Glucose metabolism activation by SHIP2 inhibitors via up-regulation of GLUT1 gene in L6 myotubes

European Journal of Pharmacology

Volumn 642, Issue 1-3, 2010, Pages 177-182

  Suwa, Akira ^a   Kurama, Takeshi ^a   Yamamoto, Tadashi ^a   Sawada, Akihiko ^a   Shimokawa, Teruhiko ^a   Aramori, Ichiro ^a  

^a ASTELLAS PHARMA INC   (Japan)

Author keywords

AS1938909 (3 (2,4 dichlorobenzyl)oxy N (2,6 difluorobenzyl)thiophene 2 carboxamide); AS1949490 (3 (4 chlorobenzyl)oxy N (1S) 1 phenylethyl 2 thiophenecarboxamide); GLUT1; Insulin signaling; SHIP2 (SH2 domain containing inositol 5' phosphatase 2); Small molecule inhibitor

Indexed keywords

3 [(2,4 DICHLOROBENZYL)OXYL] N (2,6 DIFLUOROBENZYL)THIOPHENE 2 CARBOXAMIDE; AS 1938909; GLUCOSE; GLUCOSE TRANSPORTER 1; GLUCOSE TRANSPORTER 4; INSULIN; MESSENGER RNA; PHOSPHATASE; PROTEIN KINASE B; PROTEIN TYROSINE PHOSPHATASE INHIBITOR; PROTEIN TYROSINE PHOSPHATASE SHP 2; SYNAPTOJANIN; UNCLASSIFIED DRUG; ENZYME INHIBITOR; INPPL1 PROTEIN, HUMAN;

ANIMAL CELL; ARTICLE; CONTROLLED STUDY; DRUG SELECTIVITY; DRUG STRUCTURE; EMBRYO; GLUCOSE INTAKE; GLUCOSE METABOLISM; GLUCOSE TRANSPORT; HUMAN; HUMAN CELL; INHIBITION KINETICS; MYOTUBE; NONHUMAN; NUCLEOTIDE SEQUENCE; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN PHOSPHORYLATION; RAT; RECEPTOR UPREGULATION; SIGNAL TRANSDUCTION; UPREGULATION; ANIMAL; ANTAGONISTS AND INHIBITORS; CELL LINE; DRUG EFFECTS; DRUG SCREENING; GENETICS; METABOLISM; MOUSE; PHOSPHORYLATION; SKELETAL MUSCLE; TRANSPORT AT THE CELLULAR LEVEL;

ANIMALS; BIOLOGICAL TRANSPORT; CELL LINE; DRUG EVALUATION, PRECLINICAL; ENZYME INHIBITORS; GLUCOSE; GLUCOSE TRANSPORTER TYPE 1; MICE; MUSCLE FIBERS, SKELETAL; PHOSPHORIC MONOESTER HYDROLASES; PHOSPHORYLATION; PROTO-ONCOGENE PROTEINS C-AKT; RATS; RNA, MESSENGER; UP-REGULATION;

EID: 77954625295     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejphar.2010.06.002     Document Type: Article

References (18)

