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Discovery and SAR of Novel 2,3-Dihydroimidazo[1,2-c]quinazoline PI3K Inhibitors: Identification of Copanlisib (BAY 80-6946).

Scott WJ, Hentemann MF, Rowley RB, Bull CO, Jenkins S, Bullion AM, Johnson J, Redman A, Robbins AH, Esler W, Fracasso RP, Garrison T, Hamilton M, Michels M, Wood JE, Wilkie DP, Xiao H, Levy J, Stasik E, Liu N, Schaefer M, Brands M, Lefranc J.

ChemMedChem. 2016 Jul 19;11(14):1517-30. doi: 10.1002/cmdc.201600148. Epub 2016 Jun 16.


Upregulated WDR26 serves as a scaffold to coordinate PI3K/ AKT pathway-driven breast cancer cell growth, migration, and invasion.

Ye Y, Tang X, Sun Z, Chen S.

Oncotarget. 2016 Apr 5;7(14):17854-69. doi: 10.18632/oncotarget.7439.


miR-101-2, miR-125b-2 and miR-451a act as potential tumor suppressors in gastric cancer through regulation of the PI3K/AKT/mTOR pathway.

Riquelme I, Tapia O, Leal P, Sandoval A, Varga MG, Letelier P, Buchegger K, Bizama C, Espinoza JA, Peek RM, Araya JC, Roa JC.

Cell Oncol (Dordr). 2016 Feb;39(1):23-33. doi: 10.1007/s13402-015-0247-3. Epub 2015 Oct 12.


Feedback suppression of PI3Kα signaling in PTEN-mutated tumors is relieved by selective inhibition of PI3Kβ.

Schwartz S, Wongvipat J, Trigwell CB, Hancox U, Carver BS, Rodrik-Outmezguine V, Will M, Yellen P, de Stanchina E, Baselga J, Scher HI, Barry ST, Sawyers CL, Chandarlapaty S, Rosen N.

Cancer Cell. 2015 Jan 12;27(1):109-22. doi: 10.1016/j.ccell.2014.11.008. Epub 2014 Dec 24.


PI-3 kinase p110β: a therapeutic target in advanced prostate cancers.

Li B, Sun A, Jiang W, Thrasher JB, Terranova P.

Am J Clin Exp Urol. 2014 Oct 2;2(3):188-98. eCollection 2014. Review.


Lentiviral vector-based insertional mutagenesis identifies genes involved in the resistance to targeted anticancer therapies.

Ranzani M, Annunziato S, Calabria A, Brasca S, Benedicenti F, Gallina P, Naldini L, Montini E.

Mol Ther. 2014 Dec;22(12):2056-68. doi: 10.1038/mt.2014.174. Epub 2014 Sep 8.


GSK-3 as potential target for therapeutic intervention in cancer.

McCubrey JA, Steelman LS, Bertrand FE, Davis NM, Sokolosky M, Abrams SL, Montalto G, D'Assoro AB, Libra M, Nicoletti F, Maestro R, Basecke J, Rakus D, Gizak A, Demidenko ZN, Cocco L, Martelli AM, Cervello M.

Oncotarget. 2014 May 30;5(10):2881-911. Review.


[3a,4]-Dihydropyrazolo[1,5a]pyrimidines: Novel, Potent, and Selective Phosphatidylinositol-3-kinase β Inhibitors.

Yu H, Moore ML, Erhard K, Hardwicke MA, Lin H, Luengo JI, McSurdy-Freed J, Plant R, Qu J, Raha K, Rominger CM, Schaber MD, Spengler MD, Rivero RA.

ACS Med Chem Lett. 2013 Jan 10;4(2):230-4. doi: 10.1021/ml300330m. eCollection 2013 Feb 14.


Selective anti-cancer agents as anti-aging drugs.

Blagosklonny MV.

Cancer Biol Ther. 2013 Dec;14(12):1092-7. doi: 10.4161/cbt.27350. Epub 2013 Nov 27.


Signaling via class IA Phosphoinositide 3-kinases (PI3K) in human, breast-derived cell lines.

Juvin V, Malek M, Anderson KE, Dion C, Chessa T, Lecureuil C, Ferguson GJ, Cosulich S, Hawkins PT, Stephens LR.

PLoS One. 2013 Oct 4;8(10):e75045. doi: 10.1371/journal.pone.0075045. eCollection 2013.


Advances in targeting signal transduction pathways.

McCubrey JA, Steelman LS, Chappell WH, Sun L, Davis NM, Abrams SL, Franklin RA, Cocco L, Evangelisti C, Chiarini F, Martelli AM, Libra M, Candido S, Ligresti G, Malaponte G, Mazzarino MC, Fagone P, Donia M, Nicoletti F, Polesel J, Talamini R, Bäsecke J, Mijatovic S, Maksimovic-Ivanic D, Michele M, Tafuri A, Dulińska-Litewka J, Laidler P, D'Assoro AB, Drobot L, Umezawa D, Montalto G, Cervello M, Demidenko ZN.

Oncotarget. 2012 Dec;3(12):1505-21. Review.


Ectopic NGAL expression can alter sensitivity of breast cancer cells to EGFR, Bcl-2, CaM-K inhibitors and the plant natural product berberine.

Chappell WH, Abrams SL, Franklin RA, LaHair MM, Montalto G, Cervello M, Martelli AM, Nicoletti F, Candido S, Libra M, Polesel J, Talamini R, Milella M, Tafuri A, Steelman LS, McCubrey JA.

Cell Cycle. 2012 Dec 1;11(23):4447-61. doi: 10.4161/cc.22786. Epub 2012 Nov 16.


Rapalogs in cancer prevention: anti-aging or anticancer?

Blagosklonny MV.

Cancer Biol Ther. 2012 Dec;13(14):1349-54. doi: 10.4161/cbt.22859. Epub 2012 Nov 14. Review.


Mutations and deregulation of Ras/Raf/MEK/ERK and PI3K/PTEN/Akt/mTOR cascades which alter therapy response.

McCubrey JA, Steelman LS, Chappell WH, Abrams SL, Montalto G, Cervello M, Nicoletti F, Fagone P, Malaponte G, Mazzarino MC, Candido S, Libra M, Bäsecke J, Mijatovic S, Maksimovic-Ivanic D, Milella M, Tafuri A, Cocco L, Evangelisti C, Chiarini F, Martelli AM.

Oncotarget. 2012 Sep;3(9):954-87. Review.


Abi1, a critical molecule coordinating actin cytoskeleton reorganization with PI-3 kinase and growth signaling.

Kotula L.

FEBS Lett. 2012 Aug 14;586(17):2790-4. doi: 10.1016/j.febslet.2012.05.015. Epub 2012 May 19. Review.


Prodrug strategy for PSMA-targeted delivery of TGX-221 to prostate cancer cells.

Zhao Y, Duan S, Zeng X, Liu C, Davies NM, Li B, Forrest ML.

Mol Pharm. 2012 Jun 4;9(6):1705-16. doi: 10.1021/mp3000309. Epub 2012 May 1.


Molecular damage in cancer: an argument for mTOR-driven aging.

Blagosklonny MV.

Aging (Albany NY). 2011 Dec;3(12):1130-41.


Recent progress in targeting cancer.

Demidenko ZN, McCubrey JA.

Aging (Albany NY). 2011 Dec;3(12):1154-62. Review.

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