[1]
|
Sale, E.M. and Sale, G.J. (2008) Protein Kinase B: Signalling Roles and Therapeutic Targeting. Cellular and Molecular Life Sciences, 65, Article No. 113. https://doi.org/10.1007/s00018-007-7274-9
|
[2]
|
Carnero, A., Blanco-Aparicio, C., Renner, O., Link, W. and Leal, J.F.M. (2008) The PTEN/PI3K/AKT Signalling Pathway in Cancer, Therapeutic Implications. Current Cancer Drug Targets, 8, 187-198.
https://doi.org/10.2174/156800908784293659
|
[3]
|
Zhou, B.G., Wei, C.S., Zhang, S., Zhang, Z. and Gao, H.M. (2018) Matrine Reversed Multidrug Resistance of Breast Cancer MCF-7/ADR Cells through PI3K/AKT Signaling Pathway. Journal of Cellular Biochemistry, 119, 3885-3891.
https://doi.org/10.1002/jcb.26502
|
[4]
|
Georgakis, G.V. and Younes, A. (2006) From Rapa Nui to Rapamycin: Targeting PI3K/Akt/mTOR for Cancer Therapy. Expert Review of Anticancer Therapy, 6, 131-140. https://doi.org/10.1586/14737140.6.1.131
|
[5]
|
Heerding, D.A., Rhodes, N., Leber, J.D., Clark, T.J., Keenan, R.M., Lafrance, L.V., et al. (2008) 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. Journal of Medicinal Chemistry, 51, 5663-5679.
https://doi.org/10.1021/jm8004527
|
[6]
|
Rhodes, N., Heerding, D.A., Duckett, D.R., Eberwein, D.J., Knick, V.B., Lansing, T.J., et al. (2008) Characterization of an AKT Kinase Inhibitor with Potent Pharmacodynamic and Antitumor Activity. Cancer Research, 68, 2366-2374.
https://doi.org/10.1158/0008-5472.can-07-5783
|
[7]
|
Crouthamel, M.-C., Kahana, J.A., Korenchuk, S., Zhang, S.-Y., Sundaresan, G., Eberwein, D.J., et al. (2009) Mechanism and Management of AKT Inhibitor-Induced Hyperglycemia. Clinical Cancer Research, 15, 217-225.
https://doi.org/10.1158/1078-0432.CCR-08-1253
|
[8]
|
Lippa, B., Pan, G., Corbett, M., Li, C., Kauffman, G.S., Pandit, J., et al. (2008) Synthesis and Structure Based Optimization of Novel Akt Inhibitors. Bioorganic & Medicinal Chemistry Letters, 18, 3359-2263.
https://doi.org/10.1016/j.bmcl.2008.04.034
|
[9]
|
Freeman-Cook, K.D., Autry, C., Borzillo, G., Gordon, D., Barbacci-Tobin, E., Bernardo, V., et al. (2010) Design of Selective, ATP-Competitive Inhibitors of Akt. Journal of Medicinal Chemistry, 53, 4615-4622.
https://doi.org/10.1021/jm1003842
|
[10]
|
Caldwell, J.J., Davies, T.G., Donald, A., McHardy, T., Rowlands, M.G., Wynne Aherne, G., et al. (2008) Identification of 4-(4-aminopiperidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidines as Selective Inhibitors of Protein Kinase B through Fragment Elaboration. Journal of Medicinal Chemistry, 51, 2147-2157. https://doi.org/10.1021/jm701437d
|
[11]
|
McHardy, T., Caldwell, J.J., Cheung, K.-M., Hunter, L.J., Taylor, K., Rowlands, M., Ruddle, R., et al. (2010) Discovery of 4-amino-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamides as Selective, Orally Active Inhibitors of Protein Kinase B (Akt). Journal of Medicinal Chemistry, 53, 2239-2249. https://doi.org/10.1021/jm901788j
|
[12]
|
Addie, M., Ballard, P., Buttar, D., Crafter, C., Currie, G., Davies, B.R., Debreczeni, J., et al. (2013) 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. Journal of Medicinal Chemistry, 56, 2059-2073.
https://doi.org/10.1021/jm301762v
|
[13]
|
Rice, K.D., Kim, M.H., Bussenius, J., Anand, N.K., Blazey, C.M., Bowles, O.J., et al. (2012) Pyrazolopyrimidines as Dual Akt/p70S6K Inhibitors. Bioorganic & Medicinal Chemistry Letters, 22, 2693-2697.
https://doi.org/10.1016/j.bmcl.2012.03.011
|
[14]
|
Lin, X., Murray, J.M., Rico, A.C., Wang, M.X., Chu, D.T., Zhou, Y., Rosario, M.D., Kaufman, S., Ma, S., Fang, E., Crawford, K. and Jefferson, A.B. (2006) Discovery of 2-pyrimidyl-5-amidothiophenes as Potent Inhibitors for AKT: Synthesis and SAR Studies. Bioorganic & Medicinal Chemistry Letters, 16, 4163-468.