1. Baumgartener J.W. SHIP2: an emerging target for the treatment of type 2 diabetes mellitus. Curr. Drug Targets Immune Endocr. Metab. Disord. 2003, 3:291-298.
2. Bell G.I., Kayano T., Buse J.B., Burant C.F., Takeda J., Lin D., Fukumoto H., Seino S. Molecular biology of mamalian glucose transporters. Diab. Care 1990, 13:198-208.
3. Buettner R., Ottinger I., Gerhardt-Salbert C., Wrede C.E., Scholmerich J., Bollheimer L.C. Antisense oligonucleotides against the lipid phosphatase SHIP2 improve muscle insulin sensitivity in a dietary rat model of the metabolic syndrome. Am. J. Physiol. Endocrinol. Metab. 2007, 292:E1871-E1878.
4. Friedman J.E., Dudek R.W., Whitehead D.S., Downes D.L., Frisell W.R., Caro J.F., Dohm G.L. Immunolocalization of glucose transporter GLUT4 within human skeletal muscle. Diabetes 1991, 40:150-154.
5. Suwa, A., Yamamoto, T., Sawada, A., Minoura, K., Hosogai, N., Tahara, A., Kurama, T., Shimokawa, T., Aramori, I., 2009. Discovery and functional characterization of a novel small molecule inhibitor of the intracellular phosphatase, SHIP2. Br. J. Pharmacol. 158, 879-887.
6. Fukui K., Wada T., Kagawa S., Nagira K., Ikubo M., Ishihara H., Kobayashi M., Sasaoka T. Impact of the liver-specific expression of SHIP2 (SH2-containing inositol 5'-phosphatase 2) on insulin signaling and glucose metabolism in mice. Diabetes 2005, 54:1958-1967.
7. Grempler R., Zibrova D., Schoelch C., van Marle A., Rippmann J.F., Redemann N. Normalization of prandial blood glucose and improvement of glucose tolerance by liver-specific inhibition of SH2 domain containing inositol phosphatase 2 (SHIP2) in diabetic KKAy mice: SHIP2 inhibition causes insulin-mimetic effects on glycogen metabolism, gluconeogenesis, and glycolysis. Diabetes 2007, 56:2235-2241.
8. Hausdorff S.F., Bennett A.M., Neel B.G., Birnbaum M.J. Different signaling roles of SHPTP2 in insulin-induced GLUT1 expression and GLUT4 translocation. J. Biol. Chem. 1995, 270:12,965-12,968.
9. Hori H., Sasaoka T., Wada T., Ishiki M., Haruta T., Ishihara H., Kobayashi M. SH2-containing inositol phosphatase 2 negatively regulates insulin-induced glycogen synthesis in L6 myotubes. Diabetologia 2001, 44:1258-1267.
10. Kagawa S., Soeda Y., Ishihara H., Oya T., Sasahara M., Yaguchi S., Oshita R., Wada T., Tsuneki H., Sasaoka T. Impact of transgenic overexpression of SH2-containing inositol 5'-phosphatase 2 on glucose metabolism and insulin signaling in mice. Endocrinology 2008, 149:642-650.
11. Marette A., Richardson J.M., Ramlal T., Balon T.W., Vranic M., Pessin J.E., Klip A. Abundance, localization, and insulin-induced translocation of glucose transporters in red and white muscle. Am. J. Physiol. 1992, 263:C443-C452.
12. Saltiel A.R., Lazar D.F. Lipid phosphatases as drug discovery targets for type 2 diabetes. Nat. Rev. Drug Discov. 2006, 5:333-342.
13. Sasaoka T., Wada T., Tsuneki H. Lipid phosphatases as a possible therapeutic target in cases of type 2 diabetes and obesity. Pharmacol. Ther. 2006, 112:799-809.
14. Sleeman M.W., Wortley K.E., Lai K.-M.V., Gowen L.C., Kintner J., Kline W.O., Garcia K., Stitt T.N., Yancopoulos G.D., Wiegand S.J., Glass D.J. Absence of the lipid phosphatase SHIP2 confers resistance to dietary obesity. Nat. Med. 2005, 11:199-205.
15. Taha C., Liu Z., Jin J., Al-Hasani H., Sonenberg N., Klip A. Opposite translational control of GLUT1 and GLUT4 glucose transporter mRNAs in response to insulin. role of mammalian target of rapamycin, protein kinase b, and phosphatidylinositol 3-kinase in GLUT1 mRNA translation. J. Biol. Chem. 1999, 274:33,085-33,091.
16. Tordjman K.M., Leingang K.A., James D.E., Mueckler M.M. Differential regulation of two distinct glucose transporter species expressed in 3T3-L1 adipocytes: effect of chronic insulin and tolbutamide treatment. Proc. Natl. Acad. Sci. USA 1989, 89:7761-7765.
17. Tordjman K.M., Leingang K.A., Mueckler M.M. Differential regulation of the HepG2 and adipocyte/muscle glucose transporters in 3T3L1 adipocytes. Effect of chronic glucose deprivation. Biochem. J. 1990, 271:201-207.
18. Wada T., Sasaoka T., Funaki M., Hori H., Murakami S., Ishiki M., Haruta T., Asano T., Ogawa W., Ishihara H., Kobayashi M. Overexpression of SH2-containing inositol phosphatase 2 results in negative regulation of insulin-induced metabolic actions in 3T3-L1 adipocytes via its 5'-phosphatase catalytic activity. Mol. Cell. Biol. 2001, 21:1633-1646.