
SCIENTIFIC PUBLICATIONS
The publications listed below have been authored or co-authored by AtheroGenics personnel. Titles may be linked to sites where the abstract of the publication is located. AtheroGenics is not responsible for, and does not endorse, the content of links to external web sites.
AGI-1067, a Novel Antioxidant and Anti-Inflammatory Agent, Inhibits Activation of JNK, IRS-1 Serine Phosphorylation and Cytokine Production in Adipocytes
Chen X, Dodd G, Sundell C, Kunsch C
Poster Presentation at the American Diabetes Association 68th Scientific Sessions, June 2008
AGI-1067, A Novel Antioxidant and Anti-Inflammatory Agent, Improves Insulin Sensitivity in a Rat Model of Diet-Induced Obesity
Sundell C, Kosgerau K, Chen X, Dodd G, Tang-Christensen M, Kunsch C
Poster Presentation at the American Diabetes Association 68th Scientific Sessions, June 2008
AGI-1067 Improves Glycemic Control When Added to Current Regimens in Patients with Type 2 Diabetes
Klug E, Pfeffer M, McMurray J, Fleming G, Long W, Small R, Tardif J-C, for the ARISE Trial Investigators
Poster Presentation at the American Diabetes Association 68th Scientific Sessions, June 2008
Effects of succinobucol (AGI-1067) after an acute coronary syndrome: a randomized, double-blind, placebo-controlled trial
Jean-Claude Tardif, John J V McMurray, Eric Klug, Robert Small, Jennifer Schumi, Jasmine Choi, Jim Cooper, Robert Scott, Eldrin F Lewis, Philippe L L’Allier, Marc A Pfeffer, for the Aggressive Reduction of Inflammation Stops Events (ARISE) Trial Investigators
http://www.thelancet.com Vol 371 May 24, 2008
AGI-1067, a novel vascular protectant, anti-inflammatory drug and mild antiplatelet agent for treatment of atherosclerosis
Victor L. Serebruany, Alex Malinin, Christian Eisert and Stephen Ong
Expert Rev. Cardiovasc. Ther. 5(4), 635-641 (2007)
A Novel Class of Antioxidants Inhibit LPS Induction of Tissue Factor by Selective Inhibition of the Activation of ASK1 and MAP Kinases
James P. Luyendyk, J. Daniel Piper, Michael Tencati, K. Veera Reddy, Todd Holscher, Rong Zhang, Jayraz Luchoomun, Xilin Chen, Wang Min, Charles Kunsch, Nigel Mackman
Arterioscler Thromb Vasc Biol. (June 7, 2007) DOI: 10.1161/ATVBAHA.107.143552
Assessment of Lipoprotein Profiles (ALPS study) and Antioxidant Activity in Healthy Subjects Treated with AGI-1067
MH Davidson, J Smith, R Scott, R Small, J Choi, JP Kane, and the ALPS Investigators from the Section of Preventive Medicine, Department of Cardiology, Rush University College of Medicine, Chicago, IL and Radiant Research, Chicago, IL; AtheroGenics, Inc., Alpharetta, GA; and Departments of Medicine, Biochemistry and Biophysics, University of California, School of Medicine, San Francisco, CA
Presented June 22, 2006 at the XIV International Symposium on ATHEROSCLEROSIS, Rome, in the Poster Session on “Pharmacological control of lipids and lipoproteins.”
Effects of the antioxidant succinobucol (AGI-1067) on human atherosclerosis in a randomized clinical trial
Jean-Claude Tardif, Jean Grégoire, Philippe L. L’Allier, Reda Ibrahim, Todd J. Anderson, François Reeves, Lawrence M. Title, Erick Schampaert, Michel LeMay, Jacques Lespérance et al.
Atherosclerosis (2007), doi:10.1016/j.atherosclerosis.2006.11.039
Assessment of Lipoprotein Profiles (ALPS study) and Antioxidant Activity in Healthy Subjects Treated with AGI-1067
MH Davidson, J Smith, R Scott, R Small, J Choi, JP Kane, and the ALPS Investigators from the Section of Preventive Medicine, Department of Cardiology, Rush University College of Medicine, Chicago, IL and Radiant Research, Chicago, IL; AtheroGenics, Inc., Alpharetta, GA; and Departments of Medicine, Biochemistry and Biophysics, University of California, School of Medicine, San Francisco, CA
Presented June 22, 2006 at the XIV International Symposium on ATHEROSCLEROSIS, Rome, in the Poster Session on “Pharmacological control of lipids and lipoproteins.”
Activation of Nrf2/ARE pathway protects endothelial cells from oxidant injury and inhibits inflammatory gene expression.
