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2017

Journal Article

Biased signaling by agonists of protease activated receptor 2

Jiang, Yuhong, Yau, Mei-Kwan, Kok, W. Mei, Lim, Junxian, Wu, Kai-Chen, Liu, Ligong, Hill, Timothy A., Suen, Jacky Y. and Fairlie, David P. (2017). Biased signaling by agonists of protease activated receptor 2. ACS Chemical Biology, 12 (5), 1217-1226. doi: 10.1021/acschembio.6b01088

Biased signaling by agonists of protease activated receptor 2

2017

Journal Article

Mapping transmembrane residues of proteinase activated recpetor 2 (PAR2) that influence ligand-modulated calcium signaling

Suen, J.Y., Adams, M. N., Lim, J., Madala, P.K., Xu, W, Cotterell, A., He, Y., Yua, Mei-Kwan, Hooper, J. D. and Fairlie, D.P. (2017). Mapping transmembrane residues of proteinase activated recpetor 2 (PAR2) that influence ligand-modulated calcium signaling. Pharmacological Research, 117, 328-342. doi: 10.1016/j.phrs.2016.12.020

Mapping transmembrane residues of proteinase activated recpetor 2 (PAR2) that influence ligand-modulated calcium signaling

2016

Journal Article

Receptor residence time trumps drug-likeness and oral bioavailability in determining efficacy of complement C5a antagonists

Seow, 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

Receptor residence time trumps drug-likeness and oral bioavailability in determining efficacy of complement C5a antagonists

2016

Journal Article

Benzylamide antagonists of protease activated receptor 2 with anti-inflammatory activity

Yau, 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

Benzylamide antagonists of protease activated receptor 2 with anti-inflammatory activity

2016

Conference Publication

Pharmacological Inhibition of Protease-Activated Receptor 2 (Par2) Reduces Crescent Formation in Rat Anti-Gbm Disease

Tesch, 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

Pharmacological Inhibition of Protease-Activated Receptor 2 (Par2) Reduces Crescent Formation in Rat Anti-Gbm Disease

2016

Journal Article

Potent small agonists of protease activated receptor 2

Yau, Mei-Kwan, Suen, Jacky Y., Xu, Weijun, Lim, Junxian, Liu, Ligong, Adams, Mark N., He, Yaowu, Hooper, John D., Reid, Robert C. and Fairlie, David P. (2016). Potent small agonists of protease activated receptor 2. ACS Medicinal Chemistry Letters, 7 (1), 105-110. doi: 10.1021/acsmedchemlett.5b00429

Potent small agonists of protease activated receptor 2

2016

Journal Article

PAR2 modulators derived from GB88

Yau, 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

PAR2 modulators derived from GB88

2016

Conference Publication

Protease activated-receptor-2 induced inflammation and fibrosis is mediated in part through activation of transforming growth factor-beta signalling

Owens, 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

Protease activated-receptor-2 induced inflammation and fibrosis is mediated in part through activation of transforming growth factor-beta signalling

2015

Journal Article

Potent complement C3a receptor agonists derived from oxazole amino acids: structure-activity relationships

Singh, Ranee, Reed, Anthony N., Chu, Peifei, Scully, Conor C. G., Yau, Mei-Kwan, Suen, Jacky Y., Durek, Thomas, Reid, Robert C. and Fairlie, David P. (2015). Potent complement C3a receptor agonists derived from oxazole amino acids: structure-activity relationships. Bioorganic and Medicinal Chemistry Letters, 25 (23), 5604-5608. doi: 10.1016/j.bmcl.2015.10.038

Potent complement C3a receptor agonists derived from oxazole amino acids: structure-activity relationships

2015

Journal Article

Repurposing Registered Drugs as Antagonists for Protease-Activated Receptor 2

Xu, Weijun, Lim, Junxian, Goh, Chai-Yeen, Suen, Jacky Y., Jiang, Yuhong, Yau, Mei-Kwan, Wu, Kai-Chen, Liu, Ligong and Fairlie, David P. (2015). Repurposing Registered Drugs as Antagonists for Protease-Activated Receptor 2. Journal of Chemical Information and Modeling, 55 (10), 2079-2084. doi: 10.1021/acs.jcim.5b00500

Repurposing Registered Drugs as Antagonists for Protease-Activated Receptor 2

2015

Conference Publication

Potent small agonists of protease activated receptor 2

Yau, Mei Kwan, Suen, Jacky, Xu, Weijun, Lim, Junxian, Liu, Ligong, Adams, Mark, He, Yaowu, Hooper, John, Reid, Robert and Fairlie, David (2015). Potent small agonists of protease activated receptor 2. WASHINGTON: AMER CHEMICAL SOC.

