Interleukin-1 receptor antagonist: A new therapy for type 2 diabetes mellitus

Journal of Pharmaceutical Sciences

Volumn 101, Issue 5, 2012, Pages 1647-1658

  Akash, Muhammad Sajid Hamid ^a   Shen, Qi ^a   Rehman, Kanwal ^a   Chen, Shuqing ^a  

^a ZHEJIANG UNIVERSITY   (China)

Author keywords

Absorption; Control release delivery; Drug delivery approaches; IL 1Ra; Proinflammatory mediators; Protein delivery; Protein formulation; Protein stability; Type 2 diabetes mellitus

Indexed keywords

2,4 THIAZOLIDINEDIONE DERIVATIVE; CHEMOKINE; CHLORPROPAMIDE; DIPEPTIDYL PEPTIDASE IV INHIBITOR; EXENITIDE; GLIBENCLAMIDE; GLUCAGON LIKE PEPTIDE 1 DERIVATIVE; INSULIN; INTERLEUKIN 1 RECEPTOR BLOCKING AGENT; INTERLEUKIN 6; LEPTIN; LIRAGLUTIDE; MEGLITINIDE; METFORMIN; NATEGLINIDE; PIOGLITAZONE; RECOMBINANT HUMAN SERUM ALBUMIN; REPAGLINIDE; ROSIGLITAZONE; SALSALATE; SAXAGLIPTIN; SIBUTRAMINE; SITAGLIPTIN; SULFONYLUREA; TETRAHYDROLIPSTATIN; TUMOR NECROSIS FACTOR ALPHA; UNCLASSIFIED DRUG; VILDAGLIPTIN; ANTIINFLAMMATORY AGENT; AUTACOID;

ANTIINFLAMMATORY ACTIVITY; APOPTOSIS; BIOLOGICAL ACTIVITY; CONSTIPATION; DIARRHEA; DRUG APPROVAL; DRUG HALF LIFE; EDEMA; FOOD AND DRUG ADMINISTRATION; HEART DEFECT; HEART DISEASE; HEAT SENSITIVITY; HUMAN; HYPOGLYCEMIA; IN VITRO STUDY; INFLAMMATION; INJECTION SITE REACTION; INSOMNIA; LACTIC ACIDOSIS; MACROVASCULAR DISEASE; MICROANGIOPATHY; NAUSEA; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; OVERNUTRITION; OXIDATIVE STRESS; PICHIA PASTORIS; RESPIRATORY TRACT INFECTION; REVIEW; SIDE EFFECT; STOMACH DISEASE; THERAPY EFFECT; URINARY TRACT INFECTION; VASCULAR DISEASE; WEIGHT GAIN; HALF LIFE TIME; PATHOPHYSIOLOGY; PHYSIOLOGY; UNITED STATES;

ANTI-INFLAMMATORY AGENTS; DIABETES MELLITUS, TYPE 2; DRUG APPROVAL; HALF-LIFE; HUMANS; INFLAMMATION MEDIATORS; INTERLEUKIN 1 RECEPTOR ANTAGONIST PROTEIN; OXIDATIVE STRESS; UNITED STATES; UNITED STATES FOOD AND DRUG ADMINISTRATION;

EID: 84863712145     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.23057     Document Type: Review

References (121)

1. Donath MY, Ellingsgaard H, Schumann DM, Perren A, Faulenbach M, Ehses JA. 2008. Islet inflammation in type 2 diabetes: From metabolic stress to therapy. Diabetes Care 31:S161-S164.
2. Dinarello CA. 2011. Blocking interleukin-1β in acute and chronic autoinflammaotry diseases. J Intern Med 269:16-28.
3. Aggeli IK, Theofilatos D, Beis I, Gaitanaki C. 2011. Insulin-induced oxidative stress upregulates heme oxygenase-1 via diverse signaling cascades in the C2 skeletal myoblast cell line. Endocrinology 152:1274-1283.
