Scientific publications 2012

Adams AC, Coskun T, Irizarry Rovira AR, Schneider MA, Raches DW, Micanovic R, Bina HA, Dunbar JD, Kharitonenkov A. Fundamentals of FGF19 & FGF21 Action In Vitro and In Vivo. PLOS One, 2012. Link to article.

Anavi-Goffer S, BaillieG, Irving AJ, Gertsch J, Greig IR, Pertwee RG, Ross RA. Modulation of L-α-lysophosphatidylinositol /GPR55 MAP kinase signalling by cannabinoids. J. Biol. Chem. 2012; 287, 91-104. Link to article.

Baillie GL, Horswill J, Anavi-Goffer S, Reggio PH, Abood ME, Bolognini D, McAllister S, Strange PG, Stephens GJ, Pertwee RG, Ross RA. CB1 Receptor Allosteric Modulators Display both agonist and signaling pathway specificity. Mol. Pharmacol. (2012), In Press. Link to article.

Brandvold KR, Steffey ME, Fox CC, Soellner MB. Development of a Highly Selective c-Src Kinase Inhibitor. ACS Chem. Biol. 2012; 7(8), 1393-1398. Link to article.

Canals M, Lane JR, Wen A, Scammells PJ, Sexton PM, Christopoulos A. A Monod-Wyman-Changeux mechanism can explain G protein-coupled receptor (GPCR) allosteric modulation. J. Biol. Chem. 2012; 287, 650-659. Link to article.

Davey AE, Leach K, Valant C, Conigrave AD, Sexton PM, Christopoulos A. Positive and Negative Allosteric Modulators Promote Biased Signaling at the Calcium-Sensing Receptor. Endocrinol. 2012,153(3):1232-41. Link to article.

Digby GJ, Noetzel MJ, Bubser M, Bubser TJ, Walker AG, Byun NE, Lebois EP, Xiang Z, et al. Novel Allosteric Agonists of M1 Muscarinic Acetylcholine Receptors Induce Brain Region-Specific Responses That Correspond with Behavioral Effects in Animal Models. Neurobiol. Dis. 2012, 32(25): 8532-8544. Link to article.

Fosgerau K, Jessen L, Tolborg JL, Østerlund T, Larsen KS, Rolsted K, Brorson M, Jelsing J, Neerup TSR. The novel GLP-1-gastrin dual agonist, ZP3022, increases β-cell mass and prevents diabetes in db/db mice. Diabetes Obes Metab. 2012. In Press. Link to article.

Gregory KJ, Noetzel MJ, Rook JM, Vinson PN, Stauffer SR, Rodriguez AL, Emmitte KA, Zhou Y, Chun AC, Felts AS, Chauder BA, Lindsley CW, Niswender CM, Conn PJ. Investigating mGlu5 Allosteric Modulator Cooperativity, Affinity and Agonism: Enriching Structure-function Studies and Structure-activity Relationships. Mol. Pharmacol. 2012; 82(5), 860-875. Link to article.

Halai R, Croker DE, Suen JY, Fairlie DP, Cooper MA. A Comparative Study of Impedance versus Optical Label-Free Systems Relative to Labelled Assays in a Predominantly Gi Coupled GPCR (C5aR) Signalling. Biosensors. 2012, 2(3), 273-290. Link to article.

Harikumar KG, Wootten D, Pinon DI, Koole C, Ball AM, Furness SGB, Graham B, Dong M, Christopoulos A, Miller LJ, Sexton PM. Glucagon-like peptide-1 receptor dimerization differentially regulates agonist signaling but does not affect small molecule allostery.
PNAS, 2012, 109(45),18607-18612. Link to article.

Koole C, Wootten D, Simms J, Miller LJ, Christopoulos A, Sexton PM. The second extracellular loop of the human glucagon-like peptide-1 receptor (GLP-1R) has a critical role in GLP-1 peptide binding and receptor activation. J. Biol. Chem (2012), 287(6):3642-58. Link to article.

Kraus M, Wang Y, Aleksandrowicz D, Bachman E, Szewczak AA et al. Efficacious Intermittent Dosing of a Novel JAK2 Inhibitor in Mouse Models of Polycythemia Vera. PLOS One, 2012. Link to article.

Leach K, Wen A, Davey AE, Sexton PM, Conigrave AD, Christopoulos A. Identification of Molecular Phenotypes and Biased Signaling Induced by Naturally Occurring Mutations of the Human Calcium-Sensing Receptor. Endocrinology, 2012; 153(9), 4304-4316. Link to article.

