Jilly F Evans

Summary

Publications

  1. doi request reprint What's all the FLAP about?: 5-lipoxygenase-activating protein inhibitors for inflammatory diseases
    Jilly F Evans
    Amira Pharmaceuticals, 9535 Waples Street, San Diego, CA 92121, USA
    Trends Pharmacol Sci 29:72-8. 2008
  2. doi request reprint Pharmacology of AM803, a novel selective five-lipoxygenase-activating protein (FLAP) inhibitor in rodent models of acute inflammation
    Daniel S Lorrain
    Amira Pharmaceuticals, 9535 Waples Street, Ste 100, San Diego, California 92121, USA
    Eur J Pharmacol 640:211-8. 2010
  3. doi request reprint 5-Lipoxygenase-activating protein inhibitors. Part 3: 3-{3-tert-Butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-5-(5-methyl-pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM643)-A potent FLAP inhibitor suitable for topical administ
    Nicholas Stock
    Amira Pharmaceuticals, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 20:4598-601. 2010
  4. doi request reprint Pharmacology of AM211, a potent and selective prostaglandin D2 receptor type 2 antagonist that is active in animal models of allergic inflammation
    Gretchen Bain
    Amira Pharmaceuticals, San Diego, California 92121, USA
    J Pharmacol Exp Ther 338:290-301. 2011
  5. doi request reprint Pharmacological characterization of 3-[3-tert-butylsulfanyl-1-[4-(6-methoxy-pyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM103), a novel selective 5-lipoxygenase-activating protein inhibitor that reduces acute
    Daniel S Lorrain
    Amira Pharmaceuticals, San Diego, California 92121, USA
    J Pharmacol Exp Ther 331:1042-50. 2009
  6. doi request reprint Discovery and optimization of a biphenylacetic acid series of prostaglandin D2 receptor DP2 antagonists with efficacy in a murine model of allergic rhinitis
    Jill M Scott
    Amira Pharmaceuticals, 9535 Waples Street, Suite 100, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 21:6608-12. 2011
  7. doi request reprint 5-Lipoxygenase-activating protein (FLAP) inhibitors. Part 4: development of 3-[3-tert-butylsulfanyl-1-[4-(6-ethoxypyridin-3-yl)benzyl]-5-(5-methylpyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropionic acid (AM803), a potent, oral, once daily FLAP inhib
    Nicholas S Stock
    Department of Chemistry, Amira Pharmaceuticals, San Diego, California 92121, United States
    J Med Chem 54:8013-29. 2011
  8. doi request reprint 5-Lipoxygenase-activating protein inhibitors. Part 2: 3-{5-((S)-1-Acetyl-2,3-dihydro-1H-indol-2-ylmethoxy)-3-tert-butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-1H-indol-2-yl}-2,2-dimethyl-propionic acid (AM679)--a potent FLAP inhibitor
    Nicholas Stock
    Amira Pharmaceuticals, 9535 Waples St, Suite 100, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 20:213-7. 2010
  9. doi request reprint DP2 (CRTh2) antagonism reduces ocular inflammation induced by allergen challenge and respiratory syncytial virus
    Karin J Stebbins
    Amira Pharmaceuticals, San Diego, Calif, USA
    Int Arch Allergy Immunol 157:259-68. 2012
  10. doi request reprint Therapeutic efficacy of AM156, a novel prostanoid DP2 receptor antagonist, in murine models of allergic rhinitis and house dust mite-induced pulmonary inflammation
    Karin J Stebbins
    Amira Pharmaceuticals, 9535 Waples St, Ste 100 San Diego, CA 92121, USA
    Eur J Pharmacol 638:142-9. 2010