4. Schroder K, Zhou R, Tschopp J. 2010. The NLRP3 inflammasome: A sensor for metabolic danger? Science 327:296-300.
5. Wild S, Roglic G, Green A, Sicree R, King H. 2004. Global prevalence of diabetes: Estimates for the year 2000 and projections for 2030. Diabetes Care 27:1047-1053.
6. Sachdeva MM, Stoffers DA. 2009. Minireview: Meeting the demand for insulin: Molecular mechanisms of adaptive postnatal β-cell mass expansion. Mol Endocrinol 23:747-758.
7. Wellen KE, Hotamisligil GS. 2005. Inflammation, stress, and diabetes. J Clin Invest 115:1111-1119.
8. Navab M, Gharavi N, Watson AD. 2008. Inflammation and metabolic disorders. Curr Opin Clin Nutr Metab Care 11:459-464.
9. Zhao YF, Feng DD, Chen C. 2006. Contribution of adipocyte-derived factors to β-cell dysfunction in diabetes. Int J Biochem Cell Biol 38:804-819.
10. Butler AE, Janson J, Bonner-Weir S, Ritzel R, Rizza RA, Butler PC. 2003. Beta-cell deficit and increased beta-cell apoptosis in humans with type 2 diabetes. Diabetes 52:102-110.
11. Donath MY, Halban PA. 2004. Decreased beta-cell mass in diabetes: Significance, mechanisms and therapeutic implications. Diabetologia 47:581-589.
12. Kolb H, Mandrup-Poulsen T. 2005. An immune origin of type 2 diabetes? Diabetologia 48:1038-1050.
13. Sauter NS, Schulthess FT, Galasso R, Castellani LW, Maedler K. 2008. The anti-inflammatory cytokine interleukin-1 receptor antagonist protects from high-fat diet-induced hyperglycemia. Endocrinology 149:2208-2218.
14. Bonner-Weir S. 2001. β-Cell turnover: Its assessment and implications. Diabetes 50:S20-S24.
15. Johnson JD, Ahmed NT, Luciani DS, Han Z, Tran H, Fujita J, Misler S, Edlund H, Polonsky KS. 2003. Increased islet apoptosis in Pdx1+/- mice. J Clin Invest 111:1147-1160.
16. Tilg H, Moschen AR. 2008. Inflammatory mechanisms in the regulation of insulin resistance. Mol Med 14:222-231.
17. Ehses JA, Ellingsgaard H, Boni-Schnetzler M, Donath MY. 2009. Pancreatic islet inflammation in type 2 diabetes: From α and β cell compensation to dysfunction. Arch Physiol Biochem 115:240-247.
18. Shanmugam N, Reddy MA, Guha M, Natarajan R. 2003. High glucose-induced expression of proinflammatory cytokine and chemokine genes in monocytic cells. Diabetes 52:1256-1264.
19. Homo-Delarche F, Calderari S, Irminger JC, Gangnerau MN, Coulaud J, Rickenbach K, Dolz M, Halban P, Portha B, Serradas P. 2006. Islet inflammation and fibrosis in a spontaneous model of type 2 diabetes, the GK rat. Diabetes 55:1625-1633.
20. Osborn O, Brownell SE, Sanchez-Alavez M, Salomon D, Gram H, Bartfai T. 2008. Treatment with an interleukin 1 antibody improves glycemic control in diet-induced obesity. Cytokine 44:141-148.
21. Dinarello CA. 2004. Therapeutic strategies to reduce IL-1 activity in treating local and systemic inflammation. Curr Opin Pharmacol 4:378-385.
22. Bryant C, Fitzgerald KA. 2009. Molecular mechanisms involved in inflammasome activation. Trends Cell Biol 19:455-464.
23. Guarda G, So A. 2010. Regulation of inflammasome activity. Immunology 130:329-336.
24. Maedler K, Sergeev P, Ris F, Oberholzer J, Joller-Jemelka HI, Spinas GA, Kaiser N, Halban PA, Donath MY. 2002. Glucose-induced β-cell production of IL-1β contributes to glucotoxicity in human pancreatic islets. J Clin Invest 110:851-860.
