List of publications using GDC 0941 bismesylate (Axon 1377) purchased from Axon Medchem

(Total 33 publication citations updated until AUGUST-2017)

Brenner, A. K., Reikvam, H., Rye, K. P., Hagen, K. M., Lavecchia, A., & Bruserud, Ø. (2017). CDC25 Inhibition in Acute Myeloid Leukemia–A Study of Patient Heterogeneity and the Effects of Different Inhibitors. Molecules, 22(3), 446.

Albeck, J. G., Hung, Y. P., Teragawa, C., Pargett, M., Gillies, T. E., Minguet, M., ... & Yellen, G. (2017). Akt regulation of glycolysis mediates bioenergetic stability in epithelial cells. bioRxiv, 126771.
(BEZ235, GDC0941, BMK120 and Gefitinib from Axon Medchem)

Bago, R., Sommer, E., Castel, P., Crafter, C., Bailey, F. P., Shpiro, N., ... & Alessi, D. R. (2016). The hVps34‐SGK3 pathway alleviates sustained PI3K/Akt inhibition by stimulating mTORC1 and tumour growth. The EMBO journal, 35(17), 1902-1922.

Ross, R. L., McPherson, H. R., Kettlewell, L., Shnyder, S. D., Hurst, C. D., Alder, O., & Knowles, M. A. (2016). PIK3CA dependence and sensitivity to therapeutic targeting in urothelial carcinoma. BMC cancer, 16(1), 553.

Bhatia, D. R., & Thiagarajan, P. (2016). Combination effects of sorafenib with PI3K inhibitors under hypoxia in colorectal cancer. Hypoxia, 4, 163.
(*Sorafenib, BEZ235, and GDC0941 from AXON)

Alonso-Curbelo, Direna, et al. "RAB7 counteracts PI3K-driven macropinocytosis activated at early stages of melanoma development." Oncotarget 6.14 (2015): 11848. 

Gao, Juehua, et al. "Flow cytometric detection of altered signaling in myelodysplastic syndrome and cytopenia." Leukemia research 39.12 (2015): 1396-1404. 

Bruserud, Øystein, et al. "Expression of the potential therapeutic target CXXC5 in primary acute myeloid leukemia cells-high expression is associated with adverse prognosis as well as altered intracellular signaling and transcriptional regulation." Oncotarget 6.5 (2015): 2794. 

Alliouachene, Samira, et al. "Inactivation of the class II PI3K-C2β potentiates insulin signaling and sensitivity." Cell reports 13.9 (2015): 1881-1894. 

Bago, Ruzica, et al. "Characterization ofVPS34-IN1, a selective inhibitor of Vps34, reveals that the phosphatidylinositol 3-phosphate-bindingSGK3 protein kinase is a downstream target of classIIIphosphoinositide 3-kinase." Biochemical Journal 463.3 (2014): 413-427. 

Costales, Abran Q., et al. "Compounds and compositions as protein kinase inhibitors."U.S.Patent No. 8,859,548.14 Oct. 2014.
*PD0325901, PD184352, SL327, LY294002, PI103,PIK75,PIK90,GDC0941, BEX235, AS252424,TGX221 are from Axon Medchem 

Schuler, Walter, Frank P. Stegmeier, and Markus Warmuth. "Use of a PKC inhibitor."U.S.Patent No. 8,748,428.10 Jun. 2014.
* LY294002, PI103,PIK75,PIK90, AS252424,TGX221,GDC0941 are from Axon Medchem. 

Guo, Huifang, et al. "Coordinate phosphorylation of multiple residues on single AKT1 and AKT2 molecules." Oncogene 33.26 (2014): 3463-3472.  

Gao, Meng, et al. "Site-specific activation of AKT protects cells from death induced by glucose deprivation." Oncogene 33.6 (2014): 745-755. 

Haydn, Johannes M., et al. "The MAPK pathway as an apoptosis enhancer in melanoma." Oncotarget 5.13 (2014): 5040-5053.
*PD184352 andGDC0941 were purchased from Axon Medchem 

Antileukaemic effect of PI3K-mTOR inhibitors in acute myeloid leukaemia-gene expression profiles reveal CDC25B expression as determinate of pharmacological effect.
H Reikvam, J Tamburini, S Skrede, R Holdhus, L Poulain, E Ersvær, KJ Hatfield, Ø Bruserud.
Br. J. Haematol. 2014, 164(2), 200-211.  DOI: 10.1111/bjh.12611

Binge Alcohol Drinking by Mice Requires Intact Group1 Metabotropic Glutamate Receptor Signaling Within the Central Nucleus of the Amygdale. 
Cozzoli, D. K., Courson, J., Wroten, M. G., Greentree, D. I., Lum, E. N., Campbell, R. R., ... & Szumlinski, K. K. (2014). -
Neuropsychopharmacology, 2014, 39(2), 435-444.

