Publications 2012-2018

2018

 

Complement C3a and C5a receptors promote GVHD by suppressing mitophagy in recipient dendritic cells. Nguyen H, Kuril S, Bastian D, Kim J, Zhang M, Vaena SG, Dany M, Dai M, Heinrichs JL, Daenthanasanmak A, Iamsawat S, Schutt S, Fu J, Wu Y, Fairlie DP, Atkinson C, Ogretmen B, Tomlinson S, Yu XZ. 

JCI Insight 2018 , Dec 20;3(24). pii: 121697.

 

Chemical Approaches To Modulating Complement-Mediated Diseases. Iyer A, Xu W, Reid RC, Fairlie DP. 

J Med Chem 201861, 3253-3276.

 

Bicyclic helical peptides as dual inhibitors selective for Bcl2A1 and Mcl-1 proteins. de Araujo AD, Lim J, Wu KC, Xiang Y, Good AC, Skerlj R, Fairlie DP. 

J Med Chem 201861, 2962-2972.

 

Recipient mucosal-associated invariant T cells control GVHD within the colon. Varelias A, Bunting MD, Ormerod KL, Koyama M, Olver SD, Straube J, Kuns RD, Robb RJ, Henden AS, Cooper L, Lachner N, Gartlan KH, Lantz O, Kjer-Nielsen L, Mak JY, Fairlie DP, Clouston AD, McCluskey J, Rossjohn J, Lane SW, Hugenholtz P, Hill GR. 

J Clin Invest 2018128, 1919-1936.

 

MAIT cells protect against pulmonary Legionella longbeachae infection. Wang H, D'Souza C, Lim XY, Kostenko L, Pediongco TJ, Eckle SBG, Meehan BS, Shi M, Wang N, Li S, Liu L, Mak JYW, Fairlie DP, Iwakura Y, Gunnersen JM, Stent AW, Godfrey DI, Rossjohn J, Westall GP, Kjer-Nielsen L, Strugnell RA, McCluskey J, Corbett AJ, Hinks 

Nature Communications 20189, 3350.

 

Hepatic expression profiling identifies steatosis-independent and steatosis-driven advanced fibrosis genes. Ramnath D, Irvine KM, Lukowski SW, Horsfall LU, Loh Z, Clouston AD, Patel PJ, Fagan KJ, Iyer A, Lampe G, Stow JL, Schroder K, Fairlie DP, Powell JE, Powell EE, Sweet MJ.  

JCI Insight20183, (14), pii: 120274

 

Lysine deacetylases and regulated glycolysis in macrophages. Shakespear MR, Iyer A, Cheng CY, Das Gupta K, Singhal A, Fairlie DP, Sweet MJ.  

Trends Immunol201839, 473-488.

 

Chemically diverse helix-constrained peptides using selenocysteine crosslinking. Dantas de Araujo A, Perry SR, Fairlie DP.  

Org Lett201820, 1453-1456.

 

Mucosal-associated invariant T cells augment immunopathology and gastritis in chronic Helicobacter pylori Infection. D'Souza C, Pediongco T, Wang H, Scheerlinck JY, Kostenko L, Esterbauer R, Stent AW, Eckle SBG, Meehan BS, Strugnell RA, Cao H, Liu L, Mak JYW, Lovrecz G, Lu L, Fairlie DP, Rossjohn J, McCluskey J, Every AL, Chen Z, Corbett AJ. 

J Immunol2018200, 1901-1916.

 

Glucuronic acid as a helix-inducing linker in short peptides. Wu C, Hoang HN, Liu L, Fairlie DP. 

Chemical Communications201854, 2162-2165.

 

A potent antagonist of protease-activated receptor 2 that inhibits multiple signalling functions in human cancer cells. Jiang Y, Yau MK, Lim J, Wu KC, Xu W, Suen JY, Fairlie DP. 

J Pharmacol Exp Ther2018346, 246-257.

 

Contiguous hydrophobic and charged surface patches in short helix-constrained peptides drive cell permeability. Perry SR, Hill TA, de Araujo AD, Hoang HN, Fairlie DP. 

Org Biomol Chem201816, 367-371.

 

 

2017

 

Exploiting a novel conformational switch to control innate immunity mediated by complement protein C3a. Lohman RJ, Hamidon JK, Reid RC, Rowley JA, Yau MK, Halili MA, Nielsen DS, Lim J, Wu KC, Loh Z, Do A, Suen JY, Iyer A, Fairlie DP. 

Nature Communications20178, 351.

 

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 Communications20178, 14599.

 

Drugs and drug-like molecules can modulate the function of mucosal-associated invariant T cells. 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 Immunology201718, 402-411.

 

Orally Absorbed Cyclic Peptides. Nielsen DS, Shepherd NE, Xu W, Lucke AJ, Stoermer MJ, Fairlie DP. 

Chemical Reviews2017117, 8094-8128.

 

Protease activated receptor 2 controls myelin development, resiliency and repair.Yoon H, Radulovic M, Walters G, Paulsen AR, Drucker K, Starski P, Wu J, Fairlie DP, Scarisbrick IA.  

GLIA. 2017, 65, 2070-2086.

 

Europium-Labeled Synthetic C3a Protein as a Novel Fluorescent Probe for Human Complement C3a ReceptorDantas de Araujo A, Wu C, Wu KC, Reid RC, Durek T, Lim J, Fairlie DP.  

Bioconjug Chem201728, 1669-1676.

 

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 Immunol2017198, 2989-2999.

 

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 Biol201712, 1217-1226.

 

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 Research2017117, 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*.  

Chemistry201723, 1694-1701.

 

Stereoelectronic effects on dienophile separation influence the Diels-Alder synthesis of molecular clefts.Stoermer MJ, Wickramasinghe WA, Byriel KA, Hockless DCR, Skelton BW, Sobolev AN, White AH, Mak JYW, Fairlie DP.  

Eur J Org Chem2017 , 6793-6796.

 

Downsizing Proto-oncogene cFos to short helix-constrained peptides that bind Jun.Baxter D, Perry SR, Hill TA, Kok WM, Zaccai NR, Brady RI, Fairlie DP,* Mason JM*.  

ACS Chem Biol201712, 2051-2061.

 

Tolyporphin Macrocycles from the Cyanobacterium Tolypothrix nodosa Selectively Bind Copper and Silver and Reverse Multidrug Resistance.Prinsep MR, Appleton TG, Hanson GR, Lane I, Smith CD, Puddick J, Fairlie DP.  

Inorg Chem201756, 5577-5585.

 

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

Bone201795, 162-174.

 

Alpha Helix Nucleation by a Simple Cyclic TetrapeptideHoang HN, Wu C, Beyer RL, Hill TA, Fairlie DP.  

Aust J Chem201770, 213-219.

 

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 Immunol201710, 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 Lett20178, 22-26.

 

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 Ther2017360, 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 Chem2017127, 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.

 

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 2016 , accepted for publication.

 

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.


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