25. Maedler K, Sergeev P, Ehses JA, Mathe Z, Bosco D, Berney T, Dayer JM, Reinecke M, Halban PA, Donath MY. 2004. Leptin modulates β cell expression of IL-1 receptor antagonist and release of IL-1β in human islets. Proc Natl Acad Sci U S A 101:8138-8143.
26. BöniBöniBöni-Schnetzler M, Thorne J, Parnaud G, Marselli L, Ehses JA, Kerr-Conte J, Pattou F, Halban PA, Weir GC, Donath MY. 2008. Increased interleukin (IL)-1betamessenger ribonucleic acid expression in beta-cells of individuals with type 2 diabetes and regulation of IL-1beta in human islets by glucose and autostimulation. J Clin Endocrinol Metab 93:4065-4074.
27. Boni-Schnetzler M, Boller S, Debray S, Bouzakri K, Meier DT, Prazak R, Kerr-Conte J, Pattou F, Ehses JA, Schuit FC, Donath MY. 2009. Free fatty acids induce a proinflammatory response in islets via the abundantly expressed interleukin-1 receptor I. Endocrinology 150:5218-5229.
28. Ehses JA, Perren A, Eppler E, Ribaux P, Pospisilik JA, Maor-Cahn R, Gueripel X, Ellingsgaard H, Schneider MKJ, Biollaz G, Fontana A, Reinecke M, Homo-Delarche F, Donath MY. 2007. Increased number of islet associated macrophages in type 2 diabetes. Diabetes 56:2356-2370.
29. Mandrup-Poulsen T, Bendtzen K, Nerup J, Dinarello CA, Svenson M, Nielsen JH. 1986. Affinity-purified human interleukin I is cytotoxic to isolated islets of Langerhans. Diabetologia 29:63-67.
30. Mandrup-Poulsen T. 1996. The role of interleukin-1 in the pathogenesis of IDDM. Diabetologia 39:1005-1029.
31. Donath MY, Ehses JA, Maedler K, Schumann DM, Ellingsgaard H, Eppler E, Reinecke M. 2005. Mechanisms of beta-cell death in type 2 diabetes. Diabetes 54:S108-S113.
32. Mine TMK, Okutsu T, Mitsui A, Kitahara Y. 2004. Gene expression profile in the pancreatic islets of Goto-Kakizaki (GK) rats with repeated postprandial hyperglycemia. Diabetes 53:2475A.
33. Butler AE, Jang J, Gurlo T, Carty MD, Soeller WC, Butler PC. 2004. Diabetes due to a progressive defect in β-cell mass in rats transgenic for human islet amyloid polypeptide (HIP rat): A new model for type 2 diabetes. Diabetes 53:1509-1516.
34. Marculescu R, Endler G, Schillinger M, Iordanova N, Exner M, Hayden E, Huber K, Wagner O, Mannhalter C. 2002. Interleukin-1 receptor antagonist genotype is associated with coronary atherosclerosis in patients with type 2 diabetes. Diabetes 51:3582-3585.
35. Maedler K, Dharmadhikari G, Schumann DM, Storling J. 2009. Interleukin-1 beta targeted therapy for type 2 diabetes. Expert Opin Biol Ther 9:1177-1188.
36. Larsen CM, Faulenbach M, Vaag A, Ehses JA, Donath MY, Mandrup-Poulsen T. 2009. Sustained effects of interleukin-1 receptor antagonist treatment in type 2 diabetes. Diabetes Care 32:1663-1668.
37. Hotamisligil GS, Shargill NS, Spiegelman BM. 1993. Adipose expression of tumor necrosis factor-alpha: Direct role in obesity-linked insulin resistance. Science 259:87-91.
38. Hotamisligil GS, Budavari A, Murray D, Spiegelman BM. 1994. Reduced tyrosine kinase activity of the insulin receptor in obesity-diabetes. Central role of tumor necrosis factor-alpha. J Clin Invest 94:1543-1549.
39. Burks DJ, White MF. 2001. IRS proteins and beta-cell function. Diabetes 50:S140-S145.
40. Rosenvinge A, Krogh-Madsen R, Baslund B, Pedersen BK. 2007. Insulin resistance in patients with rheumatoid arthritis: Effect of anti-TNFα therapy. Scand J Rheumatol 36:91-96.
