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Items: 1 to 20 of 108

1.

Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.

Blake JF, Xu R, Bencsik JR, Xiao D, Kallan NC, Schlachter S, Mitchell IS, Spencer KL, Banka AL, Wallace EM, Gloor SL, Martinson M, Woessner RD, Vigers GP, Brandhuber BJ, Liang J, Safina BS, Li J, Zhang B, Chabot C, Do S, Lee L, Oeh J, Sampath D, Lee BB, Lin K, Liederer BM, Skelton NJ.

J Med Chem. 2012 Sep 27;55(18):8110-27. Epub 2012 Sep 18.

PMID:
22934575
2.

Targeting activated Akt with GDC-0068, a novel selective Akt inhibitor that is efficacious in multiple tumor models.

Lin J, Sampath D, Nannini MA, Lee BB, Degtyarev M, Oeh J, Savage H, Guan Z, Hong R, Kassees R, Lee LB, Risom T, Gross S, Liederer BM, Koeppen H, Skelton NJ, Wallin JJ, Belvin M, Punnoose E, Friedman LS, Lin K.

Clin Cancer Res. 2013 Apr 1;19(7):1760-72. doi: 10.1158/1078-0432.CCR-12-3072. Epub 2013 Jan 3.

3.

Microsecond molecular dynamics simulations provide insight into the ATP-competitive inhibitor-induced allosteric protection of Akt kinase phosphorylation.

Mou L, Cui T, Liu W, Zhang H, Cai Z, Lu S, Gao G.

Chem Biol Drug Des. 2017 May;89(5):723-731. doi: 10.1111/cbdd.12895. Epub 2016 Nov 24.

PMID:
27797456
4.

Developments in selective small molecule ATP-targeting the serine/threonine kinase Akt/PKB.

Wang P, Zhang L, Hao Q, Zhao G.

Mini Rev Med Chem. 2011 Nov;11(13):1093-107. Review.

PMID:
22353219
5.

DC120, a novel and potent inhibitor of AKT kinase, induces tumor cell apoptosis and suppresses tumor growth.

Deng R, Yang F, Chang SH, Tang J, Qin J, Feng GK, Ding K, Zhu XF.

Mol Pharmacol. 2012 Aug;82(2):189-98. doi: 10.1124/mol.111.077271. Epub 2012 May 2.

6.

Discovery of potent and selective inhibitors of the mammalian target of rapamycin (mTOR) kinase.

Nowak P, Cole DC, Brooijmans N, Bursavich MG, Curran KJ, Ellingboe JW, Gibbons JJ, Hollander I, Hu Y, Kaplan J, Malwitz DJ, Toral-Barza L, Verheijen JC, Zask A, Zhang WG, Yu K.

J Med Chem. 2009 Nov 26;52(22):7081-9. doi: 10.1021/jm9012642.

PMID:
19848404
7.

Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity.

Maira SM, Stauffer F, Brueggen J, Furet P, Schnell C, Fritsch C, Brachmann S, Chène P, De Pover A, Schoemaker K, Fabbro D, Gabriel D, Simonen M, Murphy L, Finan P, Sellers W, García-Echeverría C.

Mol Cancer Ther. 2008 Jul;7(7):1851-63. doi: 10.1158/1535-7163.MCT-08-0017. Epub 2008 Jul 7.

8.

Discovery of pyrrolopyrimidine inhibitors of Akt.

Blake JF, Kallan NC, Xiao D, Xu R, Bencsik JR, Skelton NJ, Spencer KL, Mitchell IS, Woessner RD, Gloor SL, Risom T, Gross SD, Martinson M, Morales TH, Vigers GP, Brandhuber BJ.

Bioorg Med Chem Lett. 2010 Oct 1;20(19):5607-12. doi: 10.1016/j.bmcl.2010.08.053. Epub 2010 Aug 13.

PMID:
20810279
9.

Discovery of 4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide (AZD5363), an orally bioavailable, potent inhibitor of Akt kinases.

Addie M, Ballard P, Buttar D, Crafter C, Currie G, Davies BR, Debreczeni J, Dry H, Dudley P, Greenwood R, Johnson PD, Kettle JG, Lane C, Lamont G, Leach A, Luke RW, Morris J, Ogilvie D, Page K, Pass M, Pearson S, Ruston L.

J Med Chem. 2013 Mar 14;56(5):2059-73. doi: 10.1021/jm301762v. Epub 2013 Feb 26.

PMID:
23394218
10.

Antitumor efficacy profile of PKI-402, a dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor.

Mallon R, Hollander I, Feldberg L, Lucas J, Soloveva V, Venkatesan A, Dehnhardt C, Delos Santos E, Chen Z, Dos Santos O, Ayral-Kaloustian S, Gibbons J.

Mol Cancer Ther. 2010 Apr;9(4):976-84. doi: 10.1158/1535-7163.MCT-09-0954. Epub 2010 Apr 6.