Li Z, Blad CC, van der Sluis RJ, de Vries H, Van Berkel TJC, IJzerman AP, Hoekstra M. Effects of pyrazole partial agonists on HCA2-mediated flushing and VLDL-triglyceride levels in mice. Br. J. Pharmacol. 2012; 167(4), 818-825. Link to article.

Lin D, Guo Q, Luo J, Zhang J, Nguyen K, Chen M, Tran T, Dransfield PJ, Brown SP, Houze J, Vimolratana M, Jiao XY, Wang Y, Birdsall NJM, Swaminath G. Identification and Pharmacological Characterization of Multiple Allosteric Binding Sites on the FFA1 Receptor. Mol. Pharmacol. 2012; 82(5), 843-859. Link to article.

Luedtke RR, Mishra Y, Wang O, Griffin SA, Bell-Horner C, Taylor M, Vangveravong S, Dillon GH, Huang R-O, Reichert DE, Mach RH. Comparison of the binding and functional properties of two structurally different D2 dopamine receptor subtype selective compounds. ACS Chem. Neurosci. 2012, In Press. Link to article.

Luster TA, Mukherjee I, Carrell JA, Cho YH, Gill J, Kelly L, Garcia A, Ward C, Oh L, Ullrich SJ, Migone T-S, Humphreys R. Fusion toxin BLyS-Gelonin inhibits growth of malignant human B cell lines in vitro and in vivo. PloS one, 2012, 7(10): e47361. Link to article.

McRobb FM, Crosby IT, Yuriev E, Lane R, Capuano B. Homobivalent ligands of the atypical antipsychotic clozapine: Design, synthesis and pharmacological evaluation. J. Med. Chem. 2012; 55(4):1622-34. Link to article.

Molè D, Gentilin E, Gagliano T, Tagliati F, Bondanelli M, Pelizzo MR, Rossi M, Filieri C, Pansini G, degli Uberti EC, Zatelli MC. Protein Kinase C: A Putative New Target for the Control of Human Medullary Thyroid Carcinoma Cell Proliferation in Vitro. Endocrinol. 2012. 153(5):2088-2098. Link to article.

Montano-Almendras CP, Essaghir A, Schoemans H, Varis I, Noel LA, Velghe AI, Latinne D, Knoops L, Demoulin J-BB. ETV6-PDGFRB and FIP1L1-PDGFRA stimulate human hematopoietic progenitor proliferation and differentiation into eosinophils: role of NF-κB. Haematol , 2012. Link to article.

Osmond RIW, Martin-Harris MH, Crouch MF, Park J, Morreale E, Dupriez VJ. G-Protein-Coupled Receptor-Mediated MAPK and PI3-Kinase Signaling Is Maintained in Chinese Hamster Ovary Cells after γ-Irradiation. J. Biomol. Screen. 2012, 17(3), 361-369. Link to article.

Qian J, Mason JL, Holskin BP, Murray KA, Meyer SL, Ator MA, Angeles TS. Comparison of Two Homogeneous Cell-Based Kinase Assays for JAK2 V617F: SureFire® pSTAT5 and GeneBLAzer® Fluorescence Resonance Energy Transfer Assays. Assay Drug Dev Technol. 2012, 10(2):212-217. Link to article.

Sava A, Formaggio E, Carignani C, Andreetta F, Bettini E, 1, Griffante C. NMDA-induced ERK signalling is mediated by NR2B subunit in rat cortical neurons and switches from positive to negative depending on stage of development. Neuropharmacol. 2012, 62(2):925-32. Link to article.

Seljeset S, Siehler S. Receptor-specific regulation of ERK1/2 activation by members of the “free fatty acid receptor” family.” J. Recept. Sig. Trans. 2012, 32(4): 196-201. Link to article.

Shabanpoor F, Hossain MA, Ryan PJ, Belgi A, Layfield S, Kocan M, Zhang S, Samuel CS, Gundlach AL, Bathgate RAD, Separovic F, Wade JD.Minimization of relaxin-3 leading to high affinity analogues with increased selectivity for relaxin-family peptide 3 receptor (RXFP3) over RXFP1. J. Med. Chem. 2012; 55(4), pp 1671–1681. Link to article.

Sharir H, Console-Bram L, Mundy C, Popoff SN, Kapur A, Abood ME. The Endocannabinoids Anandamide and Virodhamine Modulate the Activity of the Candidate Cannabinoid Receptor GPR55. J Neuroimmune Pharmacol. 2012. Link to article.