41. Dominguez H, Storgaard H, Rask-Madsen C, Hermann TS, Ihlemann N, Nielsen DB, Spohr C, Kober L, Vaag A, Torp-Pedersen C. 2005. Metabolic and vascular effects of tumor necrosis factor-α blockade with etanercept in obese patients with type 2 diabetes. J Vasc Res 42:517-525.
42. Mooney RA. 2007. Counterpoint: Interleukin-6 does not have a beneficial role in insulin sensitivity and glucose homeostasis. J Appl Physiol 102:816-818.
43. Pedersen BK, Febbraio MA. 2007. Point: Interleukin-6 does have a beneficial role in insulin sensitivity and glucose homeostasis. J Appl Physiol 102:814-816.
44. Lagathu C, Bastard JP, Auclair M, Maachi M, Capeau J, Caron M. 2003. Chronic interleukin-6 (IL-6) treatment increased IL-6 secretion and induced insulin resistance in adipocyte: Prevention by rosiglitazone. Biochem Biophys Res Commun 311:372-379.
45. Rotter V, Nagaev I, Smith U. 2003. Interleukin-6 (IL-6) induces insulin resistance in 3T3-L1 adipocytes and is, like IL-8 and tumor necrosis factor-alpha, overexpressed in human fat cells from insulin-resistant subjects. J Biol Chem 278:45777-45784.
46. Cai D, Yuan M, Frantz DF, Melendez PA, Hansen L, Lee J, Shoelson SE. 2005. Local and systemic insulin resistance resulting from hepatic activation of IKK-β and NF-κB. Nat Med 11:183-190.
47. Donath MY, Shoelson SE. 2011. Type 2 diabetes as an inflammatory disease. Nat Rev Immunol 11:98-107.
48. Kern PA, Ranganathan S, Li C, Wood L, Ranganathan G. 2001. Adipose tissue tumor necrosis factor and interleukin-6 expression in human obesity and insulin resistance. Am J Physiol Endocrinol Metab 280:E745-E751.
49. Kirwan JP, Jing M. 2002. Modulation of insulin signaling in human skeletal muscle in response to exercise. Exerc Sport Sci Rev 30:85-90.
50. Emanuelli B, Peraldi P, Filloux C, Sawka-Verhelle D, Hilton D, Obberghen EV. 2000. SOCS-3 is an insulin-induced negative regulator of insulin signaling. J Biol Chem 275:15985-15991.
51. Fève B, Bastard JP. 2009. The role of interleukins in insulin resistance and type 2 diabetes mellitus. Nat Rev Endocrinol 5:305-311.
52. Pradhan AD, Manson JE, Rifai N, Buring JE, Ridker PM. 2001. C-reactive protein, interleukin 6, and risk of developing type 2 diabetes mellitus. JAMA 286:327-334.
53. Ogata A, Morishima A, Hirano T, Hishitani Y, Hagihara K, Shima Y, Narazaki M, Tanaka T. 2011. Improvement of HbA1c during treatment with humanised anti-interleukin 6 receptor antibody, tocilizumab. Ann Rheum Dis 70:1164-1165.
54. Otero M, Lago R, Lago F, Casanueva FF, Dieguez C, Gómez-Reino JJ, Gualillo O. 2005. Leptin, from fat to inflammation: Old questions and new insights. FEBS Lett 579:295-301.
55. Maedler K, Schulthess FT, Bielman C, Berney T, Bonny C, Prentki M, Donath MY, Roduit R. 2008. Glucose and leptin induce apoptosis in human β-cells and impair glucose-stimulated insulin secretion through activation of c-Jun N-terminal kinases. FASEB J 22:1905-1913.
56. Herder C, Baumert J, Thorand B, Koenig W, De Jager W, Meisinger C, Illig T, Martin S, Kolb H. 2006. Chemokines as risk factors for type 2 diabetes: Results from the MONICA/KORA Augsburg study, 1984-2002. Diabetologia 49:921-929.