Collaborators

Detail Information

Publications23

  1. doi request reprint What's all the FLAP about?: 5-lipoxygenase-activating protein inhibitors for inflammatory diseases
    Jilly F Evans
    Amira Pharmaceuticals, 9535 Waples Street, San Diego, CA 92121, USA
    Trends Pharmacol Sci 29:72-8. 2008
    ..In addition, the recent determination of the crystal structure of inhibitor-bound FLAP offers exciting potential for novel FLAP inhibitor design...
  2. doi request reprint Pharmacology of AM803, a novel selective five-lipoxygenase-activating protein (FLAP) inhibitor in rodent models of acute inflammation
    Daniel S Lorrain
    Amira Pharmaceuticals, 9535 Waples Street, Ste 100, San Diego, California 92121, USA
    Eur J Pharmacol 640:211-8. 2010
    ..In summary, AM803 is a novel, potent and selective FLAP inhibitor that has excellent pharmacodynamic properties in vivo and is effective in animal models of acute inflammation and in a model of lethal shock...
  3. doi request reprint 5-Lipoxygenase-activating protein inhibitors. Part 3: 3-{3-tert-Butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-5-(5-methyl-pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM643)-A potent FLAP inhibitor suitable for topical administ
    Nicholas Stock
    Amira Pharmaceuticals, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 20:4598-601. 2010
    ..Dermal application of 6 using a prototypical vehicle in a murine ear arachidonic acid model showed significant reduction in the concentrations of leukotrienes in mouse skin with concomitant reduction in ear swelling...
  4. doi request reprint Pharmacology of AM211, a potent and selective prostaglandin D2 receptor type 2 antagonist that is active in animal models of allergic inflammation
    Gretchen Bain
    Amira Pharmaceuticals, San Diego, California 92121, USA
    J Pharmacol Exp Ther 338:290-301. 2011
    ..AM211 represents a potent and selective antagonist of DP2 that may be used clinically to evaluate the role of DP2 in T helper 2-driven allergic inflammatory diseases...
  5. doi request reprint Pharmacological characterization of 3-[3-tert-butylsulfanyl-1-[4-(6-methoxy-pyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM103), a novel selective 5-lipoxygenase-activating protein inhibitor that reduces acute
    Daniel S Lorrain
    Amira Pharmaceuticals, San Diego, California 92121, USA
    J Pharmacol Exp Ther 331:1042-50. 2009
    ..In summary, AM103 is a novel, potent and selective FLAP inhibitor that has excellent pharmacodynamic properties in vivo and is effective in animal models of acute and chronic inflammation and in a model of lethal shock...
  6. doi request reprint Discovery and optimization of a biphenylacetic acid series of prostaglandin D2 receptor DP2 antagonists with efficacy in a murine model of allergic rhinitis
    Jill M Scott
    Amira Pharmaceuticals, 9535 Waples Street, Suite 100, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 21:6608-12. 2011
    ....
  7. doi request reprint 5-Lipoxygenase-activating protein (FLAP) inhibitors. Part 4: development of 3-[3-tert-butylsulfanyl-1-[4-(6-ethoxypyridin-3-yl)benzyl]-5-(5-methylpyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropionic acid (AM803), a potent, oral, once daily FLAP inhib
    Nicholas S Stock
    Department of Chemistry, Amira Pharmaceuticals, San Diego, California 92121, United States
    J Med Chem 54:8013-29. 2011
    ..This compound has successfully completed phase 1 clinical studies in healthy volunteers and is currently undergoing phase 2 trials in asthmatic patients...
  8. doi request reprint 5-Lipoxygenase-activating protein inhibitors. Part 2: 3-{5-((S)-1-Acetyl-2,3-dihydro-1H-indol-2-ylmethoxy)-3-tert-butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-1H-indol-2-yl}-2,2-dimethyl-propionic acid (AM679)--a potent FLAP inhibitor
    Nicholas Stock
    Amira Pharmaceuticals, 9535 Waples St, Suite 100, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 20:213-7. 2010
    ..Subsequent SAR on the N-benzyl substituent of the indole led to the discovery of compound 39 (AM679) which showed potent inhibition of leukotrienes in human blood and in a rodent bronchoalvelolar lavage (BAL) challenge model...
  9. doi request reprint DP2 (CRTh2) antagonism reduces ocular inflammation induced by allergen challenge and respiratory syncytial virus
    Karin J Stebbins
    Amira Pharmaceuticals, San Diego, Calif, USA
    Int Arch Allergy Immunol 157:259-68. 2012
    ..PGD(2), therefore, may be involved in both early and late phase reactions in response to allergen challenge...
  10. doi request reprint Therapeutic efficacy of AM156, a novel prostanoid DP2 receptor antagonist, in murine models of allergic rhinitis and house dust mite-induced pulmonary inflammation
    Karin J Stebbins
    Amira Pharmaceuticals, 9535 Waples St, Ste 100 San Diego, CA 92121, USA
    Eur J Pharmacol 638:142-9. 2010
    ..These results suggest that selective prostanoid DP(2) receptor antagonists such as AM156 may provide beneficial effects for the clinical treatment of diseases such as allergic rhinitis and asthma...
  11. doi request reprint Sodium [2'-[(cyclopropanecarbonyl-ethyl-amino)-methyl]-4'-(6-ethoxy-pyridin-3-yl)-6-methoxy-biphenyl-3-yl]-acetate (AM432): a potent, selective prostaglandin D2 receptor antagonist