https://doi.org/10.1016/j.bmcl.2006.05.092
|
[15]
|
Chang, S., Zhang, Z., Zhuang, X., Luo, J., Cao, X., Li, H., Tu, Z., Lu, X., Ren, X. and Ding, K. (2012) New Thiazole Carboxamides as Potent Inhibitors of AKT Kinases. Bioorganic & Medicinal Chemistry Letters, 22, 1208-1212.
https://doi.org/10.1016/j.bmcl.2011.11.080
|
[16]
|
Zhan, W., Li, D., Che, J., Zhang, L., Yang, B., Hu, Y., Liu, T. and Dong, X. (2014) Integrating Docking Scores, Interaction Profiles and Molecular Descriptors to Improve the Accuracy of Molecular Docking: Toward the Discovery of Novel Akt1 Inhibitors. European Journal of Medicinal Chemistry, 75, 11-20.
https://doi.org/10.1016/j.ejmech.2014.01.019
|
[17]
|
Saxty, G., Woodhead, S.J., Berdini, V., Davies, T.G., Verdonk, M.L., Wyatt, P.G., et al. (2007) Identification of Inhibitors of Protein Kinase B Using Fragment-Based Lead Discovery. Journal of Medicinal Chemistry, 50, 2293-2296.
https://doi.org/10.1021/jm070091b
|
[18]
|
Yap, T.A., Walton, M.I., Grimshaw, K.M., te Poele, R.H., Eve, P.D., Valenti, M.R., et al. (2012) AT13148 Is a Novel, Oral Multi-AGC Kinase Inhibitor with Potent Pharmacodynamic and Antitumor Activity. Clinical Cancer Research, 18, 3912-3923. https://doi.org/10.1158/1078-0432.CCR-11-3313
|
[19]
|
Dumble, M., Crouthamel, M.-C., Zhang, S.-Y., Schaber, M., Levy, D., Robell, K., et al. (2014) Discovery of Novel AKT Inhibitors with Enhanced Anti-Tumor Effects in Combination with the MEK Inhibitor. PLoS ONE, 9, e100880.
https://doi.org/10.1371/journal.pone.0100880
|
[20]
|
Tolcher, A.W., Patnaik, A., Papadopoulos, K.P., Rasco, D.W., Becerra, C.R., Allred, A.J., et al. (2015) Phase I study of the MEK Inhibitor Trametinib in Combination with the AKT Inhibitor Afuresertib in Patients with Solid Tumors and Multiple Myeloma. Cancer Chemotherapy and Pharmacology, 75, 183-189.
https://doi.org/10.1007/s00280-014-2615-5
|
[21]
|
Zhan, W., Xu, L., Dong, X., Dong, J., Yi, X., Ma, X., et al. (2016) Design, Synthesis and Biological Evaluation of Pyrazol-Furan Carboxamide Analogues as Novel Akt Kinase Inhibitors. European Journal of Medicinal Chemistry, 117, 47-58. https://doi.org/10.1016/j.ejmech.2016.03.074
|
[22]
|
Dong, X., Zhan, W., Zhao, M., Che, J., Dai, X., Wu, Y., et al. (2019) Discovery of 3,4,6-Trisubstituted Piperidine Derivatives as Orally Active, Low hERG Blocking AKT Inhibitors via Conformational Restriction and Structure-Based Design. Journal of Medicinal Chemistry, 62, 7264-7288. https://doi.org/10.1021/acs.jmedchem.9b00891
|
[23]
|
Blake, J.F., Kallan, N.C., Xiao, D., Xu, R., Bencsik, J.R., Skelton, N.J., et al. (2010) Discovery of Pyrrolopyrimidine Inhibitors of AKT. Bioorganic & Medicinal Chemistry Letters, 20, 5607-5612.
https://doi.org/10.1016/j.bmcl.2010.08.053
|
[24]
|
Bencsik, J.R., Xiao, D., Blake, J.F., Kallan, N.C., Mitchell, I.S., Spencer, K.L., et al. (2010) Discovery of Dihydrothieno- and Dihydrofuropyrimidines as Potent Pan AKT Inhibitors. Bioorganic & Medicinal Chemistry Letters, 20, 7037-7041. https://doi.org/10.1016/j.bmcl.2010.09.112
|
[25]
|
Blake, J.F., Xu, R., Bencsik, J.R., Xiao, D., Kallan, N.C., Schlachter, S., et al. (2012) Discovery and Preclinical Pharmacology of a Selective ATP-Competitive AKT Inhibitor (GDC-0068) for the Treatment of Human Tumors. Journal of Medicinal Chemistry, 55, 8110-8127. https://doi.org/10.1021/jm301024w
|
[26]
|
Lin, J., Sampath, D., Nannini, M.A., Lee, B.B., Degtyarev, M., Oeh, J., et al. (2013) Targeting Activated AKT with GDC-0068, a Novel Selective AKT Inhibitor That Is Efficacious in Multiple Tumor Models. Clinical Cancer Research, 19, 1760-1772. https://doi.org/10.1158/1078-0432.CCR-12-3072
|