57. Jiao P, Chen Q, Shah S, Du J, Tao B, Tzameli I, Yan W, Xu H. 2009. Obesity-related upregulation of monocyte chemotactic factors in adipocytes: Involvement of nuclear factor-κB and c-Jun NH2-terminal kinase pathways. Diabetes 58:104-115.
58. Lacraz G, Giroix M, Kassis N, Coulaud J, Galinier A, Noll C, Cornut M, Schmidlin F, Paul JL, Janel N, Irminger JC, Kergoat M, Portha B, Donath MY, Ehses JE, Homo-Delarche F. 2009. Islet endothelial activation and oxidative stress gene expression is reduced by IL-1Ra treatment in the type 2 diabetic GK rat. PLoS One 4:e6963.
59. Calles-Escandon J, Cipolla M. 2001. Diabetes and endothelial dysfunction: A clinical perspective. Endocr Rev 22:36-52.
60. Rojas A, Figueroa H, Re L, Morales MA. 2006. Oxidative stress at the vascular wall. Mechanistic and pharmacological aspects. Arch Med Res 37:436-448.
61. Hayden MR, Sowers JR. 2007. Isletopathy in type 2 diabetes mellitus: Implications of islet RAS, islet fibrosis, islet amyloid, remodeling, and oxidative stress. Antioxid Redox Signal 9:891-910.
62. Dedon PC, Tannenbaum SR. 2004. Reactive nitrogen species in the chemical biology of inflammation. Arch Biochem Biophys 423:12-22.
63. Charo IF, Ransohoff RM. 2006. The many roles of chemokines and chemokine receptors in inflammation. N Engl J Med 354:610-621.
64. Donath MY, Boni-Schnetzler M, Ellingsgaard H, Ehses JA. 2009. Islet inflammation impairs the pancreatic β-cell in type 2 diabetes. Physiology (Bethesda) 24:325-331.
65. Maedler K, Spinas GA, Dyntar D, Moritz W, Kaiser N, Donath MY. 2001. Distinct effects of saturated and monounsaturated fatty acids on β-cell turnover and function. Diabetes 50:69-76.
66. Roehrich ME, Mooser V, Lenain V, Herz J, Nimpf J, Azhar S, Bideau M, Capponi A, Nicod P, Haefliger JA, Waeber G. 2003. Insulin-secreting β-cell dysfunction induced by human lipoproteins. J Biol Chem 278:18368-18375.
67. Shi H, Kokoeva MV, Inouye K, Tzameli I, Yin H, Flier JS. 2006. TLR4 links innate immunity and fatty acid-induced insulin resistance. J Clin Invest 116:3015-3025.
68. Gaisano HY, Ostenson CG, Sheu L, Wheeler MB, Efendic S. 2002. Abnormal expression of pancreatic islet exocytotic soluble N-ethylmaleimide-sensitive factor attachment protein receptors in Goto-Kakizaki rats is partially restored by phlorizin treatment and accentuated by high glucose treatment. Endocrinology 143:4218-4226.
69. Briaud I, Kelpe CL, Johnson LM, Tran PO, Poitout V. 2002. Differential effects of hyperlipidemia on insulin secretion in islets of langerhans from hyperglycemic versus normoglycemic rats. Diabetes 51:662-668.
70. Ehses JA, Meier DT, Wueest S, Rytka J, Boller S, Wielinga PY, Schraenen A, Lemaire K, Debray S, Van-Lommel L, Pospisilik JA, Tschopp O, Schultze SM, Malipiero U, Esterbauer H, Ellingsgaard H, Rütti S, Schuit FC, Lutz TA, Boni-Schnetzler M, Konrad D, Donath MY. 2010. Toll-like receptor 2-deficient mice are protected from insulin resistance and β cell dysfunction induced by a high-fat diet. Diabetologia 53:1795-1806.
71. Haversen L, Danielsson KN, Fogelstrand L, Wiklund O. 2009. Induction of proinflammatory cytokines by long-chain saturated fatty acids in human macrophages. Atherosclerosis 202:382-393.