Transient anti-angiogenic treatment improves delivery of cytotoxic compounds and therapeutic outcome in lung cancer.
S Chatterjee, C Wieczorek, J Schottle, M Siobal, Y Hinze, T Franz, A Florin, J Adamczak, L Heukamp, B Neumaiaer, RT Ullrich.
Cancer Research, 2014, on March 27, 2014; DOI: 10.1158/0008-5472.CAN-13-2986 

RASA1 functions in EPHB4 signaling pathway to suppress endothelial mTORC1 activity.
J Kawasaki, S Aegerter, RD Fevurly, A Mammoto, T Mammoto, M Sahin, JD Mably, SJ Fishman and J Chan.
J Clin Invest. 2014, doi:10.1172/JCI67084.
Read more:
*GDC0941 andBEZ235 from Axon Medchem  

PDK1 Signaling Towards PLK1-Myc Activation Confers Oncogenic Transformation and Tumor Initiating Cell Activation and Resistance to mTOR-targeted Therapy.
J Tan, Z Li, PL Lee, P Guan, MY Aau, ST Lee, M Feng, CZ Lim, EYJ Lee, ZN Wee, YC Lim, RKM Karuturi and Q Yu.
Cancer Discovery, Published Online July 25, 2013.
Read more:
... 60 inhibitors including GDC0941 were purchased from Axon Medchem  

Effects of Isoform-Selective Phosphatidylinositol 3-Kinase Inhibitors on Osteoclasts: ACTIONS ON CYTOSKELETAL ORGANIZATION, SURVIVAL ANDRESORPTION.
RPP Shugg, A Thomson, N Tanabe, A Kashishian, BH Steiner, KD Puri, A Pereverzev, BJ Lannutti, FR Jirik, SJ Dixon1 and SM Sims.
J. Biol. Chem. 2013. doi: 10.1074/jbc.M113.507525.
Read more:
...GDC0941 bismesylate (1377),TGX221 (1417), AS252424 (1424) andPIK75 (1334) were purchased from Axon MedChem.  

Coordinate phosphorylation of multiple residues on single AKT1 and AKT2 molecules. 
Guo, H., Gao, M., Lu, Y., Liang, J., Lorenzi, P. L., Bai, S., ... & Ding, Z. (2013). 
Oncogene, 1, 10.

Site-specific activation of AKT protects cells from death induced by glucose deprivation.
M Gao, J Liang, Y Lu, H Guo, P German, S Bai, E Jonasch, X Yang, GB Mills and Z Ding.
Oncogene, (11 February 2013). DOI:10.1038/onc.2013.2  

AM Madera, D Poon, A Smith - U.S. Patent 20,130,096,149, issued April 18, 2013.
(10 drugs from Axon Medchem have been tested) 

AMP-dependent kinase/mammalian target of rapamycin complex 1 signaling in T-cell acute lymphoblastic leukemia: therapeutic implications.
C Grimaldi, F Chiarini, G Tabellini, F Ricci, PL Tazzari, M Battistelli, E Falcieri, R Bortul, F Melchionda, I Iacobucci, P Pagliaro, G Martinelli, A Pession, JT Barata, JA McCubrey, AM Martelli.
Leukemia, 2012, 26, 91–100.   DOI:10.1038/leu.2011.269.  

Akt and ERK Control the Proliferative Response of Mammary Epithelial Cells to the Growth Factors IGF-1 and EGF Through the Cell Cycle Inhibitor p57Kip2.
DT Worster, T Schmelzle, N.L Solimini, ES Lightcap, B Millard, GB Mills, JS Brugge, JG Albeck,. 
Science Signal. 2012, 5, ra19. DOI: 10.1126/scisignal.2001986   

Genetic disruption of the PI3K regulatory subunits, p85α, p55α, and p50α, normalizes mutant PTPN11-induced hypersensitivity to GM-CSF.
CB Goodwin, Z Yang, F Yin, M Yu, RJ Chan.
Haematol, 2012, 97(7), 1042-1047.  DOI: 10.3324/haematol.2011.046896   

The p110α and p110β isoforms of PI3K play divergent roles in mammary gland development and tumorigenesis.
T Utermark, T Rao, H Cheng, Q Wang, SH Lee, ZC Wang, JD Iglehart, TM Roberts, WJ Muller, JJ Zhao.
Genes & Dev. 2012, 26, 1573-1586.  doi: 10.1101/gad.191973.112  

Compounds and Compositions as Protein Kinase Inhibitors.
AQ Costales, S Huang, J Jin, Z Liu, S Pecchi, D Poon, J Tellew, Q Zhang.
US Patent Application 20120225899.  

Compounds and compositions as protein kinase inhibitors.
AQ Costales, S Huang, JX Jin, Z Liu, S Pecchi, D Poon, J Tellew, and Q Zhang.
U.S. Patent 8,242,260, issuedAugust 14, 2012.   

PI3K inhibition results in enhanced HER signaling and acquired ERK dependency in HER2-overexpressing breast cancer.
V Serra, M Scaltriti, L Prudkin, PJA Eichhorn, YH Ibrahim, S Chandarlapaty, B Markman, O Rodriguez, M Guzman, S Rodriguez, M Gili, M Russillo, JL Parra, S Singh, J Arribas, N Rosen, J Baselga.
Oncogene, 2011, 30, 2547–2557.  DOI:10.1038/onc.2010.626. 

Physical Association of PDK1 with AKT1 Is Sufficient for Pathway Activation Independent of Membrane Localization and Phosphatidylinositol 3 Kinase.
Z Ding, J Liang, J Li, Y Lu, V Ariyaratna, Z Lu, MA Davies, JK Westwick, GB Mills.  
PLoS ONE 2010, 5(3): e9910.  doi:10.1371/journal.pone.0009910  

High-Throughput Screening Compatible Cell-Based Assay for Interrogating Activated Notch Signaling.
MK Hancock, L Kopp, K Bi.
Assay & Drug Devel. Tech. 2009, 7(1), 68-79. DOI:10.1089/adt.2008.173 

(This is an incomplete list, udated AUGUST-2017)

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