Potent small agonists of protease activated receptor 2

2015

Journal Article

Short hydrophobic peptides with cyclic constraints are potent glucagon-like peptide-1 receptor (GLP-1R) agonists

Hoang, Huy N., Song, Kun, Hill, Timothy A., Derksen, David R., Edmonds, David J., Kok, W. Mei, Limberakis, Chris, Liras, Spiros, Loria, Paula M., Mascitti, Vincent, Mathiowetz, Alan M., Mitchell, Justin M., Piotrowski, David W., Price, David A., Stanton, Robert V., Suen, Jacky Y., Withka, Jane M., Griffith, David A. and Fairlie, David P. (2015). Short hydrophobic peptides with cyclic constraints are potent glucagon-like peptide-1 receptor (GLP-1R) agonists. Journal of Medicinal Chemistry, 58 (9), 4080-4085. doi: 10.1021/acs.jmedchem.5b00166

Short hydrophobic peptides with cyclic constraints are potent glucagon-like peptide-1 receptor (GLP-1R) agonists

2015

Conference Publication

Downsizing Proteins Without Losing Potency or Function

Fairlie, 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

Downsizing Proteins Without Losing Potency or Function

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

2014

Journal Article

Biased signalling and proteinase-activated receptors (PARs): Targeting inflammatory disease

Hollenberg, M. D., Mihara, K., Polley, D., Suen, J. Y., Han, A., Fairlie, D. P. and Ramachandran, R. (2014). Biased signalling and proteinase-activated receptors (PARs): Targeting inflammatory disease. British Journal of Pharmacology, 171 (5), 1180-1194. doi: 10.1111/bph.12544

Biased signalling and proteinase-activated receptors (PARs): Targeting inflammatory disease

2013

Journal Article

Downsizing a human inflammatory protein to a small molecule with equal potency and functionality

Reid, Robert C., Yau, Mei-Kwan, Singh, Ranee, Hamidon, Johan K., Reed, Anthony N., Chu, Peifei, Suen, Jacky Y., Stoermer, Martin J., Blakeney, Jade S., Lim, Junxian, Faber, Jonathan M. and David P. Fairlie, (2013). Downsizing a human inflammatory protein to a small molecule with equal potency and functionality. Nature Communications, 4 (2802) 2802, 1-9. doi: 10.1038/ncomms3802

Downsizing a human inflammatory protein to a small molecule with equal potency and functionality

2013

Journal Article

Inflammatory Responses Induced by Lipopolysaccharide Are Amplified in Primary Human Monocytes but Suppressed in Macrophages by Complement Protein C5a

Seow, Vernon, Lim, Junxian, Iyer, Abishek, Suen, Jacky Y., Ariffin, Juliana K., Hohenhaus, Daniel M., Sweet, Matthew J. and Fairlie, David P. (2013). Inflammatory Responses Induced by Lipopolysaccharide Are Amplified in Primary Human Monocytes but Suppressed in Macrophages by Complement Protein C5a. Journal of Immunology, 191 (8), 4308-4316. doi: 10.4049/jimmunol.1301355

Inflammatory Responses Induced by Lipopolysaccharide Are Amplified in Primary Human Monocytes but Suppressed in Macrophages by Complement Protein C5a

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

C5aR and C3aR antagonists each inhibit diet-induced obesity, metabolic dysfunction, and adipocyte and macrophage signaling

Liu, Junxian, Iyer, Abishek, Suen, Jacky Y., Seow, Vernon, Reid, Robert C., Brown, Lindsay and Fairlie, David P. (2013). C5aR and C3aR antagonists each inhibit diet-induced obesity, metabolic dysfunction, and adipocyte and macrophage signaling. The FASEB Journal, 27 (2), 822-831. doi: 10.1096/fj.12-220582

C5aR and C3aR antagonists each inhibit diet-induced obesity, metabolic dysfunction, and adipocyte and macrophage signaling