Publications 2009 – 2017

2017

The Ribosomal Protein S19 Suppresses Antitumor Immune Responses via the Complement C5a Receptor 1. Markiewski MM, Vadrevu SK, Sharma SK, Chintala NK, Ghouse S, Cho JH, Fairlie DP, Paterson Y, Astrinidis A, Karbowniczek M.

J Immunol 2017, 198, 2989-2999.

Stabilising short-lived Schiff base derivatives of 5-aminouracils that activate mucosal-associated invariant T cells. Mak JYW, Xu W, Reid RC, Corbett AJ, Meehan B, Wang H, Chen Z, Rossjohn J, McCluskey J, Liu L, Fairlie DP.

Nature Communications 2017, 8, 14599. (doi: 10.1038/ncomms14599)

Drugs and drug-like molecules can modulate the function of mucosal-associated invariant T cells.  Keller AN#, Eckle SB#, Xu W#, Liu L, Hughes VA, Mak JY, Meehan BS, Pediongco T, Birkinshaw RW, Chen Z, Wang H, D’Souza C, Kjer-Nielsen L, Gherardin NA, Godfrey DI, Kostenko L, Corbett AJ, Purcell AW, Fairlie DP*, McCluskey J*, Rossjohn J*.

Nature Immunology 2017, Feb 6. doi: 10.1038/ni.3679.

Biased signaling by agonists of protease activated receptor 2. Jiang Y, Yau MK, Kok WM, Lim J, Wu KC, Liu L, Hill TA, Suen JY, Fairlie DP.

ACS Chem Biol 2017, Feb 7. doi: 10.1021/acschembio.6b01088.

Mapping transmembrane residues of proteinase activated receptor 2 (PAR2) that influence ligand-modulated calcium signaling. Suen JY, Adams MN, Lim J, Madala PK, Xu W, Cotterell AJ, He Y, Yau MK, Hooper JD, Fairlie DP.

Pharmacol Research 2017, 117, 328-342.

Total Synthesis of Mycobacterium tuberculosis Dideoxymycobactin-838 and Stereoisomers: Diverse CD1a-Restricted T Cells Display a Common Hierarchy of Lipopeptide Recognition. Cheng JM, Liu L, Pellicci DG, Reddiex SJ, Cotton RN, Cheng TY, Young DC, Van Rhijn I, Moody DB, Rossjohn J, Fairlie DP, Godfrey DI, Williams SJ.

Chemistry 2017, 23, 1694-1701.

Histone deacetylases (HDAC) in physiological and pathological bone remodelling. Cantley MD, Zannettino AC, Bartold PM, Fairlie DP, Haynes DR.

Bone 2017, 95, 162-174.

Mucosal-associated invariant T-cell activation and accumulation after in vivo infection depends on microbial riboflavin synthesis and co-stimulatory signals. Chen Z, Wang H, D’Souza C, Sun S, Kostenko L, Eckle SB, Meehan BS, Jackson DC, Strugnell RA, Cao H, Wang N, Fairlie DP, Liu L, Godfrey DI, Rossjohn J, McCluskey J, Corbett AJ.

Mucosal Immunol 2017, 10, 58-68.

Electrophilic helical peptides that bond covalently, irreversibly and selectively in a protein-protein interaction site. Dantas de Araujo A, Lim J, Good AC, Skerlj RT, Fairlie DP.

ACS Med Chem Lett 2017, 8, 22−26.  [Featured Article]

An HDAC6 inhibitor confers protection and selectively inhibits B-cell infiltration in DSS-induced colitis in mice. Do A, Reid RC, Lohman RJ, Sweet MJ, Fairlie DP*, Iyer A*.

J Pharmacol Exp Ther 2017, 360, 140-151.

Helix-constraints and amino acid substitution in GLP-1 increase cAMP and insulin secretion but not beta arrestin 2 signalling. Plisson F, Hill TA, Mitchell JM, Hoang HN, de Araujo AD, Xu W, Cotterell A, Edmonds DJ, Stanton RV, Derksen DR, Loria PM, Griffith DA, Price DA, Liras S, Fairlie DP.

Eur J Med Chem 2017, 127, 703-714.

2016

A three-stage intrathymic development pathway for the mucosal-associated invariant T cell lineage. Koay H-F, Gherardin NA, Enders A, Loh L, Mackay LK, Almeida CF, Russ BE, Nold-Petry CA, Nold MF, Bedoui S, Chen Z, Corbett AJ, Eckle SBG, Meehan B, d’Udekem Y, Konstantinov IE, Lappas M, Liu L, Goodnow CG, Fairlie DP, Rossjohn J, Chong MM, Kedzierska K, Berzins SP, Belz GT, McCluskey J, Uldrich AP, Godfrey DI, and Pellicci DG.

Nature Immunology201617, 1300-1311.

PAR2 modulators derived from GB88. Yau MK, Liu L, Suen JY, Lim J, Lohman RJ, Cotterell AJ, Barry GD, Mak JYC, Vesey DA, Reid RC, Fairlie DP.

ACS Med Chem Lett 20167, 1179-1184.

Product release is rate-limiting for catalytic processing by Dengue virus protease.Shannon, AE, Pedroso MM, Chappell KJ, Watterson D, Liebscher S, Kok WM, Fairlie DP, Schenk G, Young PR.