Chen XL, Dodd G, Thomas S, Zhang X, Wasserman MA, Rovin BH, Kunsch
JAJP – Heart 290:1862-1870, 2006.
Abstract:
AGI-1067, An Antioxidant, Anti-Inflammatory Vascular Protectant, Reduces Activity in Platelets from Subjects with Multiple Risk Factors for Vascular Disease
Serebruany V, Malinin A, Scott, R.
J Oral presentation at 2005 American Heart Association Scientific Sessions.
Discovery of novel phenolic antioxidants as inhibitors of vascular cell adhesion molecule-1 expression for use in chronic inflammatory diseases.
Meng CG, Somers PK, Hoong LK, Zheng XS, Ye Z, Worsencroft KJ, Simpson JE, Hotema MR, Weingarten MD, MacDonald ML, Hill RR, Marino EM, Suen KL, Luchoomun J, Kunsch C, Landers LK, Stefanopoulos D, Howard RB, Sundell CL, Saxena U, Wasserman MA, Sikorski JA.
J Med Chem. 2004 Dec 2; 47(25):6420-32
Sphingosine Kinase-1 mediates TNF-alpha-induced MCP-1 gene expression in endothelial cells: upregulation by oscillatory flow.
Chen XL, Grey JY, Thomas S, Qiu FH, Medford RM, Wasserman MA, Kunsch C.
Am J Physiol Heart Circ Physiol. 2004 Oct; 287(4):H1452-8
A new era in atherosclerosis drug discovery
Meng CQ.
Expert Rev Cardiovasc Ther. 2004 Sep; 2(5):633-6
Effects of AGI-1096, a novel antioxidant compound with anti-inflammatory and antiproliferative properties, on rodent allograft arteriosclerosis.
Murata S, Sundell CL, Lijkwan MA, Balsam LB, Hammainen P, Coleman C, York C, Luchoomun J, Suen KL, Howard R, Somers PK, Morris RE, Robbins RC.
ETransplantation. 2004 May 27; 77(10):1494-500
Review: Recent advances in therapeutic chalcones
Ni L, Meng C, Sikorski J
Expert Opin. Ther. Patents (2004) 14(12):1669-1691
Induction of Cytoprotective Genes Through Nrf2/Antioxidant Response Element Pathway: A New Therapeutic Approach for the Treatment of Inflammatory Diseases
Chen, X-L and Kunsch C
Current Pharmaceutical Design, 2004, 10, 879-891
Discovery of novel heteroaryl-substituted chalcones as inhibitors of TNF-alpha-induced VCAM-1 expression
Meng C, Zheng X, Ni L, Zhihong Y, Simpson J, Worsencroft K, Hotema M, Weingarten M, Skudlarek J, Gilmore J, Hoong L, Hill R, Marino E, Suen K-L, Kunsch C, Wasserman M. and Sikorski J.
Bioorganic & Medicinal Chemistry Letters 14 (2004) 1513-1517
Selective Inhibition of Endothelial and Monocyte Redox-Sensitive Genes by AGI-1067: A Novel Antioxidant and Anti-Inflammatory Agent
Kunsch C, Luchoomun J, Grey J, Olliff L, Saint L, Arrendale R, Wasserman M, Saxena U, Medford M.
The Journal of Pharmacology and Experimental Therapeutics
JPET 308:820-829, 2004
Superoxide, H2O2, and iron are required for TNF-alpha-induced MCP-1 gene expression in endothelial cells: role of Rac1 and NADPH oxidase
Chen X-L, Zhang Q, Zhao R, Medford R.
Am J Physiol Heart Circ Physiol 286: H1001-H1007, 2004
Abstract:
Activation of the Nrf2/antioxidant response element pathway protects endothelial cells from oxidant injury and inhibits redox-sensitive inflammatory gene expression: A novel vascular protective pathway
Chen X-L, Thomas S, Wasserman M, Kunsch C.
Oral presentation at 2003 American Heart Association Scientific Sessions.
Abstract:
Design and Synthesis of Novel Chalcones as Potential Treatments for Asthma
Ni L, Meng C, Weingarten M, Ye Z, Simpson J, Skudlarek J, Worsencroft K, Marino E, Qiu F-H, Sundell C, Howard R, Wasserman M, Sikorski J
Presented September 2003 at New York American Chemical Society Meeting.
Abstract:
Effect of Novel Synthetic Chalcone Derivatives on In Vitro Eosinophil Survival, Degranulation and on In Vivo Eosinophilia
J. Luchoomun, J.B. Sedgwick, C.L. Sundell, C.Q. Meng, E.M. Marino, L.K. Landers, K-L. Suen, C. Kunsch, W.W. Busse and M. A. Wasserman
Presented May 20, 2003 at the 99th International Conference of the ATS session entitled, The E Inflammatory Mediators: Eicosanoids and Eosinophils.
