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Page 1
Preclinical evaluation of an inhibitor of cytosolic phospholipase A2α for the treatment of asthma.
Hewson CA, Patel S, Calzetta L, Campwala H, Havard S, Luscombe E, Clarke PA, Peachell PT, Matera MG, Cazzola M, Page C, Abraham WM, Williams CM, Clark JD, Liu WL, Clarke NP, Yeadon M. Hewson CA, et al. Among authors: clark jd. J Pharmacol Exp Ther. 2012 Mar;340(3):656-65. doi: 10.1124/jpet.111.186379. Epub 2011 Dec 7. J Pharmacol Exp Ther. 2012. PMID: 22160268
Benzenesulfonamide indole inhibitors of cytosolic phospholipase A2alpha: optimization of in vitro potency and rat pharmacokinetics for oral efficacy.
Lee KL, Behnke ML, Foley MA, Chen L, Wang W, Vargas R, Nunez J, Tam S, Mollova N, Xu X, Shen MW, Ramarao MK, Goodwin DG, Nickerson-Nutter CL, Abraham WM, Williams C, Clark JD, McKew JC. Lee KL, et al. Among authors: clark jd. Bioorg Med Chem. 2008 Feb 1;16(3):1345-58. doi: 10.1016/j.bmc.2007.10.060. Epub 2007 Oct 22. Bioorg Med Chem. 2008. PMID: 17998165
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.
McKew JC, Lee KL, Shen MW, Thakker P, Foley MA, Behnke ML, Hu B, Sum FW, Tam S, Hu Y, Chen L, Kirincich SJ, Michalak R, Thomason J, Ipek M, Wu K, Wooder L, Ramarao MK, Murphy EA, Goodwin DG, Albert L, Xu X, Donahue F, Ku MS, Keith J, Nickerson-Nutter CL, Abraham WM, Williams C, Hegen M, Clark JD. McKew JC, et al. Among authors: clark jd. J Med Chem. 2008 Jun 26;51(12):3388-413. doi: 10.1021/jm701467e. Epub 2008 May 23. J Med Chem. 2008. PMID: 18498150
Cytosolic phospholipase A2α blockade abrogates disease during the tissue-damage effector phase of experimental autoimmune encephalomyelitis by its action on APCs.
Thakker P, Marusic S, Stedman NL, Lee KL, McKew JC, Wood A, Goldman SJ, Leach MW, Collins M, Kuchroo VK, Wolf SF, Clark JD, Hassan-Zahraee M. Thakker P, et al. Among authors: clark jd. J Immunol. 2011 Aug 15;187(4):1986-97. doi: 10.4049/jimmunol.1002789. Epub 2011 Jul 11. J Immunol. 2011. PMID: 21746963
Blockade of cytosolic phospholipase A2 alpha prevents experimental autoimmune encephalomyelitis and diminishes development of Th1 and Th17 responses.
Marusic S, Thakker P, Pelker JW, Stedman NL, Lee KL, McKew JC, Han L, Xu X, Wolf SF, Borey AJ, Cui J, Shen MW, Donahue F, Hassan-Zahraee M, Leach MW, Shimizu T, Clark JD. Marusic S, et al. Among authors: clark jd. J Neuroimmunol. 2008 Nov 15;204(1-2):29-37. doi: 10.1016/j.jneuroim.2008.08.012. J Neuroimmunol. 2008. PMID: 18829119
In vitro allergen challenge of peripheral blood induces differential gene expression in mononuclear cells of asthmatic patients: inhibition of cytosolic phospholipase A2alpha overcomes the asthma-associated response.
Whalen KA, Legault H, Hang C, Hill A, Kasaian M, Donaldson D, Bensch GW, Bensch G, Baker J, Reddy PS, Wood N, Ramarao MK, Ellis DK, Csimma C, McKee C, Clark JD, Ryan J, Dorner AJ, O'Toole M. Whalen KA, et al. Among authors: clark jd. Clin Exp Allergy. 2008 Oct;38(10):1590-605. doi: 10.1111/j.1365-2222.2008.03059.x. Epub 2008 Jul 28. Clin Exp Allergy. 2008. PMID: 18665843 Free PMC article.
Discovery of Ecopladib, an indole inhibitor of cytosolic phospholipase A2alpha.
Lee KL, Foley MA, Chen L, Behnke ML, Lovering FE, Kirincich SJ, Wang W, Shim J, Tam S, Shen MW, Khor S, Xu X, Goodwin DG, Ramarao MK, Nickerson-Nutter C, Donahue F, Ku MS, Clark JD, McKew JC. Lee KL, et al. Among authors: clark jd. J Med Chem. 2007 Mar 22;50(6):1380-400. doi: 10.1021/jm061131z. Epub 2007 Feb 17. J Med Chem. 2007. PMID: 17305324
507 results