Science Reports20166, 24575.

Downsizing the BAD BH3 peptide to small constrained α-helices with improved ligand efficiency. Shepherd NE, Harrison RS, Ruiz-Gomez G, Abbenante G, Mason JM, Fairlie DP.

Org Biomol Chem201614, 10939-10945.

Human mucosal-associated invariant T cells contribute to antiviral influenza immunity via IL-18-dependent activation. Loh L, Wang Z, Sant S, Koutsakos M, Jegaskanda S, Corbett AJ, Liu L, Fairlie DP, Crowe J, Rossjohn J, Xu J, Doherty PC, McCluskey J, Kedzierska K.

PNAS2016113, 10133-10138.

Antagonism of the proinflammatory and pronociceptive actions of canonical and biased agonists of protease-activated receptor-2. Lieu T, Savage E, Zhao P, Edgington-Mitchell L, Barlow N, Bron R, Poole DP, McLean P, Lohman RJ, Fairlie DP, Bunnett NW.

Br J Pharmacol2016173, 2752-2765.

Truncated Glucagon-like Peptide-1 and Exendin-4 α-Conotoxin pl14a Peptide Chimeras Maintain Potency and α-Helicity and Reveal Interactions Vital for cAMP Signaling in Vitro. Swedberg JE, Schroeder CI, Mitchell JM, Fairlie DP, Edmonds DJ, Griffith DA, Ruggeri RB, Derksen DR, Loria PM, Price DA, Liras S, Craik DJ.

J. Biol. Chem. 2016291, 15778-15787.

Potent small Agonists of Protease Activated Receptor 2. Yau MK, Suen JY, Xu W, Lim J, Liu L, Adams MN, He Y, Hooper JD, Reid RC, Fairlie DP.

ACS Med Chem Lett.20167, 105-110.

Membrane-anchored serine protease matriptase is a trigger of pulmonary fibrogenesis. Bardoue O, Menou A, Francois C, Duitman JW, von der Thusen JH, Borie R, Sales KU, Mutze K, Castier Y, Sage E, Liu L, Bugge TH, Fairlie DP, Konigshoff M, Crestani B, Borensztajn KS.

Am J Respir Crit Care Med.2016193, 847-860.

Helix nucleation by the smallest known a-Helix in water. Hoang HN, Driver RW, Beyer RL, Hill TA, D de Araujo A, Plisson F, Harrison RS, Goedecke L Shepherd NE, Fairlie DP.

Angew Chem Int Ed Engl.201655, 8275-8279.

Histone deacetylase inhibitors promote mitochondrial reactive oxygen species production and bacterial clearance by human macrophages. Ariffin JK, Gupta KD, Kapetanovic R, Iyer A, Reid RC, Fairlie DP. and Sweet MJ.

Antimicrobial Agents and Chemotherapy 201660, 1521-1529.

Benzylamide antagonists of protease activated receptor 2 with anti-inflammatory activity. Yau MK, Liu L, Lim J, Lohman RJ, Cotterell AJ, Suen JY, Vesey DA, Reid RC, Fairlie DP.

Bioorg Chem Med Lett.201626, 986-991.

Stapling peptides using cysteine crosslinking. Fairlie DP, de Araujo AD.

Biopolymers2016,  accepted for publication.

Development of cell-penetrating peptide-based drug leads to inhibit MDMX:p53 and MDM2:p53 interactions. Philippe G, Huang Y-H, Cheneval O, Lawrence N, Zhang Z, Fairlie DP, Craik DJ, De Araujo AD, Henriques ST.

Biopolymers2016,  accepted for publication.

Histone deacetylases in monocyte/macrophage development, activation and metabolism: refining HDAC targets for inflammatory and infectious diseases. Gupta KD, Shakespear MR, Iyer A, Fairlie DP. and Sweet MJ.

Clinical and Translational Immunology20165, e62.

Protease activated receptor 2 (PAR2) modulators: a patent review (2010-2015). Yau MK, Lim J, Liu L. and Fairlie DP.

Expert Opinion on Therapeutic Patents2016 , 471-483.

Diversity of T Cells restricted by the MHC Class I-related molecule MR1 facilitates differential antigen recognition. Gherardin NA, Keller AN, Woolley RE, Le Nours J, Ritchie DS, Neeson PJ, Birkinshaw RW, Eckle SBG, Waddington JN, Liu L, Fairlie DP, Uldrich AP, Pellicci DG, McCluskey J, Godfrey DI, Rossjohn J.

Immunity201644, 32-45.

Differential anti-inflammatory activity of HDAC inhibitors in human macrophages and rat arthritis. Lohman RJ, Iyer A, Fairlie TJ, Cotterell A, Gupta P, Reid RC, Vesey DA, Sweet MJ, and Fairlie DP.

J Pharmacol Exp Ther.2016356, 387-396.

The intracellular pathway for the presentation of vitamin B-related antigens by the antigen-presenting molecule MR1. McWilliam HE, Eckle SB, Theodossis A, Liu L, Chen Z, Wubben J, Fairlie DP, Strugnell RA, Mintern JD, McCluskey J, Rossjohn J, Villadangos JA.

Nature Immunology 2016 17, 531-537.

Simultaneous uncoupled expression and purification of the dengue virus NS3 protease and NS2B co-factor domain. Shannon AE, Chappell KJ, Stoermer MJ, Chow SY, Kok WM, Fairlie DP, Young PR.