Abstract:
A Novel Synthetic Chalcone, Inhibits Eosinophilia, Inflammatory Gene Expression and Airway Hyperresponsiveness in a Murine Asthma Model
C.L. Sundell, L.K. Landers, F.H. Qiu, L. Ni, K.S. Karu, A. Scarborough, M. MacDonald, R.B. Howard, C. Meng, J.A. Sikorski, C. Kunsch and M.A. Wasserman
Presented May 19, 2003 at the 99th International Conference of the ATS session entitled, Asthma Therapy: Effects of Airway Inflammation.
Abstract:
Pharmacologic Inhibition of VCAM-1 Gene Expression and TNF-a Production By A Novel, Synthetic Chalcone: Characterization of AGI-2048 as a New Anti-Inflammatory Agent
F.H. Qiu, E.M. Marino, R.B. Howard, K.S. Karu, D. Stefanopoulos, J. Luchoomun, A. Smith, A.M. Whalen, C.Q. Meng, L. Ni, J.A. Sikorski, K.L. Suen, C.L. Sundell, M.A. Wasserman, and C. Kunsch.
Presented May 18, 2003 at the 99th International Conference of the American Thoracic Society (ATS) session entitled, Macrolides and Anti-inflammatory Therapeutics.
Abstract:
TNF- -induced MCP-1 Expression Is Activated by the RAC1 and NADPH Oxidase-Dependent Pathway in Endothelial Cells: Roles of Superoxide and H2O2.
Chen X-L Zhang Q, Zhao R and Medford R.
Presented May 2003 at the 4th Annual Conference on Arterialsclerosis, Thrombosis and Vascular Biology.
Abstract:
Sphingosine Kinase-1 Is Up-regulated by Oscillatory Flow and Mediates TNF-a-Induced MCP-1 Gene Expression in Endothelial Cells.
Chen X-L, Grey J, Thomas S, Qiu FH, Marino-Rodriguez M, Medford R, Wasserman M, and Kunsch C.
Presented May 2003 at the 4th Annual Conference on Arterialsclerosis, Thrombosis and Vascular Biology.
Rac1 and Superoxide Are Required for the Expression of Cell Adhesion Molecules
Induced by Tumor Necrosis Factor- in Endothelial Cells
Chen X, Zhang Q, Zhao R, Ding X, Tummala P, and Medford R.
The Journal of Pharmacology and Experimental Therapeutics JPET 305:573-580, 2003
Abstract:
Characterization of AGI-2048: a novel synthetic chalcone with multiple anti-inflammatory properties.
Qui F, Sundell C, Karu K, Marino E, Landers L, Howard R, Luchoomun J, Stefanopoulos D, Scarborough A, MacDonald M, Smith A, Whalen A, Suen K, Ni L, Meng C, Sikorski J, Wasserman M, Kunsch C.
Presented April 2003 at the FASEB Experimental Biology 2003 meeting.
AGI-1067: A Multifunctional Phenolic Antioxidant, Lipid Modulator, Anti-Inflammatory and Antiatherosclerotic Agent.
Sundell C, Somers, P, Meng C, Hoong L, Suen K, Hill R, Landers L, Chapman A, Butteiger D, Jones M, Edwards D, Daugherty A, Wasserman M, Alexander R, Medford R, Saxena U.
JPET 305:1116-1123, February 24, 2003
Effects of AGI-1067 and Probucol After Percutaneous Coronary Interventions.
Tardif J-C, Gregoire J, Schwartz L, title L, Laramee L, Reeves F, Lesperance J, Bourassa M, L'Allier P, glass M, Lambert J, Guertin M-C; for the Canadian Antioxidant Restenosis Trial (CART-1) Investigators.
CIRCULATION, Volume 107, Number 4, February 4, 2003
Chemistry and Pharmacology of Vascular Protectants: A Novel Approach to the Treatment of Atherosclerosis and Coronary Artery Disease.
Wasserman M, Sundell C, Kunsch C, Edwards D, Meng C, Medford R.
Am J Cardiol 2003;91(suppl):34A-40A
Lead Discovery of a,B-Unsaturated Sulfones from a Combinatorial Library as Inhibitors of Inducible VCAM-1 Expression
Ni L, Zheng S, Somers P, Hoong L, Hill R, Marina E, Suen K, Saxena U, Meng, C.
Biorganic & Medicinal Chemistry Letters 13 (2003) 745-748
Laminar Flow Induction of Antioxidant Response Element-mediated Genes in Endothelial Cells - A NOVEL ANTI-INFLAMMATORY MECHANISM.
Chen XL, Varner SE, Rao AS, Grey JY, Thomas S, Cook CK, Wasserman MA, Medford RM, Jaiswal AK, Kunsch C.