    Nicholas Stock
    Amira Pharmaceuticals, 9535 Waples St, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 21:1036-40. 2011
    ....
  12. pmc Pharmacodynamics, pharmacokinetics and safety of GSK2190915, a novel oral anti-inflammatory 5-lipoxygenase-activating protein inhibitor
    Gretchen Bain
    Bristol Myers Squibb, San Diego, CA 92121, USA
    Br J Clin Pharmacol 75:779-90. 2013
    ....
  13. doi request reprint 5-lipoxygenase-activating protein inhibitors: development of 3-[3-tert-butylsulfanyl-1-[4-(6-methoxy-pyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM103)
    John H Hutchinson
    Departments of Chemistry, Amira Pharmaceuticals, San Diego, California 92121, USA
    J Med Chem 52:5803-15. 2009
    ..Compound 11j was selected for clinical development and has successfully completed phase 1 trials in healthy volunteers...
  14. ncbi request reprint The 5-lipoxygenase pathway promotes pathogenesis of hyperlipidemia-dependent aortic aneurysm
    Lei Zhao
    Center for Experimental Therapeutics, University of Pennsylvania, Philadelphia, Pennsylvania 19104 6160, USA
    Nat Med 10:966-73. 2004
    ..These data link the 5-LO pathway to hyperlipidemia-dependent inflammation of the arterial wall and to pathogenesis of aortic aneurysms through a potential chemokine intermediary route...
  15. pmc Expression, purification and crystallization of human 5-lipoxygenase-activating protein with leukotriene-biosynthesis inhibitors
    Shihua Xu
    Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA
    Acta Crystallogr Sect F Struct Biol Cryst Commun 63:1054-7. 2007
    ..The crystals exhibit tetragonal symmetry (P42(1)2) and diffracted to a resolution limit of 4 A...
  16. ncbi request reprint Crystal structure of inhibitor-bound human 5-lipoxygenase-activating protein
    Andrew D Ferguson
    Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA
    Science 317:510-2. 2007
    ..This structural information provides a platform for the development of therapeutics for respiratory and cardiovascular diseases...
  17. pmc Cysteinyl leukotriene 2 receptor and protease-activated receptor 1 activate strongly correlated early genes in human endothelial cells
    Barbara Uzonyi
    Institute for Vascular Medicine aud Institute for Medical Statistics, Computer Sciences, and Documentation, Friedrich Schiller University, Bachstrasse 18, 07743 Jena, Germany
    Proc Natl Acad Sci U S A 103:6326-31. 2006
    ..These data show that cysLT2-R activation results in a proinflammatory EC phenotype. Because LTD4 and thrombin are likely to be formed concomitantly in vivo, cysLT2-R and PAR-1 may cooperate to augment vascular injury...
  18. ncbi request reprint Localization and upregulation of cysteinyl leukotriene-1 receptor in asthmatic bronchial mucosa
    Jie Zhu
    Lung Pathology, Imperial College London, Royal Brompton Hospital, Sydney Street, London SW3 6NP, United Kingdom
    Am J Respir Cell Mol Biol 33:531-40. 2005
    ....
  19. pmc The membrane organization of leukotriene synthesis
    Asim K Mandal
    Department of Medicine, Massachusetts General Hospital, 149 The Navy Yard, 13th Street, Charlestown, MA 02129, USA
    Proc Natl Acad Sci U S A 101:6587-92. 2004
    ..The results indicate that the formation of LTC(4) and LTB(4) may be determined by the compartmentalization of biosynthetic enzymes in discrete molecular complexes...
  20. ncbi request reprint Transgenic smooth muscle expression of the human CysLT1 receptor induces enhanced responsiveness of murine airways to leukotriene D4
    Guochang Yang
    Center for Experimental Therapeutics, Rm 814BRBII III, Univ of Pennsylvania, 421 Curie Blvd, Philadelphia, PA 19104 6160, USA
    Am J Physiol Lung Cell Mol Physiol 286:L992-1001. 2004
    ..These results indicate that a selective hCysLT(1)R-induced contractile mechanism synergizes with allergic AHR. We speculate that hCysLT(1)R signaling contributes to a hypercontractile state of the airway smooth muscle...
  21. ncbi request reprint A cysteinyl leukotriene 2 receptor variant is associated with atopy in the population of Tristan da Cunha
    Miles D Thompson
    Department of Pharmacology, University of Toronto, Toronto, Ontario, Canada
    Pharmacogenetics 13:641-9. 2003
    ..0015). This represents the first association of a coding mutation in the CysLT2 receptor gene, located on chromosome 13q14, with the atopic phenotype found in the Tristan da Cunha population...
  22. ncbi request reprint The cysteinyl leukotriene receptors
    Jilly F Evans
    Pharmacology Department, Merck Research Laboratories, Merck and Co, Inc, 770 Sumneytown Pike, West Point, PA 19486, USA
    Prostaglandins Leukot Essent Fatty Acids 69:117-22. 2003
    ..Two human and mouse CysLT receptors have been molecularly cloned and characterized. The properties of these receptors agrees well with previous pharmacological CysLT agonist and antagonist characterizations of the CysLT receptors...
  23. ncbi request reprint Inhibition of cyclooxygenase-2 by rofecoxib attenuates the growth and metastatic potential of colorectal carcinoma in mice
    Min Yao
    Section of Gastroenterology, Boston University School of Medicine and Boston Medical Center, Boston, Massachusetts 02118, USA
    Cancer Res 63:586-92. 2003
    ....