Next-generation Akt inhibitors provide greater specificity: Effects on glucose metabolism in adipocytes

Biochemical Journal

Volumn 435, Issue 2, 2011, Pages 539-544

  Tan, Shixiong ^a   Ng, Yvonne ^a   James, David E ^a,b  

^a GARVAN INSTITUTE OF MEDICAL RESEARCH   (Australia)

^b UNIVERSITY OF NEW SOUTH WALES   (Australia)

Author keywords

Adipocyte; Akt inhibitor; Cancer; Insulin; MK 2206; Signalling

Indexed keywords

GLUCOSE; GLUCOSE TRANSPORTER 4; INSULIN; MK 2206; PROTEIN KINASE B; PROTEIN KINASE B INHIBITOR; SERINE; THREONINE; UNCLASSIFIED DRUG;

ADIPOCYTE; ALLOSTERISM; ARTICLE; CONTROLLED STUDY; DRUG EFFICACY; DRUG INHIBITION; DRUG SPECIFICITY; GENE TRANSLOCATION; GLUCOSE METABOLISM; GLUCOSE TRANSPORT; HUMAN; HUMAN CELL; IC 50; IN VIVO STUDY; PRIORITY JOURNAL; PROTEIN PHOSPHORYLATION; SOLID TUMOR;

3T3-L1 CELLS; ADIPOCYTES; ANIMALS; ANTINEOPLASTIC AGENTS; CELLS, CULTURED; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG EVALUATION, PRECLINICAL; GLUCOSE; GLUCOSE TRANSPORTER TYPE 4; HETEROCYCLIC COMPOUNDS, 3-RING; HUMANS; MICE; PROTEIN KINASE INHIBITORS; PROTEIN TRANSPORT; PROTO-ONCOGENE PROTEINS C-AKT; SUBSTRATE SPECIFICITY;

MAMMALIA;

EID: 79953186071     PISSN: 02646021     EISSN: 14708728     Source Type: Journal    
DOI: 10.1042/BJ20110040     Document Type: Article

References (28)