Journal of Biological Chemistry Vol 278, Issue Jan 10, pp. 703-711, 2003.
Novel phenolic antioxidants as multifunctional inhibitors of inducible VCAM-1 expression for use in atherosclerosis.
Meng CQ, Somers PK, Rachita CL, Holt LA, Hoong LK, Zheng XS, Simpson JE, Hill RR, Olliff LK, Kunsch C, Sundell CL, Parthasarathy S, Saxena U, Sikorski JA, Wasserman MA.
Bioorganic & Medl Chem Ltrs 12(18), 2545-2548, 2002.
Abstract:
AGIX-4207: A novel antioxidant and anti-inflammatory compound inhibits progression of collagen II arthritis in the rat.
Sundell CL, Suen KL, Moore AR, Somers PK, Kunsch C. Discovery Research, AtheroGenics, Inc., Alpharetta, GA Celltech Chiroscience, Berks, UK
FASEB Journal Vol. 16, Nov. 4, PP. A182, March 20, 2002.
April 20-24, 2002, Annual Meeting of the Professional Research Scientists on Experimental Biology, ISSN 0892-6638
Oxidative Stress as a Regulator of Gene Expression in the Vasculature.
Kunsch C and Medford RM.
Circ Res 85(8) Oct 15 1999.
Oscillatory Shear Stress Stimulates Adhesion Molecule Expression in Cultured Human Endothelium.
Chappell, DC, Varner SE, Nerem RM, Medford RM, and Alexander RW.
Circ Res 82(5):532-539, March 23, 1998.
Role of Activating Protein-1 in the Regulation of the Vascular Cell Adhesion Molecule-1 Gene Expression by Tumor Necrosis Factor-alpha.
Ahmad M, Theofanidis P, Medford RM.
J Biol Chem 273(8):4616-4621, February 20, 1998.
Generation of a Polyclonal Antibody Against Lipid Peroxide-Modified Proteins.
Kim JG, Sabbagh F, Santanam N, Wilcox JN, Medford RM, Parthasarathy S.
Free Radic Biol Med 23(2):251-259, 1997.
E-selectin Gene Expression in Vascular Smooth Muscle Cells. Evidence for a Tissue-Specific Repressor Protein.
Chen XL, Tummala PE, Olliff L, Medford RM.
Circ Res 80(3):305-311, March 1997.
Nitric Oxide Regulates Vascular Cell Adhesion Molecule 1 Gene Expression and Redox-Sensitive Transcriptional Events in Human Vascular Endothelial Cells.
Khan BV, Harrison DG, Olbrych MT, Alexander RW, Medford RM.
Proc Natl Acad Sci U S A, 93(17):9114-9119, August 20, 1996.
Selective Inhibition of Tumor Necrosis Factor-Induced Vascular Cell Adhesion Molecule-1 Gene Expression by a Novel Flavonoid: Lack of Effect of Transcription Factor NF-kB.
Wolle J, Hill RR, Ferguson E, Devall LJ, Devall BK, Trivedi BK, Newton RS, Saxena U.
Arterioscler Thromb Vasc Biol 16:1501-1508, 1996.
Activation of the Double-Stranded-RNA-Activated Protein Kinase and Induction of Vascular Cell Adhesion Molecule-1 by Poly (I):Poly (C) in Endothelial Cells.
Offermann MK, Zimring J, Mellits KH, Hagan MK, Shaw R, Medford RM, Mathews MB, Goodbourn S, Jagus R.
Eur J Biochem, 232(1):28-36, August 15, 1995.
Cell Type-Specific Transactivation of the VCAM-1 Promoter Through an NF-kappa B Enhancer Motif.
Ahmad M, Marui N, Alexander RW, Medford RM.
J Biol Chem, 270(15):8976-8983, April 14, 1995.
Modified Low Density Lipoprotein and its Constituents Augment Cytokine-Activated Vascular Cell Adhesion Molecule-1 Gene Expression in Human Vascular Endothelial Cells.
Khan BV, Parthasarathy SS, Alexander RW, Medford RM.
J Clin Invest, 95(3):1262-1270, March 1995.
Antioxidants and Atherosclerosis: A Molecular Perspective.
Offermann MK, Medford RM.
Heart Dis Stroke, 3(1):52-57, January, 1994.
Vascular Cell Adhesion Molecule-1 (VCAM-1) Gene Transcription and Expression are Regulated Through an Antioxidant-Sensitive Mechanism in Human Vascular Endothelial Cells.
Marui N, Offermann MK, Swerlick R, Kunsch C, Rosen CA, Ahmad M, Alexander RW, Medford RM.
Journal of Clinical Investigation, 92(4):1866-1874, October, 1993.
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