Protein Exp Purif2016 119, 124-129.

Receptor residence time trumps druglikeness and oral bioavailability in determining efficacy of complement C5a antagonists. Seow V, Lim J, Cotterell AJ, Yau MK, Xu W, Lohman RJ, Kok WM, Stoermer MJ, Sweet MJ, Reid RC, Suen JY, Fairlie DP.

Scientific Reports2016 6, 24575.

2015

Nutrient and immune sensing are obligate pathways in metabolism, immunity, and disease. Iyer A, Brown L, Whitehead JP, Prins JB, Fairlie DP.

FASEB J2015 29, 3612-3625.

Identification of phenotypically ad finctionally heterogeneous mouse mucosal-associated invariant T cells using MR1 tetramers. Rahimpour A, Koay HF, Enders A, Clanchy R, Eckle SBG, Meehan B, Chen Z, Whittle B, Liu L, Fairlie DP, Goodnow CC, McCluskey J, Rossjohn J, Uldrich AP, Pellicci DG, and Godfrey DI.

J Exp Med2015212, 1095-1108.

Functional Heterogeneity and antimycobacterial effects of mouse mucosal-associated invariant T Cells specific for Riboflavin metabolites. Sakala IG, Kjer-Nielsen L, Eickhoff CS, Wang X, Blazevic A, Liu L, Fairlie DP, Rossjohn J, Fremont DH, Hansen TH, Hoft DF.

J Immunol.2015195, 587-601.

Downsizing Proteins without losing potency or function. Fairlie DP, Yau MK, Hamidon JK, Singh R, Lim J, Suen JY, Rowley JA, Lohman RJ, Stoermer MJ, Iyer A, Reid RC.

Proc 24th Amer Peptide Symp (June 2015)2015  24APS.2015.016.

Histone deacetylase enzymes as drug targets for the control of the sheep blowfly, Lucilia cuprina. Kotze AC, Hines BM, Bagnall NH, Anstead CA, Gupta P, Reid RC, Ruffell AP, Fairlie DP.

Int. J.for Parasitology: Drugs and Drug Resistance 20155 , 201-208.

Thiazoles in peptides and peptidomimetics. Mak JYW, Xu W, Fairlie DP.

Topics in Heterocyclic Chemistry: “Heterocyclic Peptidomimetics” Chapter 12015  1-32.

Inhibiting histone deacetylase 1 (HDAC 1) suppresses both inflammation and bone loss in arthritis. Cantley MD, Fairlie DP, Bartold PM, Marino V. Gupta PK, Haynes DR.

Rheumatology201554, 1713-1723.

Facile synthesis of mono- and bis- methylated Fmoc-Dap, -Dab and -Orn amino acids. Lindahl F, Hoang HN, Fairlie DP, Cooper MA.

Chem Commun201551, 4496-4498.

Short hydrophobic peptides with cyclic constraints are potent glucagon-like peptide-1 receptor (GLP-1R) agonists. Hoang HN, Song K, Hill TA, Derksen DR, Edmonds DJ, Kok WM, Limberakis C, Liras S, Loria PM, Mascitti V, Mathiowetz AM, Mitchell JM, Piotrowski DW, Price DA, Stanton RV, Suen JY, Withka JM, Griffith DA, Fairlie DP.

J Med Chem201558, 4080-4085.

Peptide inhibitors of the Escherichia coli DsbA oxidative machinery essential for bacterial virulence. Duprez W, Premkumar L, Halili M, Lindahl F, Reid RC, Fairlie DP, Martin JL.

J Med Chem 201558, 577-587.

Small molecule inhibitors of disulfide bond formation by the bacterial DsbA-DsbB dual enzyme system. Halili MA, Bachu P, Lindahl F, Bechara C, Mohanty B, Reid RC, Scanlon MJ, Robinson CV, Fairlie DP, Martin JL.

ACS Chem Biol 201510, 957-964.

Helix-constrained nociceptin peptides are potent agonists and antagonists of ORL-1 and nociceptin. Lohman RJ, Harrison RS, Ruiz-Gomez G, Hoang HN, Shepherd NE, Chow S, Hill TA, Madala PK, Fairlie DP.

Vitamins and Hormones 201597, 1-55.

Potent complement C3a receptor agonists derived from oxazole amino acids: Structure-activity relationships. Singh R, Reed AN, Chu P, Scully CC, Yau MK, Suen JY, Durek T, Reid RC, Fairlie DP.

Bioorg Med Chem Lett 201525, 5604-5608.

Flexibility versus Rigidity for Orally Bioavailable Cyclic Hexapeptides. Nielsen DS, Lohman RJ, Hoang HN, Hill TA, Jones A, Lucke AJ, Fairlie DP.

Chembiochem 201516, 2289-2293.

Recognition of Vitamin B precursors and byproducts by Mucosal Associated Invariant T cells. Eckle SB, Corbett AJ, Keller A, Chen Z, Godfrey DI, Liu L, Mak JY, Fairlie DP, Rossjohn J, McCluskey J.

J Biol Chem 2015

Toward peptide-based inhibitors as therapies for Parkinson’s disease. Mason JM, Fairlie DP.

Future Med Chem 20157, 2103-2105.