11.

Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).

Takeuchi CS, Kim BG, Blazey CM, Ma S, Johnson HW, Anand NK, Arcalas A, Baik TG, Buhr CA, Cannoy J, Epshteyn S, Joshi A, Lara K, Lee MS, Wang L, Leahy JW, Nuss JM, Aay N, Aoyama R, Foster P, Lee J, Lehoux I, Munagala N, Plonowski A, Rajan S, Woolfrey J, Yamaguchi K, Lamb P, Miller N.

J Med Chem. 2013 Mar 28;56(6):2218-34. doi: 10.1021/jm3007933. Epub 2013 Mar 7.

PMID:
23394126
12.

Docking of protein kinase B inhibitors: implications in the structure-based optimization of a novel scaffold.

Hernández-Campos A, Velázquez-Martínez I, Castillo R, López-Vallejo F, Jia P, Yu Y, Giulianotti MA, Medina-Franco JL.

Chem Biol Drug Des. 2010 Sep 1;76(3):269-76. doi: 10.1111/j.1747-0285.2010.01002.x. Epub 2010 Jun 22.

PMID:
20572809
13.

Evaluation and clinical analyses of downstream targets of the Akt inhibitor GDC-0068.

Yan Y, Serra V, Prudkin L, Scaltriti M, Murli S, Rodríguez O, Guzman M, Sampath D, Nannini M, Xiao Y, Wagle MC, Wu JQ, Wongchenko M, Hampton G, Ramakrishnan V, Lackner MR, Saura C, Roda D, Cervantes A, Tabernero J, Patel P, Baselga J.

Clin Cancer Res. 2013 Dec 15;19(24):6976-86. doi: 10.1158/1078-0432.CCR-13-0978. Epub 2013 Oct 18.

14.

Recent progress in the development of ATP-competitive and allosteric Akt kinase inhibitors.

Lindsley CW, Barnett SF, Yaroschak M, Bilodeau MT, Layton ME.

Curr Top Med Chem. 2007;7(14):1349-63. Review.

PMID:
17692025
15.

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
16.

Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.

Shallal HM, Russu WA.

Eur J Med Chem. 2011 Jun;46(6):2043-57. doi: 10.1016/j.ejmech.2011.02.057. Epub 2011 Mar 3.

PMID:
21429632
17.

Synthesis and structure-activity relationship of 3,4'-bispyridinylethylenes: discovery of a potent 3-isoquinolinylpyridine inhibitor of protein kinase B (PKB/Akt) for the treatment of cancer.

Li Q, Woods KW, Thomas S, Zhu GD, Packard G, Fisher J, Li T, Gong J, Dinges J, Song X, Abrams J, Luo Y, Johnson EF, Shi Y, Liu X, Klinghofer V, Des Jong R, Oltersdorf T, Stoll VS, Jakob CG, Rosenberg SH, Giranda VL.

Bioorg Med Chem Lett. 2006 Apr 1;16(7):2000-7. Epub 2006 Jan 18.

PMID:
16413780
18.

Preclinical pharmacology, antitumor activity, and development of pharmacodynamic markers for the novel, potent AKT inhibitor CCT128930.

Yap TA, Walton MI, Hunter LJ, Valenti M, de Haven Brandon A, Eve PD, Ruddle R, Heaton SP, Henley A, Pickard L, Vijayaraghavan G, Caldwell JJ, Thompson NT, Aherne W, Raynaud FI, Eccles SA, Workman P, Collins I, Garrett MD.

Mol Cancer Ther. 2011 Feb;10(2):360-71. doi: 10.1158/1535-7163.MCT-10-0760. Epub 2010 Dec 29.

19.

Discovery and optimization of a series of 3-(3-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amines: orally bioavailable, selective, and potent ATP-independent Akt inhibitors.

Ashwell MA, Lapierre JM, Brassard C, Bresciano K, Bull C, Cornell-Kennon S, Eathiraj S, France DS, Hall T, Hill J, Kelleher E, Khanapurkar S, Kizer D, Koerner S, Link J, Liu Y, Makhija S, Moussa M, Namdev N, Nguyen K, Nicewonger R, Palma R, Szwaya J, Tandon M, Uppalapati U, Vensel D, Volak LP, Volckova E, Westlund N, Wu H, Yang RY, Chan TC.

J Med Chem. 2012 Jun 14;55(11):5291-310. doi: 10.1021/jm300276x. Epub 2012 May 31.

PMID:
22533986
20.

Inhibition of tumor cell growth, proliferation and migration by X-387, a novel active-site inhibitor of mTOR.

Chen SM, Liu JL, Wang X, Liang C, Ding J, Meng LH.

Biochem Pharmacol. 2012 May 1;83(9):1183-94. doi: 10.1016/j.bcp.2012.01.019. Epub 2012 Jan 26.

PMID:
22305748

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