Bibliography
- Burke JE, Dennis EA. Phospholipase A2 structure/function, mechanism, and signaling. J Lipid Res 2009;50:S237-42
- Burke JE, Dennis EA. Phospholipase A2 biochemistry. Cardiovasc Drugs Ther 2009;23:45-59
- Kudo I, Murakami M. Phospholipase A2 enzymes. Prostaglandins Other Lipid Mediat 2002;68-69:3-58
- Funk CD. Prostaglandins and leukotrienes: advances in eicosanoid biology. Science 2001;294:1871-5
- Rivera R, Chun J. Biological effects of lysophospholipids. Rev Physiol Biochem Pharmacol 2008;160:25-46
- Schaloske RH, Dennis EA. The phospholipase A(2) superfamily and its group numbering system. Biochim Biophys Acta 2006;1761:1246-59
- Kokotos G, Nicolaou A. Bioactive lipids. The Oily Press: Bridgewater, England; 2004
- Kokotos G. Lipolytic enzymes as therapeutic targets. Eur J Lipid Sci Technol 2008;110:1081-3
- Reid RC. Inhibitors of secretory phospholipase A2 Group IIA. Curr Med Chem 2005;12:3011-26
- Magrioti V, Kokotos G. Synthetic inhibitors of group IVA and group VIA phospholipase A2. Antiinflammatory Antiallergy Agents Med Chem 2006;5:189-203
- Lehr M. Inhibitors of cytosolic phospholipase A2alpha as potential anti-inflammatory drugs. Antiinflammatory Antiallergy Agents Med Chem 2006;5:149-61
- Lehr M. Phospholipase A2 inhibitors in inflammation. Expert Opin Ther Pat 2001;11:1123-36
- Clark JD, Tam S. Potential therapeutic uses of phospholipase A2 inhibitors. Expert Opin Ther Pat 2004;14:937-50
- Seilhamer J, Pruzanski W, Vadas P, Cloning and recombinant expression of phospholipase A2 present in rheumatoid arthritis synovial fluid. J Biol Chem 1989;264:5335-8
- Masuda S, Murakami M, Komiyama K, Various secretory phospholipase A2 enzymes are expressed in rheumatoid arthritis and augment prostaglandin production in cultured synovial cells. FEBS J 2005;272;655-72
- Berg OG, Gelb MH, Tsai M-D, Jain MK. Interfacial enzymology: the secreted phospholipase A2-paradigm. Chem Rev 2001;101:2613-54
- Lambeau G, Gelb MH. Biochemistry and physiology of mammalian secreted phospholipases A2. Annu Rev Biochem 2008;77:495-520
- Boyanovsky BB, Webb NR. Biology of secretory phospholipase A2. Cardiovasc Drugs Ther 2009;23:61-72
- Murakami M, Kudo I. Secretory phospholipase A2. Biol Pharm Bull 2004;27:1158-64
- Balestrieri B, Arm JP. Group V sPLA2: classical and novel functions. Biochim Biophys Acta 2006;1761:1280-8
- Rosengren B, Jonsson-Rylander A-C, Peilot H, Distinctiveness of secretory phospholipase A2 group IIA and V suggesting unique roles in atherosclerosis. Biochim Biophys Acta 2006;1761:1301-8
- Kimura-Matsumoto M, Ishikawa Y, Komiyama K, Expression of secretory phospholipase A2s in human atherosclerosis development. Atherosclerosis 2008;196:81-91
- Hanasaki K, Yamada K, Yamamoto S, Potent modification of low density lipoprotein by group X secretory phospholipase A2 is linked to macrophage foam cell formation. J Biol Chem 2002;277:29116-24
- Wooton-Kee CR, Boyanovsky BB, Nasser MS, Group V sPLA2 hydrolysis of low-density lipoprotein results in spontaneous particle aggregation and promotes macrophage foam cell formation. Arterioscler Thromb Vasc Biol 2004;24:762-7
- Karabina S-A, Brocheriou I, Le Naour G, Atherogenic properties of LDL particles modified by human group X secreted phospholipase A2 on human endothelial cell function. FASEB J 2006;20:E1890-900
- Bostrom MA, Boyanovsky BB, Jordan CT, Group V secretory phospholipase A2 promotes atherosclerosis: Evidence from genetically altered mice. Arterioscler Thromb Vasc Biol 2007;27:600-6