Cyclic alpha-conotoxin peptidomimetic chimeras as potent GLP-1R agonists. Swedberg JE, Schroeder CI, Mitchell JM, Durek T, Fairlie DP, Edmonds DJ, Griffith DA, Ruggeri RB, Derksen DR, Loria PM, Liras S, Price DA, Craik DJ.

Eur J Med Chem 2015103, 175-184.

Comparing Sixteen Scoring Functions for Predicting Biological Activities of Ligands for Protein Targets. Xu W, Lucke AJ, Fairlie DP.

J Mol Graphics Modelling 201557, 76-88.

Three Homology Models of PAR2 Derived from Different Templates: Applications to Antagonist Discovery. Perry SR, Xu W, Wirija A, Lim J, Yau MK, Stoermer MJ, Lucke AJ, Fairlie DP.

J Chem Inf Model 201555, 1181-1191.

Repurposing Registered Drugs as Antagonists for Protease-Activated Receptor 2. Xu W, Lim J, Goh CY, Suen JY, Jiang Y, Yau MK, Wu KC, Liu L, Fairlie DP.

J Chem Inf Model 201555, 2079-2084.

Virtual Screening of Peptide and Peptidomimetic Fragments Targeted to Inhibit Bacterial Dithiol Oxidase DsbA. Duprez W, Bachu P, Stoermer MJ, Tay S, McMahon RM, Fairlie DP, Martin JL.

PLoS One 201510(7): e0133805.

Profiling the anti-protozoal activity of anti-cancer HDAC inhibitors against Plasmodium and Trypanosoma parasites. Engel JA, Jones AJ, Avery VM, Sumanadasa SD, Ng SS, Fairlie DP, Adams TS, Andrews KT.

Int J Parasitol Drugs Drug Resist 20155, 117-126.

2014

Nielson DS, Hoang HN, Lohman RJ, Hill TA, Lucke AJ, Craik DJ, Edmonds DJ, Griffith DA, Rotter CJ, Ruggeri RB, Price DA, Liras S, Fairlie DP. Improving on Nature: Making a Cyclic Heptapeptide Orally Bioavailable.

Angew Chem Int Ed 2014, 53, 12059 –12063.

Reid R, Yau M, Singh R, Lim J, Fairlie D. Stereoelectronic effects dictate molecular conformation and biological function of heterocyclic amides.

J Am Chem Soc. 2014, 136, 11914-11917.

Hill TA, Shepherd NE, Diness F, Fairlie DP. Constraining Cyclic peptides to Mimic Protein Structure Motifs.

Angew Chem Into Edit.  2014,  accepted 23 April.

de Arujo AD, Hoang HN, Kok WM, Diness F, Gupta G, Hill TA, Driver RW, Price DA, Liras S, Fairlie DP. Comparative α-Helicity of Cyclic Pentapeptides in Water.

Angew Chem Int Edit 2014, 53, 6965-6969.

Kurth F, Duprez W, Premkuman L, Schembri M, Fairlie DP, Martin JL. Crystal Structure of the Dithiol Oxidase DsbA Enzyme from Proteus Mirabilis Bound Non-Covalently to an Active Site Peptide Ligand.

J Biol Chem 2014, 289, 19810-19822.

Vadrevu SK, Chintala NK, Sharma SK, Sharma P, Cleveland C, Riediger L, Manne S, Fairlie DP, Gorczyca W, Almanza O, Karbowniczek M, Markiewski MM. Complement C5a receptor facilitates cancer metastasis by altering T cell responses in the metastatic niche.

Cancer Research 2014, 74, 3454-3465.

Corbett AJ, Eckle SBG, Birkinshaw RW, Liu L, Patel O, Mahony J, Chen Z, Reantra-goon R, Meehan B, Cao H, Williamson NA, Strugnell RA, Sinderen DV, Mak JYW, Fairlie DP*, Lars Kjer0Nielsen*, Rossjohn J*, McCluskey J*. T Cell activation by transitory neo-antigens derived from distinct microbial pathways.

Nature 2014, 509, 361-365.

Reid RC, Yau MK, Singh R, Hamidon JK, Lim J, Stoermer MJ, Fairlie DP. Potent Heterocyclic Ligands for Human Complement C3a Receptor.

J Med Chem  2014 57, 8459-8470.

Hill T, Lohman RJ, Hoang HN, Nielsen DS, Scully CSG, Kok WM, Liu L, Lucke AJ, Stoermer MJ, Schroeder CT, Chaousis S, Colless B, Bernhardt PV, Edmonds DJ, Griffith DA, Rotter CJ, Ruggeri RB, Price DA, Liras S, Craik DJ, Fairlie DP. Cyclic Penta- and Hexa- Leucine Peptides Without N-Methylation Are Orally Absorbed.

ACS Med Chem Lett 2014 5, 1148-1151.

Harrison RS, Shepherd NE, Hoang HN, Beyer RL, Ruiz-Gómez G, Kelso MJ, WM Kok, TA Hill, Abbenante G, Fairlie DP. Helical cyclic pentapeptides constrain HIV-1 Rev peptide for enhanced RNA binding.

Tetrahedron 2014  70, 7645 – 7650.

Trenholme K, Marek L, Duffy S, Pradel G, Fisher G, Hansen FK, Skinner-Adams TS, Butterworth A, Julius Ngwa C, Moecking J, Goodman CD, McFadden GI, Sumanadasa SD, Fairlie DP, Avery VM, Kurz T, Andrews KT. Lysine acetylation in sexual stage malaria parasites is a target for antimalarial small molecules.

