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2008 4
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103 results

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Page 1
Inhibitor GSK690693 extends Drosophila lifespan via reduce AKT signaling pathway.
Cheng X, Xie M, Luo L, Tian Y, Yu G, Wu Q, Fan X, Yang D, Mao X, Gaur U, Yang M. Cheng X, et al. Mech Ageing Dev. 2022 Mar;202:111633. doi: 10.1016/j.mad.2022.111633. Epub 2022 Jan 20. Mech Ageing Dev. 2022. PMID: 35065134
Furthermore, GSK690693 treatment reduced the activation of AKT and ERK, consequently activating FOXO, GSK-3beta and apoptosis to modulate longevity of flies. Remarkably, GSK690693 did not induce hyperglycemia after treatment. The results indicate that GSK690693
Furthermore, GSK690693 treatment reduced the activation of AKT and ERK, consequently activating FOXO, GSK-3beta and apoptosis to modu …
GSK690693 delays tumor onset and progression in genetically defined mouse models expressing activated Akt.
Altomare DA, Zhang L, Deng J, Di Cristofano A, Klein-Szanto AJ, Kumar R, Testa JR. Altomare DA, et al. Clin Cancer Res. 2010 Jan 15;16(2):486-96. doi: 10.1158/1078-0432.CCR-09-1026. Clin Cancer Res. 2010. PMID: 20075391 Free PMC article.
We used genetically defined mouse models that develop spontaneous tumors exhibiting activated Akt to determine if Akt inhibition by GSK690693 is effective in the treatment of cancer. The broad long-term objective of this project was to use preclinical cancer models with pr …
We used genetically defined mouse models that develop spontaneous tumors exhibiting activated Akt to determine if Akt inhibition by GSK69
ZIP10 drives osteosarcoma proliferation and chemoresistance through ITGA10-mediated activation of the PI3K/AKT pathway.
Li H, Shen X, Ma M, Liu W, Yang W, Wang P, Cai Z, Mi R, Lu Y, Zhuang J, Jiang Y, Song Y, Wu Y, Shen H. Li H, et al. J Exp Clin Cancer Res. 2021 Oct 27;40(1):340. doi: 10.1186/s13046-021-02146-8. J Exp Clin Cancer Res. 2021. PMID: 34706747 Free PMC article.
Treatment with the CREB inhibitor 666-15 or the PI3K/AKT inhibitor GSK690693 impaired tumor chemoresistance in ZIP10-overexpressing cells. ...
Treatment with the CREB inhibitor 666-15 or the PI3K/AKT inhibitor GSK690693 impaired tumor chemoresistance in ZIP10-overexpressing c …
AKT inhibitor, GSK690693, induces growth inhibition and apoptosis in acute lymphoblastic leukemia cell lines.
Levy DS, Kahana JA, Kumar R. Levy DS, et al. Blood. 2009 Feb 19;113(8):1723-9. doi: 10.1182/blood-2008-02-137737. Epub 2008 Dec 8. Blood. 2009. PMID: 19064730 Free article.
We evaluated the effect of a novel, pan-AKT kinase inhibitor, GSK690693, on the proliferation of 112 cell lines representing different hematologic neoplasia. Fifty-five percent of all cell lines tested were sensitive to AKT inhibitor (EC(50)<1 microM), with acute lympho …
We evaluated the effect of a novel, pan-AKT kinase inhibitor, GSK690693, on the proliferation of 112 cell lines representing differen …
Initial testing (stage 1) of the Akt inhibitor GSK690693 by the pediatric preclinical testing program.
Carol H, Morton CL, Gorlick R, Kolb EA, Keir ST, Reynolds CP, Kang MH, Maris JM, Billups C, Smith MA, Houghton PJ, Lock RB. Carol H, et al. Pediatr Blood Cancer. 2010 Dec 15;55(7):1329-37. doi: 10.1002/pbc.22710. Epub 2010 Aug 25. Pediatr Blood Cancer. 2010. PMID: 20740623 Free PMC article.