- Masuda S, Murakami M, Ishikawa Y, Diverse cellular localizations of secretory phospholipase A2 enzymes in several human tissues. BBA Mol Cell Biol Lipids 2005;1736:200-10
- Henderson WR, Chi EY, Bollinger JG, Importance of group X-secreted phospholipase A2 in allergen-induced airway inflammation and remodelling in a mouse asthma model. J Exp Med 2007;204:865-77
- Valentin E, Lambeau G. Increasing molecular diversity of secreted phospholipases A2 and their receptors and binding proteins. Biochim Biophys Acta 2000;1488:59-70
- Arita H, Hanasaki K, Nakano T, Novel proliferative effect of phospholipase A2 in Swiss 3T3 cells via specific binding site. J Biol Chem 1991;266:19139-41
- Cupillard L, Mulherkar R, Gomez N, Both group IB and group IIA secreted phospholipases A2 are natural ligands of the mouse 180-kDa M-type receptor. J Biol Chem 1999;274:7043-51
- Rouault M, Le Calvez C, Boilard E, Recombinant production and properties of binding of the full set of mouse secreted phospholipases A2 to the mouse M-type receptor. Biochemistry 2007;46:1647-62
- Kramer RM, Checani GC, Deykin A, Solubilization and properties of Ca2+-dependent human platelet phospholipase A2. Biochim Biophys Acta 1986;878:394-403
- Clark JD, Lin L-L, Kriz RW, A novel arachidonic acid-selective cytosolic PLA2 contains a Ca2+-dependent translocation domain with homology to PKC and GAP. Cell 1991;65:1043-51
- Kramer RM, Roberts EF, Manetta J, Putnam JE. The Ca2+-sensitive cytosolic phospholipase A2 is a 100-kDa protein in human monoblast U937 cells. J Biol Chem 1991;266:5268-72
- Ghosh MD, Tucker DE, Burchett SA, Leslie CC. Properties of the group IV phospholipase A2 family. Prog Lipid Res 2006;45:487-510
- Dessen AJ, Tang J, Schmidt H, Crystal structure of human cytosolic phospholipase A2 reveals a novel topology and catalytic mechanism. Cell 1999;97:349-60
- Sharp JD, Pickard RT, Chiou XG, Serine 228 is essential for catalytic activities of 85-kDa cytosolic phospholipase A2. J Biol Chem 1994;269:23250-4
- Huang Z, Fayette P, Abdullah K, Functional identification of the active-site nucleophile of the human 85-kDa cytosolic phospholipase A2. Biochemistry 1996;35:3712-21
- Bonventre JV, Huang Z, Taheri MR, Reduced fertility and postischaemic brain injury in mice deficient in cytosolic phospholipase A2. Nature 1997;390:622-5
- Uozumi N, Kume K, Nagase T, Role of cytosolic phospholipase A2 in allergic response and parturition. Nature 1997;390:618-22
- Nagase T, Uozumi N, Ishii S, Acute lung injury by sepsis and acid aspiration: a key role for cytosolic phospholipase A2. Nat Immunol 2000;1:42-6
- Patel MI, Singh J, Niknami M, Cytosolic phospholipase A2-alpha: a potential therapeutic target for prostate cancer. Clin Cancer Res 2008;14:8070-9
- O Sanchez-Mejia R, Newman JW, Toh S, Phospholipase A2 reduction ameliorates cognitive deficits in a mouse model of Alzheimer's disease. Nat Neurosci 2008;11:1311-18
- Larsson PK, Claesson HE, Kennedy BP. Multiple splice variants of the human calcium-independent phospholipase A2 and their effect on enzyme activity. J Biol Chem 1998;273:207-14
- Ackermann EJ, Kempner ES, Dennis EA. Ca2+-independent cytosolic phospholipase A2 from macrophage-like P388D1 cells. Isolation and characterization. J Biol Chem 1994;269:9227-33
- Balsinde J, Balboa MA. Cellular regulation and proposed biological functions of group VIA calcium-independent phospholipase A(2) in activated cells. Cell Signal 2005;17:1052-62