Antimicrob Agents Chemother 2014, 58, 3666-3678.

Suen JY, Cotterell A, Lohman RJ, Lim J, Han A, Yau MK, Liu L, Cooper MA, Vesey DA, Fairlie DP. Pathway Selective Antagonism of Proteinase Activated Receptor 2.

Br J Pharmacol 2014, 171, 4112-4124.

Hollenberg MD, Mihara K, Polley D, Suen JY, Han A, Fairlie DP, Ramachandran R. Biased Signalling and Proteinase-Activated Receptors (PARS): Targeting Inflammatory Disease.

Br J Pharmacol 2014, 171, 1180-1194.

Eckle SBG, Birkinshaw RW, Kosteno L, Corbett AJ, McWilliam HEG, Reantragood R, Chen Z, Gherardin NA, Beddoe T, Liu L, Patel O, Meehan B, Fairlie DP, Villadangos JA, Godfrey DI, Kjer Nielsen L, McCluskey J, Rossjohn J. A Molecular Basis underpinning the T Cell Heterogeneity of Mucosal Associated Invariant T Cells.

J Exp Med 2014, 210, 2305-2320.

Poursharifi O, Lapointe M, Fisette A, Lu H, Roy C, Munkonda MN, Fairlie DP, Cianflone K. C5aR and C5L2 act in Concert to Balance Immunometabolism in Adipose Tissue.

Molecular and Cellular Endocronology  2014, 382 1180-1194.

2013

Reid RC, Yau M-K, Singh R, Hamidon JK, Reed AN, Chu P, Suen JY, Stoermer MJ, Blakeney JS, Lim J, Faber JM, Fairlie DP. Downsizing a Human Inflammatory Protein to a Small Molecule with Equal Potency and Functionality.

Nature Communications 2013, 4:2802. doi: 10.1038/ncomms3802.

Lim J, Iyer A, Liu L, Suen JY, Lohman RJ, Seow V, Yau MK, Brown L, Fairlie DP. Diet-induced obesity, adipose inflammation, and metabolic dysfunction correlating with PAR2 expression are attenuated by PAR2 antagonism.

FASEB J. 201327, 4757-4767.

Reantragoon R, Corbett AJ, Sakala IG, Gherardin NA, Furness JB, Birkinshaw R, Chen Z, Patel O, Kostenko L, Meehan B, Eckle SBG, Kedzierska K, Pellicci D, Liu L, Fairlie DP, Godfrey DI, Hansen TH, Kjer-Nielsen L, Rossjohn J, McCluskey J. Antigen-loaded MR1 tetramers define T cell receptor heterogeneity in Mucosal-Associated Invariant T-cells.

J Exp Med. 2013210, 2305-2320.

Seow V, Lim J, Iyer A, Suen JY, Ariffin JK, Hohenhaus DM, Sweet MJ, Fairlie DP. Inflammatory responses induced by lipopolysaccharide are amplified in primary human monocytes but suppressed in macrophages by complement protein C5a.

J Immunol. 2013, 191, 4308-4316.

Yau MK, Liu L, Fairlie DP. Towards Drugs for Protease-Activated Receptor 2 (PAR2).

J Med Chem. 201356, 7477–7497.

Patel O, Kjer-Nielsen L, Nours JL, Eckle SBG, Bikinshaw R, Beddoe T, Corbett AJ, Liu L, Miles JJ, Mehan B, Reantragoon R, Sandoval-Romero ML, Sullivan LC, Brooks AG, Chen Z, Fairlie DP, McCluskey J, Rossjohn J.  Recognition of vitamin B metabolites by mucosal-associated invariant T cells.

Nature Commun. 20134, 2142. doi: 10.1038/ncomms3142.

Shakespear MR, Hohenhaus DM, Kelly GM, Kamal NA, Gupta P, Labzin LI, Schroder K, Garceau V, Barbero S, Iyer A, Hume DA, Reid RC, Irvine KM, Fairlie DP, Sweet MJ.  Histone deacetylase 7 promotes Toll-like Receptor 4-dependent pro-inflammatory gene expression in macrophages.

J Biol Chem. 2013288, 25362-25374.

Lim J, Iyer A, Suen JY, Seow V, Reid RC, Brown L, Fairlie DP.   C5aR and C3aR antagonists each inhibit diet-induced obesity, metabolic dysfunction, and adipocyte and macrophage signaling.

FASEB J 201327, 822-831.

Artin Ghassemian,zy Ching-I Anderson Wang,y Mei-Kwan Yau, Robert C. Reid, Richard J. Lewis, David P. Fairlie, Paul F. Alewood and Thomas Durek.  Efficient chemical synthesis of human complement protein C3a.

Chem Commun, 2013, 49, 2356-2358.

Premkumar L, Heras B, Duprez W, Walden P, Halili M, Kurth F, Fairlie DP, Martin JL.  Rv2969c, essential for optimal growth in Mycobacterium tuberculosis, is a DsbA-like enzyme that interacts with VKOR-derived peptides and has atypical features of DsbA-like disulfide oxidases.

Acta Crystallogr D Biol Crystallogr. 2013D69, 1981–1994.