1. Vasudevan, K. M., Barbie, D. A., Davies, M. A., Rabinovsky, R., McNear, C. J., Kim, J. J., Hennessy, B. T., Tseng, H., Pochanard, P., Kim, S. Y. et al. (2009) AKT-independent signaling downstream of oncogenic PIK3CA mutations in human cancer. Cancer Cell 16, 21-32
2. Vivanco, I. and Sawyers, C. L. (2002) The phosphatidylinositol 3-kinase-AKT pathway in human cancer. Nat. Rev. Cancer 2, 489-501
3. Liu, L. Z., Zhou, X. D., Qian, G., Shi, X., Fang, J. and Jiang, B. H. (2007) AKT1 amplification regulates cisplatin resistance in human lung cancer cells through the mammalian target of rapamycin/p70S6K1 pathway. Cancer Res. 67, 6325-6332
4. Bellacosa, A., Kumar, C. C., Di Cristofano, A. and Testa, J. R. (2005) Activation of AKT kinases in cancer: implications for therapeutic targeting. Adv. Cancer Res. 94, 29-86
5. Barnett, S. F., Defeo-Jones, D., Fu, S., Hancock, P. J., Haskell, K. M., Jones, R. E., Kahana, J. A., Kral, A. M., Leander, K., Lee, L. L. et al. (2005) Identification and characterization of pleckstrin-homology-domain-dependent and isoenzyme-specific Akt inhibitors. Biochem. J. 385, 399-408 (Pubitemid 40165072)
6. DeFeo-Jones, D., Barnett, S. F., Fu, S., Hancock, P. J., Haskell, K. M., Leander, K. R., McAvoy, E., Robinson, R. G., Duggan, M. E., Lindsley, C. W. et al. (2005) Tumor cell sensitization to apoptotic stimuli by selective inhibition of specific Akt/PKB family members. Mol. Cancer Ther. 4, 271-279
7. Jiang, B. H. and Liu, L. Z. (2008) PI3K/PTEN signaling in tumorigenesis and angiogenesis. Biochim. Biophys. Acta 1784, 150-158
8. Whiteman, E. L., Cho, H. and Birnbaum, M. J. (2002) Role of Akt/protein kinase B in metabolism. Trends Endocrinol. Metab. 13, 444-451
9. Ng, Y., Ramm, G., Lopez, J. A. and James, D. E. (2008) Rapid activation of Akt2 is sufficient to stimulate GLUT4 translocation in 3T3-L1 adipocytes. Cell Metab. 7, 348-356
10. Kohn, A. D., Summers, S. A., Birnbaum, M. J. and Roth, R. A. (1996) Expression of a constitutively active Akt Ser/Thr kinase in 3T3-L1 adipocytes stimulates glucose uptake and glucose transporter 4 translocation. J. Biol. Chem. 271, 31372-31378
11. Gonzalez, E. and McGraw, T. E. (2006) Insulin signaling diverges into Akt-dependent and-independent signals to regulate the recruitment/docking and the fusion of GLUT4 vesicles to the plasma membrane. Mol. Biol. Cell 17, 4484-4493
12. Tan, S. X., Ng, Y. and James, D. E. (2010) Akt inhibitors reduce glucose uptake independently of their effects on Akt. Biochem. J. 432, 191-197
13. Green, C. J., Goransson, O., Kular, G. S., Leslie, N. R., Gray, A., Alessi, D. R., Sakamoto, K. and Hundal, H. S. (2008) Use of Akt inhibitor and a drug-resistant mutant validates a critical role for protein kinase B/Akt in the insulin-dependent regulation of glucose and system A amino acid uptake. J. Biol. Chem. 283, 27653-27667
14. Hirai, H., Sootome, H., Nakatsuru, Y., Miyama, K., Taguchi, S., Tsujioka, K., Ueno, Y., Hatch, H., Majumder, P. K., Pan, B. S. and Kotani, H. (2010) MK-2206, an allosteric Akt inhibitor, enhances antitumor efficacy by standard chemotherapeutic agents or molecular targeted drugs in vitro and in vivo. Mol. Cancer Ther. 9, 1956-1967
15. Chen, D., Elmendorf, J. S., Olson, A. L., Li, X., Earp, H. S. and Pessin, J. E. (1997) Osmotic shock stimulates GLUT4 translocation in 3T3L1 adipocytes by a novel tyrosine kinase pathway. J. Biol. Chem. 272, 27401-27410
16. Chen, D., Fucini, R. V., Olson, A. L., Hemmings, B. A. and Pessin, J. E. (1999) Osmotic shock inhibits insulin signaling by maintaining Akt/protein kinase B in an inactive dephosphorylated state. Mol. Cell. Biol. 19, 4684-4694
17. Li, D., Randhawa, V. K., Patel, N., Hayashi, M. and Klip, A. (2001) Hyperosmolarity reduces GLUT4 endocytosis and increases its exocytosis from a VAMP2-independent pool in l6 muscle cells. J. Biol. Chem. 276, 22883-22891
18. Gould, G. W., Thomas, H. M., Jess, T. J. and Bell, G. I. (1991) Expression of human glucose transporters in Xenopus oocytes: kinetic characterization and substrate specificities of the erythrocyte, liver, and brain isoforms. Biochemistry 30, 5139-5145
19. Rudlowski, C., Moser, M., Becker, A. J., Rath, W., Buttner, R., Schroder, W. and Schurmann, A. (2004) GLUT1 mRNA and protein expression in ovarian borderline tumors and cancer. Oncology 66, 404-410 (Pubitemid 39194363)
20. Younes, M., Lechago, L. V., Somoano, J. R., Mosharaf, M. and Lechago, J. (1996) Wide expression of the human erythrocyte glucose transporter Glut1 in human cancers. Cancer Res. 56, 1164-1167 (Pubitemid 26065417)
21. Gonzalez, E. and McGraw, T. E. (2009) The Akt kinases: isoform specificity in metabolism and cancer. Cell Cycle 8, 2502-2508
22. Staal, S. P. (1987) Molecular cloning of the akt oncogene and its human homologues AKT1 and AKT2 : amplification of AKT1 in a primary human gastric adenocarcinoma. Proc. Natl. Acad. Sci. U.S.A. 84, 5034-5037
23. Stal, O., Perez-Tenorio, G., Akerberg, L., Olsson, B., Nordenskjold, B., Skoog, L. and Rutqvist, L. E. (2003) Akt kinases in breast cancer and the results of adjuvant therapy. Breast Cancer Res. 5, R37-R44
24. Cheng, J. Q., Godwin, A. K., Bellacosa, A., Taguchi, T., Franke, T. F., Hamilton, T. C., Tsichlis, P. N. and Testa, J. R. (1992) AKT2 , a putative oncogene encoding a member of a subfamily of protein-serine/threonine kinases, is amplified in human ovarian carcinomas. Proc. Natl. Acad. Sci. U.S.A. 89, 9267-9271
25. Cheng, J. Q., Ruggeri, B., Klein, W. M., Sonoda, G., Altomare, D. A., Watson, D. K. and Testa, J. R. (1996) Amplification of AKT2 in human pancreatic cells and inhibition of AKT2 expression and tumorigenicity by antisense RNA. Proc. Natl. Acad. Sci. U.S.A. 93, 3636-3641
26. Roy, H. K., Olusola, B. F., Clemens, D. L., Karolski, W. J., Ratashak, A., Lynch, H. T. and Smyrk, T. C. (2002) AKT proto-oncogene overexpression is an early event during sporadic colon carcinogenesis. Carcinogenesis 23, 201-205
27. Stahl, J. M., Sharma, A., Cheung, M., Zimmerman, M., Cheng, J. Q., Bosenberg, M. W., Kester, M., Sandirasegarane, L. and Robertson, G. P. (2004) Deregulated Akt3 activity promotes development of malignant melanoma. Cancer Res. 64, 7002-7010 (Pubitemid 39331010)
28. Nakatani, K., Thompson, D. A., Barthel, A., Sakaue, H., Liu, W., Weigel, R. J. and Roth, R. A. (1999) Up-regulation of Akt3 in estrogen receptor-deficient breast cancers and androgen-independent prostate cancer lines. J. Biol. Chem. 274, 21528-21532