti C, Chiarini F, Grimaldi C, Manzoli L, McCubrey JA.

Expert Opin Investig Drugs. 2009 Sep;18(9):1333-49. doi: 10.1517/14728220903136775. Review.

PMID:
19678801
19.

4-Substituted-7-azaindoles bearing a ureidobenzofuranone moiety as potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR).

Tsou HR, MacEwan G, Birnberg G, Zhang N, Brooijmans N, Toral-Barza L, Hollander I, Ayral-Kaloustian S, Yu K.

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2259-63. doi: 10.1016/j.bmcl.2010.02.012. Epub 2010 Feb 6.

PMID:
20188551
20.

Compensatory activation of Akt in response to mTOR and Raf inhibitors - a rationale for dual-targeted therapy approaches in neuroendocrine tumor disease.

Zitzmann K, Rüden Jv, Brand S, Göke B, Lichtl J, Spöttl G, Auernhammer CJ.

Cancer Lett. 2010 Sep 1;295(1):100-9. doi: 10.1016/j.canlet.2010.02.018. Epub 2010 Mar 30.

PMID:
20356670

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