Tan CS, Hobson-Peters JM, Stoermer MJ, Fairlie DP, Khromykh AA, Hall RA.  An interaction between the methyltransferase and RNA dependent RNA polymerase domains of the West Nile virus NS5 protein.

J Gen Virol. 201394, 1961-1971.

Rao T, Ruiz-Gómez G, Hill TA, Hoang HN, Fairlie DP, Mason JM.  Truncated and helix-constrained peptides with high affinity and specificity for the cFos coiled-coil of AP-1.

PLoS One, 20138(3), e59415.

Kevin R.W. Ngoei, Dominic C.H. Ng, Paul R. Gooley, David P. Fairlie, Martin J. Stoermer, Marie A. Bogoyevitch.  Identification and characterization of bi-thiazole-2,2′-diamines as kinase inhibitory scaffolds.

Biochimica et Biophysica Acta20131834, 1077-1088.

Croker DE, Halai R, Fairlie DP, Cooper MA.  C5a, but not C5a-des Arg, induces upregulation of heteromer formation between complement C5a receptors C5aR and C5L2.

Immunol Cell Biol. 2013, doi: 10.1038/icb.2013.48. [Epub ahead of print]

Vesey DA,  Suen JY, Seow V, Lohman R-J, Liu L, Gobe GC, Johnson DW, Fairlie DP.  PAR2-induced inflammatory responses in human kidney tubular epithelial cells.

Am J Physiol Renal Physiol. 2013304, F737-F750.

Craik DJ, Fairlie DP, Liras S, Price D.  The Future of Peptide-Based Drugs.

Chem Biol Drug Des. 201381, 136-147.

Walden PM, Halili MA, Archbold JK, Lindahl F, Fairlie DP, Inaba K, Martin JL. The α-Proteobacteria Wolbachia pipientis Protein Disulfide Machinery Has a Regulatory Mechanism Absent in γ-Proteobacteria.

PLOS One  20138 (11), e81440.

2012

Madala PK, Fairlie DP, Bodén M. Matching cavities in G protein-coupled receptors to infer ligand-binding sites
J Chemo Info Model 2012, 52, 1401-1410.
Kjer-Nielsen L, Patel O, Nours JL, Meehan B, Corbett AJ, Liu L, Bhati M, Chen Z, Kostenko L, Reantragoon R, Williamson NA, Purcell AW, Dudek NL, McConville MJ, O’Hair RAJ, Khairallah GN, Godfrey DI, Fairlie DP, Rossjohn J, McCluskey J.
MR1 presents microbial vitamin B metabolites to MAIT cells.
Nature 2012491, 717-723.
Diness F, Fairlie DP.  Catalyst-Free N-arylation Using Unactivated Fluorobenzenes.
Agnew. Chem. Int. Edit.  2012, 51, 8012-8016.
Nielsen DS, Hoang HN, Lohman RJ, Diness F, Fairlie DP.  Total Synthesis, Structure, and Oral Absorption of a Thiazole Cyclic Peptide, Sanguinamide A.

Org Lett. 2012, 14, 5720-5723.

Lohman RJ, Cotterell AJ, Barry GD, Liu L, Suen JY, Vesey DA, Fairlie DP.  An antagonist of human protease activated receptor-2 attenuates PAR2 signalling, macrophage activation, mase cell degranulation, and collagen-induced arthritis in rats.

FASEB J. 2012, 26, 2877-2887.

Iyer A, Lim J, Poudyal H, Reid RC, Suen JY, Webster J, Prins JB, Whitehead JP, Fairlie DP*, Brown L*.  An inhibitor of pla2g2a modulates adipocyte signaling and protects against diet-induced metabolic syndrome in rats.

Diabetes 201261, 2320-2329.

Andrews KT, Trn TN, Fairlie DP.  Towards Histone Deacetylase Inhibitors as New Antimalarial Drugs.

Current Pharmaceutical Design 2012, 18, 3467-79.

Lohman RJ, Cotterell AJ, Suen JY, Liu L, Do TA, Vesey DA, Fairlie DP.  Antagonism of protease activated receptor 2 protects against experimental colitis.

J Pharmacol Exp Ther.  2012, 340, 256-265.

Suen JY, Barry GD, Lohman RJ, Halili MA, Cotterell AJ, Le GT, Fairlie DP. Modulating Human Proteinase Activated Receptor 2 with a Novel Antagonist (GB88) and Agonist (GB110).

Br J Pharmacol. 2012, 165, 1413-1423.

Shepherd NE, Harrison RS, Fairlie DP.  Targetng quorum sensin and competence stimulation for antimicrobial chemotherapy.

Current Drug Targets 2012, 13, 1348-1359.

Sumanadasa SD, Goodman CD, Lucke AJ, Skinner-Adams T, Sahama I, Haque A, Do TA, McFadden GI, Fairlie DP, Andrews KT.  Anti-malarial activity of the anti-cancer HDAC inhibitor SB939.

Antimicrob Agents Chemother.  2012 56, 3849-3856.

Madala PK, Fairlie DP, Boden M.  Matching cavities in G-protein-coupled receptors to infer ligand-binding sites.

J. Chem. Inf. Model.  2012  52, 1401-1410.

Andrews KT, Gupta AP, Tran TN, Fairlie DP, Gobert GN, Bozdech Z.  Comparative Gene Expression profiling of P. falciparum Malaria Parasites Exposed to Three different Histone Deacetylase Inhibitors.

