Scientific publications 2010

Aurelio L, Valant C, Flynn BL, Sexton PM, White JM, Christopoulos A, Scammells PJ (2010) Effects of Conformational Restriction of 2-Amino-3-benzoylthiophenes on A1 Adenosine Receptor Modulation. J. Med. Chem. 53, 6550–6559. Link to article.

Avlani VA, Langmead CJ, Guida E, Wood MD, Tehan BG, Herdon HJ, Watson JM, Sexton PM, Christopoulos A (2010) Orthosteric and allosteric modes of interaction of novel selective agonists of the M1 muscarinic acetylcholine receptor. Mol. Pharmacol. 78, 94-104. Link to article.

Baffert F, Régnier CH, De Pover A, Pissot-Soldermann C, Tavares GA, Blasco F, Brueggen J, Chène P, Drueckes P, Erdmann D, Furet P, Gerspacher M, Lang M, Ledieu D, Nolan L, Ruetz S, Trappe J, Vangrevelinghe E, Wartmann M, Wyder L, Hofmann F, Radimerski T. (2010) Potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor NVP-BSK805. Mol Cancer Ther. 9(7), 1945-55. Link to article.

Breton B, Lagace M, Bouvier M (2010) Combining resonance energy transfer methods reveals a complex between the α2A-adrenergic receptor, Gαi1β1γ2, and GRK2. FASEB J. 24, 4733-4743. Link to article.

Gregory KJ, Hall NE, Tobin AB, Sexton PM, Christopoulos A (2010) Identification of orthosteric and allosteric site mutations in M2 muscarinic acetylcholine receptors that contribute to ligand-selective signaling bias. J. Biol. Chem. 285, 7459-7474. Link to article.

Harikumar KG, Simms J, Christopoulos G, Sexton PM, Miller LJ (2010) Molecular Basis of Association of Receptor Activity-Modifying Protein 3 with the Family B G Protein-Coupled Secretin. Biochem. 48, 11773-11785. Link to article.

Harrison RS, Shepherd NE, Hoang HN, Ruiz-Gómez G, Hill TA, Driver RW, Desai VS, Young PR, Abbenante G, Fairlie DP (2010) Downsizing human, bacterial, and viral proteins to short water-stable alpha helices that maintain biological potency. Proc. Natl. Acad. Sci. USA, 107, 11686-91. Link to article.

Koole C, Wootten D, Simms J, Valant C, Sridhar R, Woodman OL, Miller LJ, Summers RJ, Christopoulos A, Sexton P (2010) Allosteric ligands of the glucagon-like peptide 1 receptor (GLP-1R) differentially modulate endogenous and exogenous peptide responses in a pathway-selective manner; implications for drug screening. Mol. Pharmacol, 78, 456-465. Link to article.

Lodge AP, Langmead CJ, Daniel G, Anderson G, Werry TD (2010) Performance of mouse neural stem cells as a screening reagent: Characterisation of PAC1 Activity in medium-throughput functional assays. J. Biol. Screen. 15, 159-168. Link to article.

Leach K, Loiacono RE, Felder CC, McKinzie DL, Mogg A, Shaw DB, Sexton PM, Christopoulos A (2010) Molecular mechanisms of action and In vivo validation of an M4 muscarinic acetylcholine receptor allosteric modulator with potential antipsychotic properties. Neuropharmacol. 35(4):855-69. Link to article.

May LT, Self TJ, Briddon SJ, Hill SJ (2010) The Effect of Allosteric Modulators on the Kinetics of Agonist-G Protein-Coupled Receptor Interactions in Single Living Cells. Mol Pharmacol. 78(3), 511-523. Link to article.

Narlawar R, Lane JR, Doddareddy M, Lin J, Brussee J, IJzerman AP (2010) Hybrid Ortho/Allosteric Ligands for the Adenosine A1 Receptor. J. Med. Chem. 53(8), 3028-3037. Link to article.

Nawaratne V, Leach K, Felder CC, Sexton PM, Christopoulos A (2010) Structural determinants of allosteric agonism and modulation at the M4 muscarinic acetylcholine receptor: identification of ligand-specific and global activation. J. Biol. Chem. 285, 19012-19021. Link to article.

Osmond RIW, Crouch MF, Dupriez V (2010) An emerging role for kinase screening in GPCR drug discovery. Curr Opin Mol Ther. 12(3), 305-15.Link to article.

Osmond RIW, Das S, Crouch MF (2010) Development of cell based assays for cytokine receptor signaling, using an AlphaScreen SureFire assay format. Anal. Biochem. 403, 94-101. Link to article.

Ouertatani-Sakouhi H, El-Turk F, Fauvet B, Cho MK, Karpinar DP, Le Roy D, Dewor M, Roger T, Bernhagen J, Calandra T, Zweckstetter M, Lashuel HA. (2010) Identification and characterization of novel classes of macrophage migration inhibitory factor (MIF) inhibitors with distinct mechanisms of action. J. Biol. Chem. 285(34):26581-98. Link to article.

Shyu M-H, Kao T-C, Yen G-C (2010) Oleanolic Acid and Ursolic Acid Induce Apoptosis in HuH7 Human Hepatocellular Carcinoma Cells through a Mitochondrial-Dependent Pathway and Downregulation of XIAP. J. Agric. Food. Chem. 58(10), 6110-6118. Link to article.

Siu T, Kozina ES, Jung J, Rosenstein C, Mathur A, Altman MD, Chan G, Xu L, Bachman E, Mo J-R, Bouthillette M, Rush T, Dinsmore CJ Marshall CG, Young JR (2010) The Discovery of Tricyclic Pyridone JAK2 Inhibitors: Part 1. Hit to Lead. Bioorg Med Chem Lett, 20(24), 7421-7425. Link to article.

Stewart GD, Sexton PM, Christopoulos A (2010) Prediction of functionally selective allosteric interactions at an M3 muscarinic acetylcholine receptor mutant using Saccharomyces cerevisiae. Mol. Pharmacol. 78(2):205-14. Link to article.

Valant C, Aurelio L, Urmaliya VB, White P, Scammells PJ, Sexton PM, Christopoulos A (2010) Delineating the Mode of Action of Adenosine A1 Receptor Allosteric Modulators. Mol. Pharmacol. 78(3), 444-455. Link to article.

van der Westhuizen ET, Christopoulos A, Sexton PM, Wade JD, Summers RJ. (2010) H2 relaxin is a biased ligand relative to H3 at the relaxin family peptide receptor 3 (RXFP3). Mol Pharmacol. 77(5), 759-772. Link to article.

Werden SJ, McFadden G (2010) Pharmacological manipulation of the Akt signaling pathway regulates myxoma virus replication and tropism in human cancer cells. J. Virol. 84, 3287-3302. Link to article.

Last updated: September 2011