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2016 Journal Article Receptor residence time trumps drug-likeness and oral bioavailability in determining efficacy of complement C5a antagonistsSeow, Vernon, Lim, Junxian, Cotterell, Adam J., Yau, Mei-Kwan, Xu, Weijun, Lohman, Rink-Jan, Kok, W. Mei, Stoermer, Martin J., Sweet, Matthew J., Reid, Robert C., Suen, Jacky Y. and Farilie, David P. (2016). Receptor residence time trumps drug-likeness and oral bioavailability in determining efficacy of complement C5a antagonists. Scientific Reports, 6 (1) 24575, 24575.1-24575.12. doi: 10.1038/srep24575 |
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2016 Journal Article Benzylamide antagonists of protease activated receptor 2 with anti-inflammatory activityYau, Mei-Kwan, Liu, Ligong, Lim, Junxian, Lohman, Rink-Jan, Cotterell, Adam J., Suen, Jacky Y., Vesey, David A., Reid, Robert C. and Fairlie, David P. (2016). Benzylamide antagonists of protease activated receptor 2 with anti-inflammatory activity. Bioorganic and Medicinal Chemistry Letters, 26 (3), 986-991. doi: 10.1016/j.bmcl.2015.12.048 |
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2016 Journal Article Differential anti-inflammatory activity of HDAC inhibitors in human macrophages and rat arthritisLohman, Rink-Jan, Iyer, Abishek, Fairlie, Thomas J., Cotterell, Adam, Gupta, Praveer, Reid, Robert C., Vesey, David A., Sweet, Matthew J. and Fairlie, David P. (2016). Differential anti-inflammatory activity of HDAC inhibitors in human macrophages and rat arthritis. Journal of Pharmacology and Experimental Therapeutics, 356 (2), 387-396. doi: 10.1124/jpet.115.229328 |
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2016 Conference Publication Pharmacological Inhibition of Protease-Activated Receptor 2 (Par2) Reduces Crescent Formation in Rat Anti-Gbm DiseaseTesch, G., Han, Y., Vesey, D., Gobe, G., Lohman, R., Suen, J., Fairlie, D. and Nikolic-Paterson, D. (2016). Pharmacological Inhibition of Protease-Activated Receptor 2 (Par2) Reduces Crescent Formation in Rat Anti-Gbm Disease. 15th Asian Pacific Congress of Nephrology (APCN) and 52nd ANZSN ASM, Perth, WA, Australia, 17–21 September 2016. Richmond, VIC, Australia: Wiley-Blackwell Publishing Asia. doi: 10.1111/nep.12887 |
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2016 Journal Article PAR2 modulators derived from GB88Yau, Mei-Kwan, Liu, Ligong, Suen, Jacky Y., Lim, Junxian, Lohman, Rink-Jan, Jiang, Yuhong, Cotterell, Adam J., Barry, Grant D., Mak, Jeffrey Y. W., Vesey, David A., Reid, Robert C. and Fairlie, David P. (2016). PAR2 modulators derived from GB88. ACS Medicinal Chemistry Letters, 7 (12), 1179-1184. doi: 10.1021/acsmedchemlett.6b00306 |
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2016 Conference Publication Protease activated-receptor-2 induced inflammation and fibrosis is mediated in part through activation of transforming growth factor-beta signallingOwens, E., Iyer, A., Morais, C., Lohman, R., Suen, J., Johnson, D., Nikolic-Paterson, D., Gobe, G., Fairlie, D. and Vesey, D. (2016). Protease activated-receptor-2 induced inflammation and fibrosis is mediated in part through activation of transforming growth factor-beta signalling. The 15th Asian Pacific Congress of Nephrology (APCN) and 52nd ANZSN ASM, Perth Western Australia, 17–21 September 2016. Richmond, VIC, Australia: Wiley-Blackwell Publishing Asia. doi: 10.1111/nep.12887 |
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2015 Journal Article Flexibility versus rigidity for orally bioavailable cyclic hexapeptidesNielsen, Daniel S., Lohman, Rink-Jan, Hoang, Huy Ngoc, Hill, Timothy A., Jones, Alun, Lucke, Andrew J. and Fairlie, David P. (2015). Flexibility versus rigidity for orally bioavailable cyclic hexapeptides. Chembiochem, 16 (16), 2289-2293. doi: 10.1002/cbic.201500441 |