72. Zhou R, Tardivel A, Thorens B, Choi I, Tschopp J. 2010. Thioredoxin-interacting protein links oxidative stress to inflammasome activation. Nat Immunol 11:136-140.
73. Noor A, Gunasekaran S, Soosaimanickam A, Vijayalakshami MA. 2008. Antidiabetic activity of Aloe vera and histology of organs in streptozotocin induced diabetic rats. Curr Sci 94:1070-1075.
74. Prasad SK, Kulshreshtha A, Qureshi TN. 2009. Antidiabetic activity of some herbal plants in streptozotocin induced diabetic albino rats. Pak J Nutr 8:551-557.
75. Maritim AC, Sanders RA, Watkins III JB. 2003. Oxidative stress and antioxidants: A review. J Biochem Mol Toxicol 17:24-38.
76. Meigs JB, Rutter MK, Sullivan LM, Fox CS, D'Agostino RB Sr, Wilson PW. 2007. Impact of insulin resistance on risk of type 2 diabetes and cardiovascular disease in people with metabolic syndrome. Diabetes Care 30:1219-1225.
77. Evans JL, Goldfine ID, Maddux BA, Grodsky GM. 2002. Oxidative stress and stress-activated signaling pathways: A unifying hypothesis of type 2 diabetes. Endocr Rev 23:599-622.
78. Stocker R, Keaney JF Jr. 2004. Role of oxidative modifications in atherosclerosis. Physiol Rev 84:1381-1478.
79. Gloire G, Legrand-Poels S, Piette J. 2006. NF-kappa B activation by reactive oxygen species: Fifteen years later. Biochem Pharmacol 72:1493-1505.
80. Evans JL, Goldfine ID, Maddux BA, Grodsky GM. 2003. Are oxidative stress-activated signaling pathways mediators of insulin resistance and β-cell dysfunction? Diabetes 52:1-8.
81. Kaneto H, Katakami N, Kawamori D, Miyatsuka T, Sakamoto K, Matsuoka TA, Matsuhisa M, Yamasaki Y. 2007. Involvement of oxidative stress in the pathogenesis of diabetes. Antioxid Redox Signal 9:355-366.
82. Colagiuri S. 2010. Diabesity: Therapeutic options. Diabetes Obes Metab 12:463-473.
83. Niswender K. 2010. Diabetes and obesity: Therapeutic targeting and risk reduction-A complex interplay. Diabetes Obes Metab 12:267-287.
84. Provilus A, Abdallah M, McFarlane SI. 2011. Weight gain associated with antidiabetic medications. Therapy 8:113-120.
85. Kahn SE, Haffner SM, Heise MA, Herman WH, Holman RR, Jones NP, Kravitz BG, Lachin JM, O'Neill MC, Zinman B, Viberti G. 2006. Glycemic durability of rosiglitazone, metformin, or glyburide monotherapy. N Engl J Med 355:2427-2443.
86. DeFronzo RA, Tripathy D, Schwenke DC, Banerji M, Bray GA, Buchanan TA, Clement ST, Henry RR, Hodis HN, Kitabchi AE, Mack WJ, Mudaliar S, Ratner RE, Williams K, Stentz FB, Musi N, Reaven PD. 2011. Pioglitazone for diabetes prevention in impaired glucose tolerance. N Engl J Med 364:1104-1115.
87. Alvarsson M, Sundkvist G, Lager I, Berntorp K, Fernqvist-Forbes E, Steen L, Orn T, Holberg MA, Kirksaether N, Grill V. 2008. Effects of insulin vs. glibenclamide in recently diagnosed patients with type 2 diabetes: A 4-year follow-up. Diabetes Obes Metab 10:421-429.
88. Chyka PA, Erdman AR, Christianson G, Wax PM, Booze LL, Manoguerra AS, Caravati EM, Nelson LS, Olson KR, Cobaugh DJ, Scharam EJ, Woolf AD, Troutman WG. 2007. Salicylate poisoning: An evidence-based consensus guideline for out-of-hospital management. Clin Toxicol (Phila) 45:95-131.
