Endogenous effectors of human liver glycogen phosphorylase modulate effects of indole-site inhibitors

American Journal of Physiology - Endocrinology and Metabolism

Volumn 289, Issue 3 52-3, 2005, Pages

  Ercan Fang, Nacide ^a,d   Taylor, Miriam R ^a   Treadway, Judith L ^c   Levy, Carolyn B ^c,f   Genereux, Paul E ^c   Gibbs, E Michael ^c   Rath, Virginia L ^c,e   Kwon, Younggil ^c   Cannon, Mary C ^a,b   Nuttall, Frank Q ^a  

^a UNIVERSITY OF MINNESOTA   (United States)

^b UNIVERSITY OF MINNESOTA MEDICAL SCHOOL   (United States)

^c PFIZER INC   (United States)

^d VA MEDICAL CENTER   (United States)

^e Thios Pharmaceuticals   (United States)

^f ISIS PHARMACEUTICALS   (United States)

Author keywords

Glucose

Indexed keywords

ADENOSINE DIPHOSPHATE; ADENOSINE TRIPHOSPHATE; ENZYME INHIBITOR; FRUCTOSE 1 PHOSPHATE; GLUCOSE; GLUCOSE 6 PHOSPHATE; GLYCOGEN PHOSPHORYLASE; INDOLE DERIVATIVE; PHOSPHORYLASE; URIDINE DIPHOSPHATE GLUCOSE;

ARTICLE; CONCENTRATION RESPONSE; EFFECTOR CELL; ENZYME ACTIVE SITE; ENZYME ACTIVITY; ENZYME ASSAY; ENZYME INHIBITION; ENZYME REGULATION; GLUCOSE BLOOD LEVEL; GLYCOGENOLYSIS; HUMAN; HUMAN CELL; HYPERGLYCEMIA; IC 50; LIVER METABOLISM; PRIORITY JOURNAL;

ADENOSINE DIPHOSPHATE; ADENOSINE TRIPHOSPHATE; AMIDES; ANIMALS; BLOOD GLUCOSE; CELL LINE; DOSE-RESPONSE RELATIONSHIP, DRUG; ENZYME ACTIVATION; FRUCTOSEPHOSPHATES; GLUCOSEPHOSPHATES; GLYCOGEN; HUMANS; HYPERGLYCEMIA; HYPOGLYCEMIA; INDOLES; LIVER; MALE; PHOSPHORYLASE A; PHOSPHORYLASE B; RATS; RATS, SPRAGUE-DAWLEY; URIDINE DIPHOSPHATE GLUCOSE;

EID: 23944438864     PISSN: 01931849     EISSN: None     Source Type: Journal    
DOI: 10.1152/ajpendo.00264.2004     Document Type: Article

References (47)