PLOS One,  2012  7, e31847.

Hoang HN, Abbenante G, Hill TA, Ruiz-Gomez G, Fairlie DP.  Folding pentapeptides into left and right handed alpha helices.

Tetrahedron  2012  68, 4513-4516

Thundyil J, Pavlovski D, Hsieh YH, Gelderblom M, Magnus T, Fairlie DP, Arumugam TV.  C5a Receptor (CD88) Inhibition Improves Hypothermia-indused Neuroprotection in an In Vitro Ischemic Model.

Neuromolecular Med.  2012  14, 30-39.

Fairlie DP, Sweet MJ.  HDACs and their Inhibitors in Immunology:  Teaching Anticancer Drugs New Tricks.

Immunol Cell Biol,  2012  90, 3-5.

2011

Iyer A, Woodruff TM, Wu MC, Stylianou C, Reid RC, Fairlie DP, Taylor SM, Brown L. Inhibition of Inflammation and Fibrosis by a Complement C5a Receptor Antagonist in DOCA-Salt Hypertensive Rats.

J Cardiovasc Pharmacol. 2011, 58, 479-486.

Diness F, Nielsen DS, Fairlie DP. Synthesis of the Thiazole-Thiazoline Fragment of Largazole Analogues.

J Org Chem. 2011, 76, 9845-51.

Hoang HN, Driver RW, Beyer RL, Malde AK, Le GT, Abbenante G, Mark AE, Fairlie DP. Protein α-Turns Recreated in Structurally Stable Small Molecules.

Angew Chem Int Ed Engl. 2011, 50, 11107-11.

Cantley MD, Fairlie DP, Bartold PM, Rainsford KD, Le GT, Lucke AJ, Holding CA, and Haynes DR.* Inhibitors of Histone Deacetylases in Class I and Class II Suppress Human Osteoclasts In Vitro.

J. Cellular Physiology, 2011, 226, 3233-3241.

Marfurt J, Chalfein F, Prayoga P, Wabiser F, Kenangalem E, Piera KA, Fairlie DP, Tjitra E, Anstey NM, Andrews KT, Price RN. Ex Vivo Activity of Histone Deacetylase Inhibitors against Multidrug-Resistant Clinical Isolates of Plasmodium falciparum and P. vivax.

Antimicrob Agents Chemother. 2011, 55 961-6.

Cantley MD, Bartold PM, Marino V, Fairlie DP, Le GT, Lucke AJ, Haynes DR. Histone deacetylase inhibitors and periodontal bone loss

Journal of Periodontal Research, 2011, 46, 697-703.

Adams MN, Ramachandran R, Yau MK, Suen JY, Fairlie DP, Hollenberg MD, Hooper JD. Structure, function and pathophysiology of protease activated receptors.

Pharmacol Ther. 2011, 130, 248-282.

Singh Y, Sharpe PC, Hoang HN, Lucke AJ, McDowall AW, Bottomley SP, Fairlie DP. VIP: Amyloid Formation from an α-Helix Peptide Bundle Is Seeded by 310-Helix Aggregates.

Chemistry Eur. J. 2011, 17, 151-160.

Loughlin WA, Fairlie DP. Beta Strand Mimetics.
Protection Reactions, Medicinal Chemistry, Combinatorial Synthesis in Amino Acids,

Peptides and Proteins in Organic Chemistry 2011, 4 Chapter 3, 129-147.

Shakespear MR, Halili MA, Irvine KM, Fairlie DP, Sweet MJ. Histone deacetylases as regulators of inflammation and immunity.

Trends Immunol 2011, 32, 335-343.

2010

Iyer A, Fairlie DP, Prins JB, Hammock BD, Brown L. Inflammatory lipid mediators in adipocyte function and obesity.

Nature Reviews Endocrinology 2010, 6, 71-82.

Harrison RS, Shepherd NE, Hoang HN, Ruiz-Gomez G, Hill TA, Driver RW, Desai VS, Young PR, Abbenante G, Fairlie DP. Downsizing human, bacterial and viral proteins to short water-stable alpha helices that maintain biological potency.

Proc Natl Acad Sci U S A 2010, 107, 11686-11691.

Harrison RS, Ruiz-Gómez G, Hill TA, Chow SY, Shepherd NE, Lohman R-J, Abbenante G, Hoang HN, Fairlie DP. Novel Helix-Constrained Nociceptin Derivates Are Potent Agonists and Antagonists of ERK Phosphorylation and Thermal Analgesia in Mice.

J Med Chem 2010, 53, 8400–8408.

Barry GD, Suen JY, Le GT, Cotterell A, Reid RC, Fairlie DP. Novel Agonists and Antagonists for Human Protease Activated Receptor 2 (PAR2).

J Med Chem 2010, 53, 7428-7440.

Scully CC, Blakeney JS, Singh R, Hoang HN, Abbenante G, Reid RC, Fairlie DP. Selective hexapeptide agonists and antagonists for human complement C3a receptor.

J Med Chem 2010, 53, 4938-4948.

Löser R, Abbenante G, Madala PK, Halili M, Le GT, Fairlie DP. Non-covalent tripeptidylbenzyl and cyclohexyl amine inhibitors of the cysteine protease caspase-1.