- Balsinde J, Perez R, Balboa MA. Calcium-independent phospholipase A2 and apoptosis. Biochim Biophys Acta 2006;1761:1344-50
- Hooks SB, Cummings BS. Role of Ca2+-independent phospholipase A2 in cell growth and signaling. Biochem Pharmacol 2008;76:1059-67
- Wilkins WP, Barbour S.E. Group VI phospholipase A2: homeostatic phospholipases with significant potential as targets for novel therapeutics. Curr Drug Targets 2008;9:683-97
- Ramanadham S, Hsu FF, Zhang S, Apoptosis of insulin-secreting cells induced by endoplasmic reticulum stress is amplified by overexpression of group VIA calcium-independent phospholipase A2 (iPLA2beta) and suppressed by inhibition of iPLA2beta. Biochemistry 2004;43:918-30
- Bao S, Miller DJ, Ma Z, Male mice that do not express group VIA phospholipase A2 produce spermatozoa with impaired motility and have greatly reduced fertility. J Biol Chem 2004;279:38194-200
- Ramanadham S, Yarasheski KE, Silva MJ, Age-related changes in bone morphology are accelerated in group VIA phospholipase A2 (iPLA2beta)-null mice. Am J Pathol 2008;172:868-81
- Min J-H, Jain MK, Wilder C, Membrane-bound plasma platelet activating factor acetylhydrolase acts on substrate in the aqueous phase. Biochemistry 1999;38:12935-42
- Stafforini DM. Biology of platelet-activating factor acetylhydrolase (PAF-AH, lipoprotein associated phospholipase A2). Cardiovasc Drugs Ther 2009;23:73-83
- Tjoelker LW, Eberhardt C, Unger J, Plasma platelet-activating factor acetylhydrolase is a secreted phospholipase A2 with a catalytic triad. J Biol Chem 1995;270:25481-7
- Tjoelker LW, Wilder C, Eberhardt C, Anti-inflammatory properties of a platelet-activating factor acetylhydrolase. Nature 1995;374:549-53
- Lavi S, Herrmann J, Lavi R, Role of lipoprotein-associated phospholipase A2 in atherosclerosis. Curr Atheroscler Rep 2008;10:230-5
- Lerman A, McConnel JP. Lipoprotein-associated phospholipase A2: a risk marker or a risk factor? Am J Cardiol 2008;101:S11-22
- Eli Lilly & Co. Method for treating sepsis. WO0205796; 2002
- Abraham E, Naum C, Bandi V, Efficacy and safety of LY315920Na/S-5920, a selective inhibitor of 14-kDa group IIA secretory phospholipase A2, in patients with suspected sepsis and organ failure. Crit Care Med 2003;31:718-28
- Kearney P, Naum C. Phase IB study of a novel phospholipase A2 inhibitor in patients with severe sepsis. Mediators Inflamm 1999;8:S8
- Rosenson RS. Future role for selective phospholipase A2 inhibitor in the prevention of atherosclerotic cardiovascular disease. Cardiovasc Drugs Ther 2009;23:93-101
- Anthera Pharmaceuticals, Inc. Treatment of cardiovascular disease and dyslipidemia using secretory phospholipase A2 (sPLA2) inhibitors and sPLA2 inhibitor combination therapies. WO2008137803; 2008
- Trias J, Hislop C. Use of secretory phospholipase A2 (sPLA2) inhibitors to decrease sPLA2 levels. US2009062369; 2009
- Trias J, Fraser H, Hislop C. Prevention of atherosclerosis by sPLA2 inhibitor in a mouse model. Inflamm Res 2007;56:S384
- Shaposhnik Z, Wang X, Trias J, The synergistic inhibition of atherogenesis in apoE-/- mice between pravastatin and the sPLA2 inhibitor varespladib (A-002). Presented at ATVB 2008, April 16-18 2008
- Koenig W, Khuseyinova N. Lipoprotein-associated and secretory phospholipase A2 in cardiovascular disease: the epidemiological evidence. Cardiovasc Drugs Ther 2009;23:85-92