1. Boden G, Chen X, and Stein PT. Gluconeogenesis in moderately and severely hyperglycemic patients with type 2 diabetes mellitus. Am J Physiol Endocrinol Metab 280: E23-E30, 2001.
2. 31P magnetic resonance spectroscopy. Pediatr Res 36: 436-440, 1994.
3. Brosnan MJ, Chen L, Van Dyke TA, and Koretsky AP. Free ADP levels in transgeneic mouse liver expressing creatinine kinase. Effects of enzyme activity, phosphagen type, and substrate concentration. J Biol Chem 265: 20849-20855, 1990.
4. 2+. J Biol Chem 258: 14294-14308, 1983.
5. 31P-NMR spectroscopy. Biochim Biophys Acta 885: 12-22, 1986.
6. Dufour S, Petersen KF, Rothman DL, Yu C, Cline GW, and Shulman GI. Mechanism by which hyperglycemia per se inhibits hepatic glucose production in man (Abstract). Diabetes 51, Suppl 2: A23, 92-OR, 2002.
7. Ercan N, Gannon MC, and Nuttall FQ. Allosteric regulation of liver phosphorylase a: revisited under approximated physiological conditions. Arch Biochem Biophys 328: 255-264, 1996.
8. Ercan N, Gannon MC, and Nuttall FQ. Liver glycogen synthase, phosphorylase and glycogen concentration in rats given a single glucose load orally. A 24 hour study. Arch Biochem Biophys 315: 35-40, 1994.
9. Ercan-Fang N, Gannon MC, Rath VL, Treadway JL, Taylor MR, and Nuttall FQ. Integrated effects of multiple modulators on human liver glycogen phosphorylase a. Am J Physiol Endocrinol Metab 283: E29-E37, 2002.
10. Ercan-Fang N and Nuttall FQ. The effect of caffeine and caffeine analogs on rat liver phosphorylase a activity. J Pharmacol Exp Ther 280: 1312-1318, 1997.
11. Ercan-Fang NG, Nuttall FQ, and Gannon MC. Uric acid inhibits liver phosphorylase a activity under simulated in vivo conditions. Am J Physiol Endocrinol Metab 280: E248-E253, 2001.
12. Fletterick RJ and Madsen NB. The structures and related functions of phosphorylase a. Annu Rev Biochem 49: 31-61, 1980.
13. Gannon MC and Nuttall FQ. Effect of feeding, fasting, and diabetes on liver glycogen synthase activity, protein, and mRNA in rats. Diabetologia 40: 758-763, 1997.
14. Gannon MC, Nuttall FQ, Lane JT, Fang S, Gupta V, and Sandhofer C. Effect of twenty-four hours of starvation on plasma glucose and insulin concentrations in people with untreated non-insulin-dependent diabetes mellitus. Metabolism 45: 492-497, 1996.
15. Gastaldelli A, Baldi S, Pettiti M, Toschi E, Camastra S, Natali A, Landau BR, and Ferrannini E. Influence of obesity and type 2 diabetes on gluconeogenesis and glucose output in humans. Diabetes 49: 1367-1373, 2000.
16. Gevers G and Stalmans W. Radiochemical methods for the assay of phosphorylase in the direction of glycogenolysis. Biochem J 193: 793-798, 1981.
17. Gilboe DP, Larson KL, and Nuttall FQ. A radioactive method for the assay of glycogen phosphorylases. Anal Chem 47: 20-27, 1972.
18. Goldsmith EJ, Sprang SR, Hamlin R, Xuong N-H, and Fletterick RJ. Domain separation in the activation of glycogen phosphorylase a. Science 245: 528-532, 1989.
19. Hemmerle H, Burger H, Below P, Schubert G, Rippel R, Schindler PW, Paulus E, and Herling AW. Chlorogenic acid and synthetic chlorogenic acid derivatives: Novel inhibitors of hepatic glucose-6-phosphate translocase. J Med Chem 40: 137-146, 1997.
20. Hoover DJ, Hulin B, Martin WH, Phillips D, and Treadway JL. U.S. Patent 6 107 329, Example 166, 2000.
21. Hoover DJ, Hulin B, Martin WH, and Treadway JL. U.S. Patent 6 297 269. Example 36, 2001.
22. Hoover DJ, Lefkowitz-Snow S, Burgess-Henry JL, Martin WH, Armento SJ, Stock IA, McPherson RK, Genereux PE, Gibbs EM, and Treadway JL. Indole-2-carboxamide inhibitors of human liver glycogen phosphorylase. J Med Chem 41: 2934-2938, 1998.
23. i. Biochem J 229: 141-151, 1985.
24. Kasvinsky PJ, Fletterick RJ, and Madsen NB. Regulation of the dephosphorylation of glycogen phosphorylase a and synthase b by glucose and caffeine in isolated hepatocytes. Can J Biochem 59: 387-395, 1981.
25. Kasvinsky PJ, Madsen NB, Sygusch J, and Fletterick RJ. The regulation of glycogen phosphorylase a by nucleotide derivatives. J Biol Chem 253: 3343-3351, 1978.
