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2018

Journal Article

Bicyclic helical peptides as dual inhibitors selective for Bcl2A1 and Mcl-1 proteins

de Araujo, Aline D., Lim, Junxian, Wu, Kai-Chen, Xiang, Yibin, Good, Andrew C., Skerlj, Renato and Fairlie, David P. (2018). Bicyclic helical peptides as dual inhibitors selective for Bcl2A1 and Mcl-1 proteins. Journal of Medicinal Chemistry, 61 (7), 2962-2972. doi: 10.1021/acs.jmedchem.8b00010

Bicyclic helical peptides as dual inhibitors selective for Bcl2A1 and Mcl-1 proteins

2018

Journal Article

A potent antagonist of protease-activated receptor 2 that inhibits multiple signaling functions in human cancer cells

Jiang, Yuhong, Yau, Mei-Kwan, Lim, Junxian, Wu, Kai-Chen, Xu, Weijun, Suen, Jacky Y and Fairlie, David P (2018). A potent antagonist of protease-activated receptor 2 that inhibits multiple signaling functions in human cancer cells. The Journal of pharmacology and experimental therapeutics, 364 (2), 246-257. doi: 10.1124/jpet.117.245027

A potent antagonist of protease-activated receptor 2 that inhibits multiple signaling functions in human cancer cells

2017

Journal Article

Exploiting a novel conformational switch to control innate immunity mediated by complement protein C3a

Lohman, Rink-Jan, Hamidon, Johan K., Reid, Robert C., Rowley, Jessica A., Yau, Mei-Kwan, Halili, Maria A., Nielsen, Daniel S., Lim, Junxian, Wu, Kai-Chen, Loh, Zhixuan, Do, Anh, Suen, Jacky Y., Iyer, Abishek and Fairlie, David P. (2017). Exploiting a novel conformational switch to control innate immunity mediated by complement protein C3a. Nature Communications, 8 (1) 351, 351. doi: 10.1038/s41467-017-00414-w

Exploiting a novel conformational switch to control innate immunity mediated by complement protein C3a

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

2017

Journal Article

Electrophilic helical peptides that bond covalently, irreversibly, and selectively in a protein-protein interaction site

Dantas De Araujo, Aline, Lim, Junxian, Good, Andrew C., Skerlj, Renato T. and Fairlie, David P. (2017). Electrophilic helical peptides that bond covalently, irreversibly, and selectively in a protein-protein interaction site. ACS Medicinal Chemistry Letters, 8 (1), 22-26. doi: 10.1021/acsmedchemlett.6b00395

Electrophilic helical peptides that bond covalently, irreversibly, and selectively in a protein-protein interaction site

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

Protease activated receptor 2 (PAR2) modulators: a patent review (2010–2015)

Yau, Mei-Kwan, Lim, Junxian, Liu, Ligong and Fairlie, David P. (2016). Protease activated receptor 2 (PAR2) modulators: a patent review (2010–2015). Expert Opinion on Therapeutic Patents, 26 (4), 471-483. doi: 10.1517/13543776.2016.1154540

Protease activated receptor 2 (PAR2) modulators: a patent review (2010–2015)

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

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

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

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

Journal Article

Three homology models for PAR2 derived from different templates: Application to antagonist discovery

Perry, Samuel R., Xu, Weijun, Wirija, Anna, Lim, Junxian, Yau, Mei-Kwan, Stoermer, Martin J., Lucke, Andrew J. and Fairlie, David P. (2015). Three homology models for PAR2 derived from different templates: Application to antagonist discovery. Journal of Chemical Information And Modeling, 55 (6), 1181-1191. doi: 10.1021/acs.jcim.5b00087

Three homology models for PAR2 derived from different templates: Application to antagonist discovery

2014

Journal Article

Potent heterocyclic ligands for human complement C3a receptor

Reid, Robert C., Yau, Mei-Kwan, Singh, Ranee, Hamidon, Johan K., Lim, Junxian, Stoermer, Martin J. and Fairlie, David P. (2014). Potent heterocyclic ligands for human complement C3a receptor. Journal of Medicinal Chemistry, 57 (20), 8459-8470. doi: 10.1021/jm500956p

Potent heterocyclic ligands for human complement C3a receptor

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

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

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

2012

Journal Article

An inhibitor of phospholipase A2 group IIA modulates adipocyte signaling and protects against diet-induced metabolic syndrome in rats

Iyer, Abishek, Lim, Junxian, Poudyal, Hemant, Reid, Robert C., Suen, Jacky Y., Webster, Julie, Prins, Johannes B., Whitehead, Jonathan P., Fairlie, David P. and Brown, Lindsay (2012). An inhibitor of phospholipase A2 group IIA modulates adipocyte signaling and protects against diet-induced metabolic syndrome in rats. Diabetes, 61 (9), 2320-2329. doi: 10.2337/db11-1179

An inhibitor of phospholipase A2 group IIA modulates adipocyte signaling and protects against diet-induced metabolic syndrome in rats

2010

Journal Article

Antifibrotic activity of an inhibitor of histone deacetylases in DOCA-salt hypertensive rats

Iyer, Abishek, Fenning, Andrew, Lim, Junxian, Le, Giang T, Reid, Robert C, Halili, Maria A, Fairlie, David P and Brown, Lindsay (2010). Antifibrotic activity of an inhibitor of histone deacetylases in DOCA-salt hypertensive rats. British Journal of Pharmacology, 159 (7), 1408-1417. doi: 10.1111/j.1476-5381.2010.00637.x

Antifibrotic activity of an inhibitor of histone deacetylases in DOCA-salt hypertensive rats

2009

Journal Article

Structure-activity relationships for substrate-based inhibitors of human complement factor B

Ruiz-Gomez, G, Lim, J, Halili, M. A., Le, G. T., Madala, P. K., Abbenante, G and Fairlie, D. P. (2009). Structure-activity relationships for substrate-based inhibitors of human complement factor B. JOURNAL OF MEDICINAL CHEMISTRY, 52 (19), 6042-6052. doi: 10.1021/jm900781m

Structure-activity relationships for substrate-based inhibitors of human complement factor B