- Bradley JD, Dmintrienko A, Kivitz AJ, Randomized, double-blinded, placebo-controlled clinical trial of LY333013, a selective inhibitor of group II secretory phospholipase A2, in the treatment of rheumatoid arthritis. J Rheumatol 2005;32:417-23
- Ilypsa, Inc. Treatment of diet-related conditions using phospholipase-A2 inhibitors comprising indoles and related compounds. WO2005112646; 2005
- Ilypsa, Inc. Indole compounds having c4-amide substituents and use thereof as phospholipase-A2 inhibitors. WO2007056275; 2007
- Ilypsa, Inc. Azaindole compounds and use thereof as phospholipase-A2 inhibitors. WO2007056184; 2007
- Ilypsa, Inc. Phospholipase inhibitors localized in the gastrointestinal lumen. US2007292385; 2007
- Ilypsa, Inc. Treatment of hypercholesterolemia, hypertriglyceridemia and cardiovascular-related conditions using phospholipase-A2 inhibitors. US2008051447; 2008
- Ilypsa, Inc. Multivalent indole compounds and use thereof as phospholipase-A2 inhibitors. WO2007056281; 2007
- Ilypsa, Inc. Indole compounds having c4-acidic substituents and use thereof as phospholipase-A2 inhibitors. WO2007056280; 2007
- Ilypsa, Inc. Phospholipase inhibitors, including multi-valent phospholipase inhibitors, and use thereof, including as lumen-localized phospholipase inhibitors. WO2007056279; 2007
- Cunningham TJ, Yao L, Greenstein JI. CHEC-7 a novel sPLA2 inhibitor and methods of use for treating neurological and inflammatory disorders. US20080249027; 2008
- Philadelphia Health & Education Corporation, D/B/A Drexel University. Methods for monitoring neuroinflammatory destruction of neurons and for treating diseases having an inflammatory component related to phospholipase A2. WO2007008690; 2007
- Gopalakrishnakone P, Thwin M-M, Ong W-Y, Phospholipase A2-inhibitory peptide with anti-arthritic and neuroprotective activities. US2005069530; 2005
- Keller B. Compounds and methods for inhibition of phospholipase A2 and cyclooxygenase-2. US2004110835; 2004
- Immupharma France SA. Compositions and methods for the inhibition of phospholipase A2. WO2007074169; 2007
- Guichard G, Lena G, Muller P, Compositions and methods for the inhibition of phospholipase A2. US2008031951; 2008
- Henderson WR Jr, Chi E, Bollinger JG, Importance of group X-secreted phospholipase A2 in allergen-induced airway inflammation and remodelling in a mouse asthma model. J Exp Med 2007;204:865-77
- Munoz NM, Meliton AY, Arm JP, Deletion of secretory group V phospholipase A2 attentuates cell migration and airway hyperresponsiveness in immunosensitized mice. J Immunol 2007;179:4800-7
- Singer AG, Ghomashchi F, Le Calvez C, Interfacial kinetic and binding properties of complete set of human and mouse groups I, II, V, X, and XII secreted phospholipases A2. J Biol Chem 2002;277:48535-49
- Oslund RC, Cermak N, Gelb MH. Highly specific and broadly potent inhibitors of mammalian secreted phospholipase A2. J Med Chem 2008;51:4708-14
- Wyeth Corp. Inhibitors of cytosolic phospholipase A2. WO03048122; 2003
- Wyeth Corp. Methods for treating asthmatic conditions. US2003149029; 2003
- Wyeth Corp. Inhibitors of cytosolic phospholipase A2. WO2006128142; 2006
- Wyeth Corp. Methods for the use of inhibitors of cytosolic phospholipase A2. US2006014759; 2006
- Wyeth Corp. Liquid formulations of phospholipase enzyme inhibitors. WO2008055136; 2008
- Wyeth Corp. Liquid formulations of phospholipase enzyme inhibitors. WO2008055141; 2008
- Wyeth Corp. Formulations of phospholipase enzyme inhibitors. WO2008055146; 2008