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2015 Conference Publication Cyclic penta- and hexa leucine peptides without N-methylation are orally absorbedKok, Woan Mei, Hill, Timothy A., Lohman, Rink-Jan, Hoang, Huy N., Nielsen, Daniel S., Scully, Conor G., Schroeder, Christina I., Colless, Barbara, Bernhardt, Paul V., Edmonds, David, Griffith, David, Rotter, Charles, Ruggeri, Roger, Price, David, Liras, Spiros, Craik, David and Fairlie, David (2015). Cyclic penta- and hexa leucine peptides without N-methylation are orally absorbed. American Chemical Society Meeting, x, 2015. Washington, DC United States: American Chemical Society. |
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2015 Book Chapter Helix-constrained nociceptin peptides are potent agonists and antagonists of ORL-1 and nociceptionLohman, Rink-Jan, Harrison, Rosemary S., Ruiz-Gomez, Gloria, Hoang, Huy Ngoc, Shepherd, Nicholas E., Chow, Shiao, Hill, Timothy A., Madala, Praveen K. and Fairlie, David P. (2015). Helix-constrained nociceptin peptides are potent agonists and antagonists of ORL-1 and nociception. Nociceptin opioid. (pp. 1-55) edited by Gerald Litwack. Maryland Heights, MO, United States: Academic Press. doi: 10.1016/bs.vh.2014.10.001 |
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2015 Conference Publication Downsizing Proteins Without Losing Potency or FunctionFairlie, David P. , Yau, Mei-Kwan , Hamidon, Johan K. , Singh, Ranee , Lim, Junxian , Suen, Jacky Y. , Rowley, Jessica A. , Lohman, Rink-Jan , Stoermer, Martin J. , Iyer, Abishek and Reid, Robert C. (2015). Downsizing Proteins Without Losing Potency or Function. American Peptide Symposium 2015, Orlando , Florida, United States, 20-25 June 2015. American Peptide Society. doi: 10.17952/24APS.2015.016 |
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2014 Journal Article Rational design and synthesis of orally bioavailable peptides guided by NMR amide temperature coefficientsWang, Conan K., Northfield, Susan E., Colless, Barbara, Chaousis, Stephanie, Hamernig, Ingrid, Lohman, Rink-Jan, Nielsen, Daniel S., Schroeder, Christina I., Liras, Spiros, Price, David, A., Fairlie, David and Craik, David J. (2014). Rational design and synthesis of orally bioavailable peptides guided by NMR amide temperature coefficients. Proceedings of the National Academy of Sciences of the United States of America (PNAS), 111 (49), 17504-17509. doi: 10.1073/pnas.1417611111 |
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2014 Journal Article Improving on nature: making a cyclic heptapeptide orally bioavailableNielsen, Daniel S., Hoang, Huy N., Lohman, Rink-Jan, Hill, Timothy A., Lucke, Andrew J., Craik, David J., Edmonds, David J., Griffith, David A., Rotter, Charles J., Ruggeri, Roger B., Price, David A., Liras, Spiros and Fairlie, David P. (2014). Improving on nature: making a cyclic heptapeptide orally bioavailable. Angewandte Chemie - International Edition, 53 (45), 12059-12063. doi: 10.1002/anie.201405364 |
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2014 Journal Article Cyclic penta- and hexaleucine peptides without N-methylation are orally absorbedHill, Timothy A., Lohman, Rink-Jan, Hoang, Huy N., Nielsen, Daniel S., Scully, Conor C. G., Kok, W. Mei, Liu, Ligong, Lucke, Andrew J., Stoermer, Martin J., Schroeder, Christina I., Chaousis, Stephanie, Colless, Barbara, Bernhardt, Paul V., Edmonds, David J., Griffith, David A., Rotter, Charles J., Ruggeri, Roger B., Price, David A., Liras, Spiros, Craik, David J. and Fairlie, David P. (2014). Cyclic penta- and hexaleucine peptides without N-methylation are orally absorbed. ACS Medicinal Chemistry Letters, 5 (10), 1148-1151. doi: 10.1021/ml5002823 |