Sheehan AJ, Goodrich W, Banks P, Crouch MF, Osmond RIW. Development and validation of a single-well cell-based assay for the detection of endogenous phosphoproteins.” ASSAY and Drug Development Technologies (2012). In Press. Link to article.

Sheng, YH, Triyana S, Wang R, Das I, Gerloff K, Florin TH, Sutton P, McGuckin MA. MUC1 and MUC13 differentially regulate epithelial inflammation in response to inflammatory and infectious stimuli. Mucosal Immunol. (2012), In Press. Link to article.

Smith AL, D’Angelo ND, Bo YY, Booker SK, Cee VJ, Herberich B et al. Structure-Based Design of a Novel Series of Potent, Selective Inhibitors of the Class I Phosphatidylinositol 3-Kinases. J. Med. Chem. 2012, 55(11), 5188–5219. Link to article.

Stallaert W, Dorn JF, van der Westhuizen E, Audet M, Bouvier M. Impedance Responses Reveal β2-Adrenergic Receptor Signaling Pluridimensionality and Allow Classification of Ligands with Distinct Signaling Profiles. PLOS, 2012. Link to article.

Tan JHY, Canals M, Ludeman JP, Wedderburn J, Boston C, Butler SJ, Carrick AM, Parody TR, Taleski D, Christopoulos A, Payne RJ, Stone MJ. Design and receptor interactions of an obligate dimeric mutant of the chemokine monocyte chemoattractant protein-1 (MCP-1). J. Biol. Chem. 2012, 287(18):14692-14702. Link to article.

Tulio, AZ, Chang C, Edirisinghe I, White KD, Jablonski JE, Banaszewski K, Kangath A, Tadapaneni RK, Burton-Freeman B, Jackson LS. Berry Fruits Modulated Endothelial Cell Migration and Angiogenesis via Phosphoinositide-3 Kinase/Protein Kinase B Pathway in Vitro in Endothelial Cells. J. Ag. Food. Chem. 60(23), 5803–5812. Link to article.

Valant C, Aurelio L, Devine S, Ashton T, White JM, Sexton PM, Christopoulos A, Scammells PJ. Synthesis and Characterization of Novel 2-Amino-3-benzoylthiophene Derivatives as Biased Allosteric Agonists and Modulators of the Adenosine A1 Receptor. J. Med. Chem. 2012, 55(5), 2367–2375. Link to article.

Valant C, Felder CC, Sexton PM, Christopoulos A. Probe Dependence in the Allosteric Modulation of a G Protein-Coupled Receptor: Implications for Detection and Validation of Allosteric Ligand Effects. Mol. Pharmacol. 2012, 81(1), 41-52. Link to article.

Wookey PJ, McLean CA, Hwang P, Furness SGB, Nguyen S, Kourakis A, Hare D, Rosenfeld JV. The expression of calcitonin receptor detected in malignant cells of the brain tumour glioblastoma multiforme and functional properties in the cell line A172. Histopathology, 2012, 60(6), 895–910. Link to article.

Wootten D, Savage EE, Valant C, May LT, Sloop KW, Ficorilli J, Showalter AD, Willard FS, Christopoulos A, Sexton P. Allosteric Modulation of Endogenous Metabolites as an Avenue for Drug Discovery. Mol. Pharmacol. 2012, 82(2), 281-290. Link to article.

Xu T-R, Ward RJ, Pediani JD, Milligan G. Intramolecular fluorescence resonance energy transfer (FRET) sensors of the orexin OX1 and OX2 receptors identify slow kinetics of agonist activation. J. Biol. Chem. 2012, 287, 14937-14949. Link to article.

Zhan YZ, Zhang YM, Liu CC, Zhang J, Smith WW, Wang N, Chen YN, Zheng L, He LC. A novel taspine derivative, HMQ1611 inhibits breast cancer cell growth via estrogen receptor α and epidermal growth factor receptor signaling pathways. Cancer Prev. Res. 2012, 5(6); 864–873.Link to article.

Zimmerman B, Beautrait A, Aguila B, Charles R, Escher E, Claing A, Bouvier M, Laporte SA. Differential β-Arrestin–Dependent Conformational Signaling and Cellular Responses Revealed by Angiotensin Analogs. Sci. Signal. 2012, 5, ra33. Link to article.

Last updated: Nov 2012