PUBLICATIONS 2014

Constraining cyclic peptides to mimic protein structure motifs.

Hill TA, Shepherd NE, Diness F, Fairlie DP.Angew Chem Int Ed Engl. 2014 Nov 24;53(48):13020-41. doi: 10.1002/anie.201401058. Epub 2014 Oct 6.PMID: 25287434 Review.

 

 

 

 

 

 

 

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

Hollenberg MD, Mihara K, Polley D, Suen JY, Han A, Fairlie DP, Ramachandran R.Br J Pharmacol. 2014 Mar;171(5):1180-94. doi: 10.1111/bph.12544.PMID: 24354792 Free PMC article. Review.

 

 

 

 

 

 

 

Comparative α-helicity of cyclic pentapeptides in water.

de Araujo AD, Hoang HN, Kok WM, Diness F, Gupta P, Hill TA, Driver RW, Price DA, Liras S, Fairlie DP.Angew Chem Int Ed Engl. 2014 Jul 1;53(27):6965-9. doi: 10.1002/anie.201310245. Epub 2014 May 14.PMID: 24828311

 

 

 

 

 

 

 

Pathway-selective antagonism of proteinase activated receptor 2.

Suen JY, Cotterell A, Lohman RJ, Lim J, Han A, Yau MK, Liu L, Cooper MA, Vesey DA, Fairlie DP.Br J Pharmacol. 2014 Sep;171(17):4112-24. doi: 10.1111/bph.12757. Epub 2014 Jul 2.PMID: 24821440 Free PMC article.

 

 

 

 

 

 

 

Potent heterocyclic ligands for human complement c3a receptor.

Reid RC, Yau MK, Singh R, Hamidon JK, Lim J, Stoermer MJ, Fairlie DP.J Med Chem. 2014 Oct 23;57(20):8459-70. doi: 10.1021/jm500956p. Epub 2014 Oct 8.PMID: 25259874

 

 

 

 

 

 

 

Improving on nature: making a cyclic heptapeptide orally bioavailable.

Nielsen 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.Angew Chem Int Ed Engl. 2014 Nov 3;53(45):12059-63. doi: 10.1002/anie.201405364. Epub 2014 Sep 12.PMID: 25219505

 

 

 

 

 

 

 

T-cell activation by transitory neo-antigens derived from distinct microbial pathways.

Corbett AJ, Eckle SB, Birkinshaw RW, Liu L, Patel O, Mahony J, Chen Z, Reantragoon R, Meehan B, Cao H, Williamson NA, Strugnell RA, Van Sinderen D, Mak JY, Fairlie DP, Kjer-Nielsen L, Rossjohn J, McCluskey J.Nature. 2014 May 15;509(7500):361-5. doi: 10.1038/nature13160. Epub 2014 Apr 2.PMID: 24695216

 

 

 

 

 

 

 

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C5aR and C5L2 act in concert to balance immunometabolism in adipose tissue.

Poursharifi P, Lapointe M, Fisette A, Lu H, Roy C, Munkonda MN, Fairlie DP, Cianflone K.Mol Cell Endocrinol. 2014 Jan 25;382(1):325-333. doi: 10.1016/j.mce.2013.10.019. Epub 2013 Oct 25.PMID: 24397921

 

 

 

 

 

 

 

Complement c5a receptor facilitates cancer metastasis by altering T-cell responses in the metastatic niche.

Vadrevu SK, Chintala NK, Sharma SK, Sharma P, Cleveland C, Riediger L, Manne S, Fairlie DP, Gorczyca W, Almanza O, Karbowniczek M, Markiewski MM.Cancer Res. 2014 Jul 1;74(13):3454-65. doi: 10.1158/0008-5472.CAN-14-0157. Epub 2014 May 1.PMID: 24786787

 

 

 

 

 

 

 

Rational design and synthesis of an orally bioavailable peptide guided by NMR amide temperature coefficients.

Wang CK, Northfield SE, Colless B, Chaousis S, Hamernig I, Lohman RJ, Nielsen DS, Schroeder CI, Liras S, Price DA, Fairlie DP, Craik DJ.Proc Natl Acad Sci U S A. 2014 Dec 9;111(49):17504-9. doi: 10.1073/pnas.1417611111.PMID: 25416591 Free PMC article.

 

 

 

 

 

 

 

Lysine acetylation in sexual stage malaria parasites is a target for antimalarial small molecules.

Trenholme K, Marek L, Duffy S, Pradel G, Fisher G, Hansen FK, Skinner-Adams TS, Butterworth A, Ngwa CJ, Moecking J, Goodman CD, McFadden GI, Sumanadasa SD, Fairlie DP, Avery VM, Kurz T, Andrews KT.Antimicrob Agents Chemother. 2014 Jul;58(7):3666-78. doi: 10.1128/AAC.02721-13. Epub 2014 Apr 14.PMID: 24733477 Free PMC article.

 

 

 

 

 

 

 

A molecular basis underpinning the T cell receptor heterogeneity of mucosal-associated invariant T cells.

Eckle SB, Birkinshaw RW, Kostenko L, Corbett AJ, McWilliam HE, Reantragoon 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.J Exp Med. 2014 Jul 28;211(8):1585-600. doi: 10.1084/jem.20140484. Epub 2014 Jul 21.PMID: 25049336 Free PMC article.

 

 

 

 

 

 

 

Stereoelectronic effects dictate molecular conformation and biological function of heterocyclic amides.

Reid RC, Yau MK, Singh R, Lim J, Fairlie DP.J Am Chem Soc. 2014 Aug 27;136(34):11914-7. doi: 10.1021/ja506518t. Epub 2014 Aug 13.PMID: 25102224

 

 

 

 

 

 

 

Cyclic Penta- and Hexaleucine Peptides without N-Methylation Are Orally Absorbed.

Hill TA, Lohman RJ, Hoang HN, Nielsen DS, Scully CC, Kok WM, Liu L, Lucke AJ, Stoermer MJ, Schroeder CI, Chaousis S, Colless B, Bernhardt PV, Edmonds DJ, Griffith DA, Rotter CJ, Ruggeri RB, Price DA, Liras S, Craik DJ, Fairlie DP.ACS Med Chem Lett. 2014 Aug 4;5(10):1148-51. doi: 10.1021/ml5002823. eCollection 2014 Oct 9.PMID: 25313329 Free PMC article.

 

 

 

 

 

 

 

Crystal structure of the dithiol oxidase DsbA enzyme from proteus mirabilis bound non-covalently to an active site peptide ligand.

Kurth F, Duprez W, Premkumar L, Schembri MA, Fairlie DP, Martin JL.J Biol Chem. 2014 Jul 11;289(28):19810-22. doi: 10.1074/jbc.M114.552380. Epub 2014 May 15.PMID: 24831013 Free PMC article.