89. Larsen CM, Faulenbach M, Vaag A, Vølund A, Ehses JA, Seifert B, Mandrup-Poulsen T, Donath MY. 2007. Interleukin-1 receptor antagonist in type 2 diabetes mellitus. N Engl J Med 356:1517-1526.
90. Mandrup-Poulsen T, Pickersgill L, Donath MY. 2010. Blockade of interleukin 1 in type 1 diabetes mellitus. Nat Rev Endocrinol 6:158-166.
91. Owyang AM, Issafras H, Corbin J, Ahluwalia K, Larsen P, Pongo E, Handa M, Horwitz AH, Roell MK, Haak-Frendscho M, Masat L. 2011. XOMA 052, a potent, high-affinity monoclonal antibody for the treatment of IL-1β-mediated diseases. Landes Biosci 3(1):49-60.
92. Yuan M, Konstantopoulos N, Lee J, Hansen L, Li ZW, Karin M, Shoelson SE. 2001. Reversal of obesity- and diet-induced insulin resistance with salicylates or targeted disruption of IKKβ. Science 293:1673-1677.
93. Shoelson SE, Lee J, Goldfine AB. 2006. Inflammation and insulin resistance. J Clin Invest 116:1793-1801.
94. Fleischman A, Shoelson SE, Bernier R, Goldfine AB. 2008. Salsalate improve glycemia and inflammatory parameters in obese young adults. Diabetes Care 31:289-294.
95. Hundal RS, Petersen KF, Mayerson AB, Randhawa PS, Inzucchi S, Shoelson SE, Shulman GI. 2002. Mechanism by which high-dose aspirin improves glucose metabolism in type 2 diabetes. J Clin Invest 109:1321-1326.
96. Zumsteg U, Reimers JI, Pociot F, Mørch L, Helqvist S, Alejandro R, Mandrup-Poulsen T, Dinarello CA, Nerup J. 1993. Differential interleukin-1 receptor antagonism on pancreatic beta and alpha cells: Studies in rodent and human islets and in normal rats. Diabetologia 36:759-766.
97. Dinarello CA. 1996. Biologic basis for interleukin-1 in disease. Blood 87:2095-2147.
98. Cawthorne C, Prenant C, Smigova A, Julyan P, Maroy R, Herholz K, Rothwell N, Boutin H. 2011. Biodistribution, pharmacokinetics and metabolism of interleukin-1 receptor antagonist (IL-1RA) using [18F]-IL1RA and PET imaging in rats. Br J Pharmacol 162:659-672.
99. Holt LJ, Basran A, Jones K, Chorlton J, Jespers SL, Brewis ND, Tomlinson IM. 2008. Anti-serum albumin domain antibodies for extending the half-lives of short lived drugs. Protein Eng Des Sel 21:283-288.
100. Ehses JA, Lacraz G, Giroix M, Schmidlin F, Coulaud J, Kassis N, Irminger JC, Kergoat M, Portha B, Homo-Delarche F, Donath MY. 2009. IL-1 antagonism reduces hyperglycemia and tissue inflammation in the type 2 diabetic GK rat. Proc Natl Acad Sci U S A 106:13998-14003.
101. Betre H, Liu W, Zalutsky MR, Chilkoti A, Kraus VB, Setton LA. 2006. A thermally responsive biopolymer for intra-articular drug delivery. J Control Release 115:175-82.
102. Urry DW, Parker TM, Reid MC, Gowda DC. 1991. Biocompatibility of the bioelastic materials, poly(GVGVP) and its γ-irradiation cross-linked matrix: Summary of generic biological test results. J Bioact Compat Polym 6:263-82.
103. Shamji MF, Betre H, Kraus VB, Chen J, Chilkoti A, Pichika R, Masuda K, Setton LA. 2007. Development and characterization of a fusion protein between thermally responsive elastin-like polypeptide and interleukin-1 receptor antagonist: Sustained release of a local anti-inflammatory therapeutic. Arthritis Rheum 56:3650-3661.
104. Pichika R, Betre H, Setton LA, An HS, Masuda K. 2006. Bioactivity of IL-1 receptor antagonist (IL1Ra) and a related fusion protein in inhibiting IL-1-mediated effects in human intervertebral disc cells. Trans Orthop Res Soc 52. p 1198.