26. Kasvinsky PJ, Shechosky S, and Fletterick RJ. Synergistic regulation of phosphorylase a by glucose and caffeine. J Biol Chem 253: 9102-9106, 1978.
27. Koretsky AP, Brosnan MJ, Chen L, Chen J, and Van Dyke T. NMR detection of creatinine kinase expressed in liver of transgenic mice: Determination of free ADP levels. Proc Natl Acad Sci USA 87: 3112-3116, 1990.
28. Landau BR, Chandramouli V, Schumann WC, Ekberg K, Kumaran K, Kalhan SC, and Wahren J. Estimates of Krebs cycle activity and contributions of gluconeogenesis to hepatic glucose production in fasting healthy subjects and IDDM patients. Diabetologia 38: 831-838, 1995.
29. Maddaiah VT and Madsen NB. Kinetics of purified liver phosphorylase. J Biol Chem 241: 3873-3881, 1966.
30. Martin WH, Hoover DJ, Armento SJ, Stock IA, McPherson RK, Danley DE, Stevenson RW, Barrett EJ, and Treadway JL. Discovery of a human liver glycogen phosphorylase inhibitor that lowers blood glucose in vivo. Proc Natl Acad Sci USA 95: 1776-1781, 1998.
31. Martin WH, Hoover DJ, Armento SJ, Stock IA, McPherson RK, Danley DE, Stevenson RW, Barrett EJ, and Treadway JL. Discovery of a human liver glycogen phosphorylase inhibitor that lowers blood glucose in-vivo. Proc Natl Acad Sci USA 95: 1776-1781, 1998.
32. Newgard CB, Hwang PK, and Fletterick RJ. The family of glycogen phosphorylases: Structure and function. Crit Rev Biochem Mol Biol 24: 69-99, 1989.
33. Niewoehner CB, Gilboe DP, Nuttall GA, and Nuttall FQ. Metabolic effects of oral fructose in the liver of fasted rats. Am J Physiol Endocrinol Metab 247: E505-E512, 1984.
34. Niewoehner CB and Nuttall FQ. The relationship of hepatic glucose uptake to intrahepatic glucose concentration in fasted rats following a glucose load. Diabetes 37: 1559-1566, 1988.
35. Parker JC, VanVolkenburg MA, Levy CB, Martin WH, Burk SH, Kwon Y, Giragossian C, Gant TG, Carpino PA, McPherson RK, Vestergaard P, and Treadway JL. Plasma glucose levels are reduced in rats and mice treated with an inhibitor of glucose-6-phosphate translocase. Diabetes 47: 1630-1636, 1998.
36. Rath VL, Ammirati M, Danley D, Ekstrom JL, Gibbs EM, Hynes TR, Mathiowetz AM, McPherson RK, Olson TV, Treadway JL, and Hoover DJ. Human liver glycogen phosphorylase inhibitors bind at a new allosteric site. Chem Biol 7: 677-682, 2000.
37. Rath VL, Ammirati M, LeMotte PK, Fennell KF, Mansour MN, Danley DE, Hynes TR, Schulte GK, Wasilko DJ, and Pandit J. Activation of human liver glycogen phosphorylase by alteration of the secondary structure and packing of the catalytic core. Mol Cell 6: 139-148, 2000.
38. Rath VL, Ammiratti ML, and Hoover DJ. Inhibitors of Human Glycogen Phosphorylase. European Patent Application: EPO 978279A1, 2000.
39. Roesler WJ, Pugazhenthi S, and Khandelwal RL. Hepatic glycogen metabolism in the db/db mouse. Mol Cell Biochem 92: 99-106, 1990.
40. 13C NMR. Science 254: 573-576, 1991.
41. Sprang SR, Acharya KR, Goldsmith EJ, Stuart DI, Varvill KM, Fletterick RJ, Madsen NB, and Johnson LN. Protein phosphorylation: structural changes between glycogen phosphorylase b and a. Nature 336: 215-221, 1988.
42. Stalmans W, DeWulf H, and Hers HG. The control of liver glycogen synthetase phosphatase by phosphorylase. Eur J Biochem 18: 582-587, 1971.
43. Stingl H, Krssak M, Krebs M, Bischof MG, Nowotny P, Furnsinn C, Shulman GI, Waldhausl W, and Roden M. Lipid-dependent control of hepatic glycogen stores in healthy humans. Diabetologia 44: 48-54, 2001.
44. Tan AWH and Nuttall FQ. Characteristics of the dephosphorylated form of phosphorylase purified from rat liver and measurement of its activity in crude liver preparation. Biochim Biophys Acta 410: 45-60, 1975.
45. Treadway JL, Mendys P, and Hoover DJ. Glycogen phosphorylase inhibitors for treatment of type 2 diabetes mellitus. Exp Opin Invest Drugs 10: 439-454, 2001.
46. Van den Berghe G and Jaeken J. Adenylsuccinase deficiency. Adv Exp Med Biol 195: 27-33, 1986.
47. Westphal SA and Nuttall FQ. Comparative characterization of human and rat liver glycogen synthase. Arch Biochem Biophys 292: 479-486, 1992.