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Items: 1 to 20 of 34

1.

Discovery and Pharmacological Characterization of Novel Quinazoline-Based PI3K Delta-Selective Inhibitors.

Hoegenauer K, Soldermann N, Stauffer F, Furet P, Graveleau N, Smith AB, Hebach C, Hollingworth GJ, Lewis I, Gutmann S, Rummel G, Knapp M, Wolf RM, Blanz J, Feifel R, Burkhart C, Zécri F.

ACS Med Chem Lett. 2016 Jun 2;7(8):762-7. doi: 10.1021/acsmedchemlett.6b00119. eCollection 2016 Aug 11.

PMID:
27563400
2.

Protein crystallization screens developed at the MRC Laboratory of Molecular Biology.

Gorrec F.

Drug Discov Today. 2016 May;21(5):819-25. doi: 10.1016/j.drudis.2016.03.008. Epub 2016 Mar 24. Review.

3.

Discovery of Bifunctional Oncogenic Target Inhibitors against Allosteric Mitogen-Activated Protein Kinase (MEK1) and Phosphatidylinositol 3-Kinase (PI3K).

Van Dort ME, Hong H, Wang H, Nino CA, Lombardi RL, Blanks AE, Galbán S, Ross BD.

J Med Chem. 2016 Mar 24;59(6):2512-22. doi: 10.1021/acs.jmedchem.5b01655. Epub 2016 Mar 15.

PMID:
26943489
4.

PI3K isoform-selective inhibitors: next-generation targeted cancer therapies.

Wang X, Ding J, Meng LH.

Acta Pharmacol Sin. 2015 Oct;36(10):1170-6. doi: 10.1038/aps.2015.71. Epub 2015 Sep 14. Review.

5.

Germline recessive mutations in PI4KA are associated with perisylvian polymicrogyria, cerebellar hypoplasia and arthrogryposis.

Pagnamenta AT, Howard MF, Wisniewski E, Popitsch N, Knight SJ, Keays DA, Quaghebeur G, Cox H, Cox P, Balla T, Taylor JC, Kini U.

Hum Mol Genet. 2015 Jul 1;24(13):3732-41. doi: 10.1093/hmg/ddv117. Epub 2015 Apr 8.

6.

Dual inhibition of allosteric mitogen-activated protein kinase (MEK) and phosphatidylinositol 3-kinase (PI3K) oncogenic targets with a bifunctional inhibitor.

Van Dort ME, Galbán S, Wang H, Sebolt-Leopold J, Whitehead C, Hong H, Rehemtulla A, Ross BD.

Bioorg Med Chem. 2015 Apr 1;23(7):1386-94. doi: 10.1016/j.bmc.2015.02.053. Epub 2015 Mar 6.

7.

Idelalisib: First-in-Class PI3K Delta Inhibitor for the Treatment of Chronic Lymphocytic Leukemia, Small Lymphocytic Leukemia, and Follicular Lymphoma.

Yang Q, Modi P, Newcomb T, Quéva C, Gandhi V.

Clin Cancer Res. 2015 Apr 1;21(7):1537-42. doi: 10.1158/1078-0432.CCR-14-2034. Epub 2015 Feb 10. Review.

8.

Structural, biochemical, and biophysical characterization of idelalisib binding to phosphoinositide 3-kinase δ.

Somoza JR, Koditek D, Villaseñor AG, Novikov N, Wong MH, Liclican A, Xing W, Lagpacan L, Wang R, Schultz BE, Papalia GA, Samuel D, Lad L, McGrath ME.

J Biol Chem. 2015 Mar 27;290(13):8439-46. doi: 10.1074/jbc.M114.634683. Epub 2015 Jan 28.

9.

The function of phosphatidylinositol 5-phosphate 4-kinase γ (PI5P4Kγ) explored using a specific inhibitor that targets the PI5P-binding site.

Clarke JH, Giudici ML, Burke JE, Williams RL, Maloney DJ, Marugan J, Irvine RF.

Biochem J. 2015 Mar 1;466(2):359-67. doi: 10.1042/BJ20141333.