105. Kim DH, Smith JT, Chilkoti A, Reichert WM. 2007. The effect of covalently immobilized rhIL-1ra-ELP fusion protein on the inflammatory profile of LPS-stimulated human monocytes. Biomaterials 28:3369-3377.
106. Christensen T, Amiram M, Dagher S, Trabbic-Carlson K, Shamji MF, Setton LA, Chilkoti A. 2009. Fusion order controls expression level and activity of elastin-like polypeptide fusion proteins. Protein Sci 18:1377-1387.
107. Osborn BL, Olsen SH, Nardelli B, Murray JH, Zhou JXH, Garcia A, Moody G, Zaritskaya LS, Sung C. 2002. Pharmacokinetic and pharmacodynamic studies of a human serum albumin-interferon-α fusion protein in cynomolgus monkeys. J Pharmacol Exp Ther 303:540-548.
108. Subramanian GM, Fiscella M, Lamousé-Smith A, Zeuzem S, McHutchison JG. 2007. Albinterferon α-2b: A genetic fusion protein for the treatment of chronic hepatitis C. Nature Biotech 25:1411-1419.
109. Kratz F. 2008. Albumin as a drug carrier: Design of prodrugs, drug conjugates and nanoparticles. J Control Release 132:171-183.
110. Dai SF, Shen Q, Chen S. 2008. Inhomogeneous expression of fusion protein HSA/IL-1Ra Pichia pastoris. Zhejiang Da Xue Xue Bao Yi Xue Ban 37:134-138.
111. Shen Q, Chen S. 2009. Purification of fusion protein HSA/IL-1Ra and its bioactivity. Zhejiang Da Xue Xue Bao Yi Xue Ban 38:260-264.
112. Lavi G, Dinarello CA, Apte RN, Cohen S. 2005. Sustained release of IL-1Ra from biodegradable microspheres prolongs its IL-1-neutralizing effects. Israel J Chem 45:457-464.
113. Lavi G, Voronov E, Dinarello CA, Apte RN, Cohen S. 2007. Sustained delivery of IL-1Ra from biodegradable microspheres reduces the number of murine B16 melanoma lung metastases. J Control Release 123:123-130.
114. Jun JB, Kim JK, Kim TH, Na YI, Choi CH, Kim YH. 2011. Inhibition of the IL-1β-induced expression of matrix metalloproteinases by controlled release of IL-1 receptor antagonist using injectable and thermo-reversible gels in human osteoarthritis chondrocytes. J Rheum Dis 18:85-93.
115. Akash MSH, Shen Q, Wang H, Rehman K, Sun H, Xu Y, Gao J, Chen S. Formulation development and sustained release of IL-1Ra from Pluronic F127 based thermosensitive gel. Pharm Res (manuscript submitted).
116. Barichello JM, Morishita M, Takayama K, Nagai T. 1999. Absorption of insulin from Pluronic F-127 gels following subcutaneous administration in rats. Int J Pharm 184:189-198.
117. Katakam M, Bell LN, Banga AK. 1995. Effect of surfactants on the physical stability of rhGH. J Pharm Sci 84:713-716.
118. Stratton LP, Dong A, Manning MC, Carpenter JF. 1997. Drug delivery matrix containing native protein precipitates suspended in a polomaxamer gel. J Pharm Sci 86:1006-1010.
119. Liu Y, Lu WL, Wang JC, Zhang X, Zhang H, Wang XQ, Zhou TY, Zhang Q. 2007. Controlled delivery of recombinant hirudin based on thermo-sensitive Pluronic® F127 hydrogel for subcutaneous administration: In vitro and in vivo characterization. J Control Release 117:387-395.
120. Johnston TP, Punjabi MA, Froelich CJ. 1992. Sustained delivery of interleukin-2 from a poloxamer 407 gel matrix following intraperitoneal injection in mice. Pharm Res 9:425-434.
121. Dinarello CA. 2005. The many worlds of reducing interleukin-1. Arthritis Rheum 52:1960-1967.