BACKGROUND: GSK690693 is a small molecule ATP-competitive inhibitor of the pro-survival kinase Akt. ...No objective responses were observed and only one solid tumor met EFS T/C criteria for intermediate activity. CONCLUSIONS: GSK690693 demonstrated broad activity in …
BACKGROUND: GSK690693 is a small molecule ATP-competitive inhibitor of the pro-survival kinase Akt. ...No objective responses were ob …
Causal reasoning identifies mechanisms of sensitivity for a novel AKT kinase inhibitor, GSK690693.
Kumar R, Blakemore SJ, Ellis CE, Petricoin EF 3rd, Pratt D, Macoritto M, Matthews AL, Loureiro JJ, Elliston K. Kumar R, et al. BMC Genomics. 2010 Jul 6;11:419. doi: 10.1186/1471-2164-11-419. BMC Genomics. 2010. PMID: 20604938 Free PMC article.
In this study, causal network modeling is employed to elucidate mechanisms of action of GSK690693 that contribute to its observed biological effects. The mechanism of action of GSK690693 was evaluated in multiple human tumor cell lines from different tissues in 2-D …
In this study, causal network modeling is employed to elucidate mechanisms of action of GSK690693 that contribute to its observed bio …
Identification of 4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a novel inhibitor of AKT kinase.
Heerding DA, Rhodes N, Leber JD, Clark TJ, Keenan RM, Lafrance LV, Li M, Safonov IG, Takata DT, Venslavsky JW, Yamashita DS, Choudhry AE, Copeland RA, Lai Z, Schaber MD, Tummino PJ, Strum SL, Wood ER, Duckett DR, Eberwein D, Knick VB, Lansing TJ, McConnell RT, Zhang S, Minthorn EA, Concha NO, Warren GL, Kumar R. Heerding DA, et al. J Med Chem. 2008 Sep 25;51(18):5663-79. doi: 10.1021/jm8004527. J Med Chem. 2008. PMID: 18800763
Herein, we describe our lead optimization studies culminating in the discovery of compound 3g (GSK690693). Compound 3g is a novel ATP competitive, pan-AKT kinase inhibitor with IC 50 values of 2, 13, and 9 nM against AKT1, 2, and 3, respectively. ...
Herein, we describe our lead optimization studies culminating in the discovery of compound 3g (GSK690693). Compound 3g is a novel ATP …
Discovery of 14-3-3 protein-protein interaction inhibitors that sensitize multidrug-resistant cancer cells to doxorubicin and the Akt inhibitor GSK690693.
Mori M, Vignaroli G, Cau Y, Dinić J, Hill R, Rossi M, Colecchia D, Pešić M, Link W, Chiariello M, Ottmann C, Botta M. Mori M, et al. ChemMedChem. 2014 May;9(5):973-83. doi: 10.1002/cmdc.201400044. Epub 2014 Apr 8. ChemMedChem. 2014. PMID: 24715717
Notably, the two most active compounds promoted the translocation of c-Abl and FOXO pro-apoptotic factors into the nucleus and sensitized multidrug-resistant cancer cells to apoptotic inducers such as doxorubicin and the pan-Akt inhibitor GSK690693, thus becoming valuable …
Notably, the two most active compounds promoted the translocation of c-Abl and FOXO pro-apoptotic factors into the nucleus and sensitized mu …
Mechanism and management of AKT inhibitor-induced hyperglycemia.
Crouthamel MC, Kahana JA, Korenchuk S, Zhang SY, Sundaresan G, Eberwein DJ, Brown KK, Kumar R. Crouthamel MC, et al. Clin Cancer Res. 2009 Jan 1;15(1):217-25. doi: 10.1158/1078-0432.CCR-08-1253. Clin Cancer Res. 2009. PMID: 19118049
EXPERIMENTAL DESIGN: The effect of GSK690693 on blood glucose, insulin, and glucagon levels was characterized in mice. ...RESULTS: We report that treatment with antidiabetic agents does not significantly affect GSK690693-induced hyperglycemia in rodents. However, ad …
EXPERIMENTAL DESIGN: The effect of GSK690693 on blood glucose, insulin, and glucagon levels was characterized in mice. ...RESULTS: We …
103 results