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2014 Journal Article Pathway-selective antagonism of proteinase activated receptor 2Suen, J. Y., Cotterell, A., Lohman, R. J., Lim, J., Han, A., Yau, M. K., Liu, L., Cooper, M. A., Vesey, D. A. and Fairlie, D. P. (2014). Pathway-selective antagonism of proteinase activated receptor 2. British Journal of Pharmacology, 171 (17), 4112-4124. doi: 10.1111/bph.12757 |
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Featured 2013 Journal Article Diet-induced obesity, adipose inflammation, and metabolic dysfunction correlating with PAR2 expression are attenuated by PAR2 antagonismLim, Junxian, Iyer, Abishek, Liu, Ligong, Suen, Jacky Y., Lohman, Rink-Jan, Seow, Vernon, Yau, Mei-Kwan, Brown, Lindsay and Fairlie, David P. (2013). Diet-induced obesity, adipose inflammation, and metabolic dysfunction correlating with PAR2 expression are attenuated by PAR2 antagonism. The FASEB Journal, 27 (12), 4757-4767. doi: 10.1096/fj.13-232702 |
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2013 Journal Article PAR2-induced inflammatory responses in human kidney tubular epithelial cellsVesey, David A., Suen, Jacky Y., Seow, Vernon, Lohman, Rink-Jan, Liu, Ligong, Gobe, Glenda C., Johnson, David W. and Fairlie, David P. (2013). PAR2-induced inflammatory responses in human kidney tubular epithelial cells. American Journal of Physiology - Renal Physiology, 304 (6), F737-F750. doi: 10.1152/ajprenal.00540.2012 |
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2013 Journal Article Total synthesis, structure, and oral absorption of a thiazole cyclic peptide, sanguinamide ANielsen, Daniel S., Hoang, Huy N., Lohman, Rink-Jan, Diness, Frederik and Fairlie, David P. (2013). Total synthesis, structure, and oral absorption of a thiazole cyclic peptide, sanguinamide A. Organic Letters, 14 (22), 5720-5723. doi: 10.1021/ol3027347 |
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2013 Conference Publication Toward more orally bioavailable inhibitors of phospholipase A(2) GIIA (pla2g2a) to treat chronic inflammationBarbero, Sheila, Reid, Robert C., Stoermer, Martin J., Lohman, Rink J. and Fairlie, David P. (2013). Toward more orally bioavailable inhibitors of phospholipase A(2) GIIA (pla2g2a) to treat chronic inflammation. 246th National Meeting of the American-Chemical-Society (ACS), Indianapolis, IN, United States, 8-12 September 2013. Washington, DC, United States: American Chemical Society. |
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2012 Journal Article An antagonist of human protease activated receptor-2 attenuates PAR2 signaling, macrophage activation, mast cell degranulation, and collagen-induced arthritis in ratsLohman, Rink-Jan, Cotterell, Adam J., Barry, Grant D., Liu, Ligong, Suen, Jacky Y., Vesey, David A. and Fairlie, David P. (2012). An antagonist of human protease activated receptor-2 attenuates PAR2 signaling, macrophage activation, mast cell degranulation, and collagen-induced arthritis in rats. The FASEB Journal, 26 (7), 2877-2887. doi: 10.1096/fj.11-201004 |
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2012 Journal Article Modulating human proteinase activated receptor 2 with a novel antagonist (GB88) and agonist (GB110)Suen, J. Y., Barry, G. D., Lohman, R. J., Halili, M. A., Cotterell, A. J., Le, G. T. and Fairlie, D. P. (2012). Modulating human proteinase activated receptor 2 with a novel antagonist (GB88) and agonist (GB110). British Journal of Pharmacology, 165 (5), 1413-1423. doi: 10.1111/j.1476-5381.2011.01610.x |