- Wyeth Corp. Semi-solid formulations of phospholipase enzyme inhibitors. WO2008055148; 2008
- Wyeth Corp. Methods for the use of inhibitors of cytosolic phospholipase A2 in the treatment of thrombosis. WO2007140317; 2007
- McKew JC, Foley MA, Thakker P, Inhibition of cytosolic phospholipase A2alpha: Hit to lead optimization. J Med Chem 2006;49:135-58
- Gopalsamy A, Yang H, Ellingboe JW, 1,2,4-Oxadiazolidin-3,5-diones and 1,3,5-triazin-2,4,6-triones as cytosolic phospholipase A2alpha inhibitors. Bioorg Med Chem Lett 2006;16:2978-81
- Lee KL, Foley MA, Chen L, Discovery of ecopladib, an indole inhibitor of cytosolic phospholipase A2alpha. J Med Chem 2007;50:1380-400
- Lee KL, Behnke ML, Foley MA, Benzenesulfonamide indole inhibitors of cytosolic phospholipase A2alpha: optimization of in vitro potency and rat pharmacokinetics for oral efficacy. Bioorg Med Chem 2008;16:1345-58
- McKew JC, Lee KL, Shen MWH, Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4- dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl} benzoic acid, efipladib. J Med Chem 2008;51:3388-413
- Marusic S, Thakker P, Pelker JW, Blockade of cytosolic phospholipase A2alpha prevents experimental autoimmune encephalomyelitis and diminishes development of Th1 and Th17 responses. J Neuroimmunol 2008;204:29-37
- Chen L, Wang W, Lee KL, Reactions of functionalized sulfonamides: Application to lowering the lipophilicity of cytosolic phospholipase A2alpha inhibitors. J Med Chem 2009;52:1156-171
- Kirincich SJ, Xiang J, Green N, Benzhydrylquinazolinediones: novel cytosolic phospholipase A2alpha inhibitors with improved physicochemical properties. Bioorg Med Chem 2009;17:4383-405
- Merckle GMBH. Novel heteroaryl-substituted acetone derivatives as inhibitors of phospholipase A2. WO2004069797; 2004
- Westfaelische Wilhelms Universitat Muenster. Novel heteroaryl-substituted acetone derivative, suitable for inhibiting phospholipase A2. WO2009040314; 2009
- Ludwig J, Bovens S, Brauch C, Design and synthesis of 1-indol-1-yl-propan-2-ones as inhibitors of human cytosolic phospholipase A2alpha. J Med Chem 2006;49:2611-20
- Hess M, Schulze Elfringhoff A, Lehr M. 1-(5-Carboxy- and 5-carbamoylindol-1-yl)propan-2-ones as inhibitors of human cytosolic phospholipase A2alpha: bioisosteric replacement of the carboxylic acid and carboxamide moiety. Bioorg Med Chem 2007;15:2883-91
- Fritsche A, Elfringhoff AS, Fabian J, Lehr M. 1-(2-Carboxyindol-5-yloxy)propan-2-ones as inhibitors of human cytosolic phospholipase A2alpha: synthesis, biological activity, metabolic stability, and solubility. Bioorg Med Chem 2008;16:3489-500
- Bovens S, Kaptur M, Elfringhoff AS, Lehr M. 1-(5-Carboxyindol-1-yl)propan-2-ones as inhibitors of human cytosolic phospholipase A2alpha: synthesis and properties of bioisosteric benzimidazole, benzotriazole and indazole analogues. Bioorg Med Chem Lett 2009;19:2107-11
- University of California. Compositions and methods for inhibition of phospholipase A2 mediated inflammation. WO03076389; 2003
- University of California. Systemic and intrathecal effects of a novel series of phospholipase A2 inhibitors on hyperalgesia and spinal PGE2 release. WO2007022443; 2007
- University of California. Phospholipase A2 inhibitors and their use in treating neurological injury and disease. WO2009009449; 2009
- Kokotos G, Six DA, Loukas V, Inhibition of group IVA cytosolic phospholipase A2 by novel 2-oxoamides in vitro, in cells, and in vivo. J Med Chem 2004;47:3615-28