J Med Chem 2010, 53, 2651–2655.

Ruiz-Gómez G, Tyndall JD, Pfeiffer B, Abbenante G, Fairlie DP. Update 1 of: Over one hundred peptide-activated G protein-coupled receptors recognize ligands with turn structure.

Chemical Reviews 2010, 110, PR1-PR41.

Loughlin WA, Tyndall JD, Glenn MP, Hill TA, Fairlie DP. Update1 of: Beta-Strand Mimetics.

Chemical Reviews 2010, 110, PR32-PR69.

Madala PK, Tyndall JD, Nall T, Fairlie DP. Update 1 of: Proteases Universally Recognize Beta Strands in their active sites.

Chemical Reviews 2010, 110, PR1-PR31.

Iyer A, Fenning A, Lim J, Le GT, Reid RC, Halili MA, Fairlie DP, Brown L. Antifibrotic activity of an inhibitor of histone deacetylases in DOCA-salt hypertensive rats.

Br J Pharmacol 2010, 159, 1408-1417.

Halili MA, Andrews MR, Labzin LI, Schroder K, Matthias G, Cao C, Lovelace E, Reid RC, Le GT, Hume DA, Irvine KM, Matthias P, Fairlie DP, Sweet MJ. Differential effects of selective HDAC inhibitors on macrophage inflammatory responses to the Toll-like receptor 4 agonist LPS.

J Leukoc Biol 2010, 87, 1103-1114.

Wheatley NC, Andrews KT, Tran TL, Lucke AJ, Reid RC, Fairlie DP. Antimalarial Histone Deacetylase Inhibitors Containing Cinnamate or NSAID Components.

Bioorg Med Chem Lett 2010, 20, 7080-7084.

Gupta PK, Reid RC, Liu L, Lucke AJ, Broomfield SA, Andrews MR, Sweet MJ, Fairlie DP. Inhibitors Selective For HDAC6 In Enzymes and Cells.

Bioorg. Med. Chem. Lett. 2010, 20, 7067-7070.

Suen JY, Gardiner B, Grimmond S, Fairlie DP. Profiling gene expression induced by protease-activated receptor 2 (PAR2) activation in human kidney cells.

PLoS One 2010, 5, e13809.

2009

Shepherd NE, Hoang HN, Abbenante G, Fairlie DP. Left- and right-handed alpha-helical turns in homo- and hetero-chiral helical scaffolds.
J Am Chem Soc. 2009, 131, 15877-15886.

Ma MT, Hoang HN, Scully CC, Appleton TG, Fairlie DP. Metal clips that induce unstructured pentapeptides to be alpha-helical in water.

J Am Chem Soc. 2009, 131, 4505-4512.

Ruiz-Gómez, G.; Lim, J.; Halili, MA; Le, GT; Madala, PK; Abbenante G.; Fairlie DP Structure-activity relationships for substrate-based inhibitors of human complement factor B.

J Med Chem 2009, 52, 6042-6052

Halili MA, Ruiz-Gómez G, Le GT, Abbenante G, Fairlie DP. Complement Factor C2, Inhibiting A Latent Serine Protease In The Classical Pathway Of Complement Activation.

Biochemistry 2009, 48, 8466-8472.

Driver R. W.; Hoang, H. N.; Abbebante, G, Fairlie, D. P. A cyclic beta-strand tripeptide with an alpha-helix like CD spectrum.

Org Lett 2009, 11, 3092-3095.

Robin G, Chappell K, Stoermer MJ, Hu SH, Young PR, Fairlie DP, Martin JL. Structure of West Nile virus NS3 protease: ligand stabilization of the catalytic conformation.

J Mol Biol 2009, 385, 1568-1577.

Halili MA, Andrews MR, Sweet MJ, Fairlie DP. Histone deacetylase inhibitors in inflammatory disease;

Curr Top Med Chem 2009, 9, 309-319.

Andrews KT, Tran TN, Wheatley NC, Fairlie DP. Targeting histone deacetylase inhibitors for anti-malarial therapy.

Curr Top Med Chem 2009, 9, 292-308.

Cantley M, D.; Bartold P, M.; Marino, V.; Reid, R. C.; Fairlie, D. P.; Haynes D. R. The use of Live Animal Micro Computer Tomography to Determine the Effect of a novel Phospholipase A2 Inhibitor on Alveolar Bone Loss in an In Vivo Mouse Model of Peridontitis.

J Periodontal Research 2009, 44, 317-322.

Kampmann T.; Yennamalli, R.; Campbell P.; Stoermer, M. J.; Fairlie, D. P.; Kobe, B.; Young PR. In silico screening of small molecule libraries using the dengue virus envelope E protein has identified compounds with antiviral activity against multiple flaviviruses.

Antiviral Research 2009, 84, 234-241

Stoermer MJ, Leung D, Young PR, Fairlie DP. Base-sensitivity of Arginine Alpha-Ketoamide Inhibitors of Serine Proteases.

Aust J Chem 2009, 62, 988-992.

Hans, D.; Young, P. R.; Fairlie, D. P. Tumor Associated Antigenic Peptides As Vaccine Candidates in “Tumor Associated Antigens”, Ed. O. Gires, B. Seliger;

Wiley-VCH, Weinham, 2009, Ch. 17, p.303-316. ISBN: 978-3-527-32084-4.

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