10.

Simultaneous targeting of PI3Kδ and a PI3Kδ-dependent MEK1/2-Erk1/2 pathway for therapy in pediatric B-cell acute lymphoblastic leukemia.

Wang X, Zhang X, Li BS, Zhai X, Yang Z, Ding LX, Wang H, Liang C, Zhu W, Ding J, Meng LH.

Oncotarget. 2014 Nov 15;5(21):10732-44.

11.

Dominant-activating germline mutations in the gene encoding the PI(3)K catalytic subunit p110δ result in T cell senescence and human immunodeficiency.

Lucas CL, Kuehn HS, Zhao F, Niemela JE, Deenick EK, Palendira U, Avery DT, Moens L, Cannons JL, Biancalana M, Stoddard J, Ouyang W, Frucht DM, Rao VK, Atkinson TP, Agharahimi A, Hussey AA, Folio LR, Olivier KN, Fleisher TA, Pittaluga S, Holland SM, Cohen JI, Oliveira JB, Tangye SG, Schwartzberg PL, Lenardo MJ, Uzel G.

Nat Immunol. 2014 Jan;15(1):88-97. doi: 10.1038/ni.2771. Epub 2013 Oct 28.

12.

Phosphoinositides: tiny lipids with giant impact on cell regulation.

Balla T.

Physiol Rev. 2013 Jul;93(3):1019-137. doi: 10.1152/physrev.00028.2012. Review.

13.

L-Aminoacyl-triazine derivatives are isoform-selective PI3Kβ inhibitors that target non-conserved Asp862 of PI3Kβ

Pinson JA, Zheng Z, Miller MS, Chalmers DK, Jennings IG, Thompson PE.

ACS Med Chem Lett. 2013 Feb 14;4(2):206-210.

14.

Discovery of the novel mTOR inhibitor and its antitumor activities in vitro and in vivo.

Xie H, Lee MH, Zhu F, Reddy K, Huang Z, Kim DJ, Li Y, Peng C, Lim DY, Kang S, Jung SK, Li X, Li H, Ma W, Lubet RA, Ding J, Bode AM, Dong Z.

Mol Cancer Ther. 2013 Jun;12(6):950-8. doi: 10.1158/1535-7163.MCT-12-1241. Epub 2013 Mar 27.

15.

[18F]-FLT positron emission tomography can be used to image the response of sensitive tumors to PI3-kinase inhibition with the novel agent GDC-0941.

Cawthorne C, Burrows N, Gieling RG, Morrow CJ, Forster D, Gregory J, Radigois M, Smigova A, Babur M, Simpson K, Hodgkinson C, Brown G, McMahon A, Dive C, Hiscock D, Wilson I, Williams KJ.

Mol Cancer Ther. 2013 May;12(5):819-28. doi: 10.1158/1535-7163.MCT-12-0905. Epub 2013 Feb 20.

16.

Signaling by the phosphoinositide 3-kinase family in immune cells.

Okkenhaug K.

Annu Rev Immunol. 2013;31:675-704. doi: 10.1146/annurev-immunol-032712-095946. Epub 2013 Jan 16. Review.

17.

Dynamic steps in receptor tyrosine kinase mediated activation of class IA phosphoinositide 3-kinases (PI3K) captured by H/D exchange (HDX-MS).

Burke JE, Williams RL.

Adv Biol Regul. 2013 Jan;53(1):97-110. doi: 10.1016/j.jbior.2012.09.005. Epub 2012 Sep 13.

18.

Ras/Raf/MEK/ERK and PI3K/PTEN/Akt/mTOR cascade inhibitors: how mutations can result in therapy resistance and how to overcome resistance.

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

Oncotarget. 2012 Oct;3(10):1068-111. Review.

19.

The Therapeutic Potential for PI3K Inhibitors in Autoimmune Rheumatic Diseases.

Banham-Hall E, Clatworthy MR, Okkenhaug K.

Open Rheumatol J. 2012;6:245-58. doi: 10.2174/1874312901206010245. Epub 2012 Sep 7.

20.
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