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2015

Journal Article

Flexibility versus rigidity for orally bioavailable cyclic hexapeptides

Nielsen, 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

Flexibility versus rigidity for orally bioavailable cyclic hexapeptides

2014

Journal Article

Rational design and synthesis of orally bioavailable peptides guided by NMR amide temperature coefficients

Wang, 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

Rational design and synthesis of orally bioavailable peptides guided by NMR amide temperature coefficients

2014

Journal Article

Improving on nature: making a cyclic heptapeptide orally bioavailable

Nielsen, 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

Improving on nature: making a cyclic heptapeptide orally bioavailable

2014

Journal Article

Cyclic penta- and hexaleucine peptides without N-methylation are orally absorbed

Hill, 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

Cyclic penta- and hexaleucine peptides without N-methylation are orally absorbed

2014

Journal Article

Pathway-selective antagonism of proteinase activated receptor 2

Suen, 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

Pathway-selective antagonism of proteinase activated receptor 2

Featured

2013

Journal Article

Diet-induced obesity, adipose inflammation, and metabolic dysfunction correlating with PAR2 expression are attenuated by PAR2 antagonism

Lim, 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

Diet-induced obesity, adipose inflammation, and metabolic dysfunction correlating with PAR2 expression are attenuated by PAR2 antagonism

2013

Journal Article

PAR2-induced inflammatory responses in human kidney tubular epithelial cells

Vesey, 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

PAR2-induced inflammatory responses in human kidney tubular epithelial cells

2013

Journal Article

Total synthesis, structure, and oral absorption of a thiazole cyclic peptide, sanguinamide A

Nielsen, 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

Total synthesis, structure, and oral absorption of a thiazole cyclic peptide, sanguinamide A

2012

Journal Article

An antagonist of human protease activated receptor-2 attenuates PAR2 signaling, macrophage activation, mast cell degranulation, and collagen-induced arthritis in rats

Lohman, 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

An antagonist of human protease activated receptor-2 attenuates PAR2 signaling, macrophage activation, mast cell degranulation, and collagen-induced arthritis in rats

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

Modulating human proteinase activated receptor 2 with a novel antagonist (GB88) and agonist (GB110)

2012

Journal Article

Antagonism of protease-activated receptor 2 protects against experimental colitis.

Lohman, Rink-Jan, Cotterell, Adam J., Suen, Jacky, Liu, Ligong, Do, Anh T., Vesey, David A. and Fairlie, David P. (2012). Antagonism of protease-activated receptor 2 protects against experimental colitis.. Journal of Pharmacology and Experimental Therapeutics, 340 (2), 256-265. doi: 10.1124/jpet.111.187062

Antagonism of protease-activated receptor 2 protects against experimental colitis.

2010

Journal Article

Novel helix-constrained nociceptin derivatives are potent agonists and antagonists of ERK phosphorylation and thermal analgesia in mice

Harrison, Rosemary S., Ruiz-Gomez, Gloria, Hill, Timothy A., Chow, Shiao Y., Shepherd, Nicholas E., Lohman, Rink-Jan, Abbenante, Giovanni, Hoang, Huy N. and Fairlie, David P. (2010). Novel helix-constrained nociceptin derivatives are potent agonists and antagonists of ERK phosphorylation and thermal analgesia in mice. Journal of Medicinal Chemistry, 53 (23), 8400-8408. doi: 10.1021/jm101139f

Novel helix-constrained nociceptin derivatives are potent agonists and antagonists of ERK phosphorylation and thermal analgesia in mice