- Yaksh TL, Kokotos G, Svensson CI, Systemic and intrathecal effects of a novel series of phospholipase A 2 inhibitors on hyperalgesia and spinal prostaglandin E2 release. J Pharm Exp Ther 2006;316:466-75
- Stephens D, Barbayianni E, Constantinou-Kokotou V, Differential inhibition of group IVA and group VIA phospholipases A 2 by 2-oxoamides. J Med Chem 2006;49:2821-8
- Six DA, Barbayianni E, Loukas V, Structure-activity relationship of 2-oxoamide inhibition of group IVA cytosolic phospholipase A2 and group V secreted phospholipase A2. J Med Chem 2007;50:4222-35
- Antonopoulou G, Barbayianni E, Magrioti V, Structure-activity relationships of natural and non-natural amino acid-based amide and 2-oxoamide inhibitors of human phospholipase A2 enzymes. Bioorg Med Chem 2008;16:10257-69
- Barbayianni E, Stephens D, Grkovich A, 2-Oxoamide inhibitors of phospholipase A2 activity and cellular arachidonate release based on dipeptides and pseudodipeptides. Bioorg Med Chem 2009;17:4833-43
- Burke JE, Babakhani A, Gorfe AA, Location of inhibitors bound to group IVA phospholipase A2 determined by molecular dynamics and deuterium exchange mass spectrometry. J Am Chem Soc 2009;131:8083-91
- Pasteur Institut, Institute National de la Sante et de la Rechearch Medicale. Use of at least one cytosolic phospholipase A2 inhibitor as a medicine for symptomatic treatment of mucoviscidosis. WO2007118996; 2007
- McGill University. Use of inhibitors of phospholipase A2 for the treatment, prevention or diagnosis of neural inflammatory or demyelinating disease. WO03101487; 2003
- Jannsen Pharmaceutica NV. Substituted isothiazolones. WO2007001932; 2007
- Bristol-Myers Squibb Co, Banville J, Remillard R, Alpha-amino, -thio, -oxo substituted ketones as phospholipase inhibitors. US6924391; 2005
- Seno K, Okuno T, Nishi K, Pyrrolidine inhibitors of human cytosolic phospholipase A2. J Med Chem 2000;43:1041-4
- Eno K, Okuno T, Nishi K, Pyrrolidine inhibitors of human cytosolic phospholipase A2. Part 2: synthesis of potent and crystallized 4-triphenylmethylthio derivative ‘pyrrophenone’. Bioorg Med Chem Lett 2001;11:587-90
- Ono T, Yamada K, Chikazawa Y, Characterization of a novel inhibitor of cytosolic phospholipase A2alpha, pyrrophenone. Biochem J 2002;363:727-35
- Tai N, Kuwabara K, Kobayashi M, Cytosolic phospholipase A2 alpha inhibitor, pyrroxyphene, displays anti-arthritic and anti-bone destructive action in a murine arthritis model. Inflamm Res; published online 5 August 2009, doi 10.1007/s00011-009-0069-8
- Yamamoto M, Haruna T, Imura K, Inhibitory effect of a potent and selective cytosolic phospholipase A2alpha inhibitor RSC-3388 on skin inflammation in mice. Pharmacology 2008;81:301-11
- McGill University, University of Athens, University of California. Perfluoroketone compounds and uses thereof. WO2008122119; 2008
- Baskakis C, Magrioti V, Cotton N, Synthesis of polyfluoro ketones for selective inhibition of human phospholipase A2 enzymes. J Med Chem 2008;51:8027-37
- Kokotos CG, Baskakis C, Kokotos G. Synthesis of medicinally interesting polyfluoro ketones via perfluoroalkyl lithium reagents. J Org Chem 2008;73:8623-6
- López-Vales R, Navarro X, Shimizu T, Intracellular phospholipase A2 group IVA and group VIA play important roles in wallerian degeneration and axon regeneration after peripheral nerve injury. Brain 2008;131:2620-31
- Kalyvas A, Baskakis C, Magrioti V, Differing roles for members of the phospholipase A2 superfamily in experimental autoimmune encephalomyelitis. Brain 2009;132:1221-35
- Smithkline Beecham PLC. Pyrimidine-4-one derivatives as LDL-PLA2 inhibitors. WO0160805; 2001
- Mohler ER III, Ballantyne CM, Davidson MH, The effect of darapladib on plasma lipoprotein-associated phospholipase A2 activity and cardiovascular biomarkers in patients with stable coronary heart disease or coronary heart diseaserisk equivalent: the results of a multicenter, randomized, double-blind, placebo-controlled study. J Am Coll Cardiol 2008;51:1632-41
- Wilensky RL, Shi Y, Mohler III ER, Inhibition of lipoprotein-associated phospholipase A2, reduces complex coronary atherosclerotic plaque development. Nat Med 2008;14:1059-66
- Serruys PW, Garcia-Garcia HM, Buszman P, Effects of the direct lipoprotein-associated phospholipase A2 inhibitor darapladib on human coronary atherosclerotic plaque. Circulation 2008;118:1172-82
- Smithkline Beecham PLC. Pharmaceutical formulation comprising pyriminine-4-one derivative coated with an enteric polymer. US2006287346; 2006
- Macphee CH, Tew DG. Lipoprotein associated phospholipase A2, inhibitors thereof and use of the same in diagnosis and therapy. US2005106611; 2005
- Smithkline Beecham PLC. Lipoprotein associated phospholipase A2, inhibitors thereof and use of the same in diagnosis and therapy. US2006040371; 2006
- Macphee CH, Tew DG. Lipoprotein associated phospholipase A2, inhibitors thereof and use of the same in diagnosis and therapy. US2007077251; 2007
- Macphee CH, Tew DG. Lipoprotein associated phospholipase A2, inhibitors thereof and use of the same in diagnosis and therapy. US2009136969; 2009
- Reddy KJ, Singh M, Bangit JR, Batsell RR. The role of lipoprotein-associated phospholipase A2 on cardiovascular disease risk assessment and plaque rupture: a clinical review. J Clin Lipidol 2009;3:85-93
- Garcia-Garcia HM, Serruys PW. Phospholipase A2 inhibitors. Curr Opin Lipidol 2009;20:327-32
- Street IP, Lin H-K, Laliberte F, Slow- and tight-binding inhibitors of the 85-kDa human phospholipase A2. Biochemistry 1993;32:5935-40
- Ghomashchi F, Loo R, Balsinde J, Trifluoromethyl ketones and methyl fluorophosphonates as inhibitors of group IV and VI phospholipases A2: structure-function studies with vesicle, micelle, and membrane assays. Biochim Biophys Acta 1999;1420:45-56
- Leis HJ, Windischhofer W. Inhibition of cyclooxygenases 1 and 2 by the phospholipase-blocker, arachidonyl trifluoromethyl ketone. Br J Pharmacol 2008;155:731-7
- Balsinde J, Dennis EA. Distinct roles in signal transduction for each of the phospholipase A2 enzymes present in P388D1 macrophages. J Biol Chem 1996;271:6758-65
- Balsinde J, Dennis EA. Function and inhibition of intracellular calcium-independent phospholipase A2. J Biol Chem 1997;272:16069-72
- Song H, Ramanadham S, Bao S, A bromoenol lactone suicide substrate inactivates group VIA phospholipase A2 by generating a diffiusible bromomethyl keto acid that alkylates cysteine thiols. Biochemistry 2006;45:1061-73
- Curfs DMJ, Ghesquiere SA, Vergouwe MN, Macrophage secretory phospholipase A2 group X enhances anti-inflammatory responses, promotes lipid accumulation, and contributes to aberrant lung pathology. J Biol Chem 2008;283:21640-8
- Nevalainen TJ, Graham GG, Scott KF. Antibacterial actions of secreted phospholipases A2. Biochim Biophys Acta 2008;1781:1-9
- Cummings BS. Phospholipase A2 as targets for anti-cancer drugs. Biochem Pharmacol 2007;74:949-59