Scientific publications 2011

Alvarez-Curto E, Prihandoko R, Tautermann CS, Zwier JM, Pediani JD, Lohse MJ, Hoffmann C, Tobin AB, Milligan G. Developing Chemical Genetic Approaches to Explore G Protein-coupled Receptor Function – Validation of the use of a Receptor Activated Solely by Synthetic Ligand (RASSL). Mol Pharmacol. 2011, 80(6):1033-1046. Link to article.

Aurelio L, Christopoulos A, Flynn BL, Scammells PJ, Sexton PM, Valant C. The synthesis and biological evaluation of 2–amino–4,5,6,7,8,9–hexahydrocycloocta[b]thiophenes as allosteric modulators of the A1 adenosine receptor. Bioorg. Med. Chem .Lett. 2011, 21(12):3704-3707.Link to article.

Babij C, Zhang Y, Kurzeja RJM, Munzli A, Shehabeldin A, Fernando M, Quon K, Kassner PD, Ruefli-Brasse AA, Watson VJE, Fajardo F, Jackson A, Zondlo J, Sun Y, Ellison AR, Plewa CA, San Miguel T, Robinson J, McCarter J, Schwandner R, Judd T, Carnahan J, Dussault I. STK33 Kinase Activity is Non-Essential in KRAS-Dependent Cancer Cells. Cancer Res. 2011, 71, 5818. Link to article.

Berg KA, Rowan M, Sanchez TA, Silva M, Patwardhan AM, Milam SB, Hargreaves KM, Clarke WP. Regulation of kappa opioid receptor signaling in peripheral sensory neurons in vitro and in vivo. J.Pharmacol. Exp. Ther. 2011, 338(1), 92-99. Link to article.

Bouchecareilh M, Higa A, Fribourg S, Moenner M, Chevet E. Peptides derived from the bifunctional kinase/RNase enzyme IRE1α modulate IRE1α activity and protect cells from endoplasmic reticulum stress. FASEB J. 2011, 25(9), 3115-3129. Link to article.

D’Angelo ND, Kim T-S, Andrews K, Booker SK, Caenepeel S, Chen K, D’Amico D, Freeman D, Jiang J, Liu L, McCarter JD, San Miguel T, Mullady EL, Schrag M, Subramanian R, Tang J, Wahl RC, Wang L, Whittington DA, Wu T, Xi N, Xu Y, Yakowec P, Yang K, Zalameda LP, Zhang N, Hughes P, Norman MH. Discovery and Optimization of a Series of Benzothiazole Phosphoinositide 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Dual Inhibitors. J. Med. Chem. 2011, 54(6):1789-1811. Link to article.

Dalrymple MB, Jaeger WC, Eidne KA, Pfleger KDG. Temporal Profiling of Orexin Receptor-Arrestin-Ubiquitin Complexes Reveals Differences between Receptor Subtypes. J Biol Chem. 2011, 286(19), 16726-16733. Link to article.

Drew AE, Al-Assaad S, Yu V, Andrews P, Merkel P, Szilvassy S, Emkey R, Lewis R, Brake RL Comparison of 2 Cell-Based Phosphoprotein Assays to Support Screening and Development of an ALK Inhibitor. J. Biomol. Screen. 2011, 16(2), 164-173. Link to article.

Drolet RE, Sanders JM, Kern JT. Leucine-Rich Repeat Kinase 2 (LRRK2) Cellular Biology: A Review of Recent Advances in Identifying Physiological Substrates and Cellular Functions. J Neurogenet. 2011, 25(4):140-151. Link to article.

Gao Z-G, Verzijl D, Zweemer A, Ye K, Göblyös A, IJzerman AP, Jacobson KA. Functionally biased modulation of A3 adenosine receptor agonist efficacy and potency by imidazoquinolinamine allosteric enhancers. Biochem. Pharmacol. 2011, 82(6), 658-668. Link to article.

Harrison RS, Ruiz-Gómez G, Hill TA, Chow SY, Shepherd NE, Lohman RJ, Abbenante G, Hoang HN, Fairlie DP. Novel Helix-Constrained Nociceptin Derivatives Are Potent Agonists and Antagonists of ERK Phosphorylation and Thermal Analgesia in Mice. J. Med. Chem. 2011, 53(23), 8400–8408. Link to article.

KleppeM, Soulier J, Asnafi V, Mentens N, Hornakova T, Knoops L, Constantinescu S, Sigaux F, Meijerink JP, Vandenberghe P, Tartaglia M, Foa R, Macintyre E, Haferlach T, Cools J. PTPN2 negatively regulates oncogenic JAK1 in T-cell acute lymphoblastic leukemia. Blood, 2011, 117(26), 7090-7098. Link to article.

Koole C, Wootten D, Simms J, Valant C, Miller LJ, Christopoulos A, Sexton PM. Polymorphism and ligand dependent changes in human glucagon-like peptide-1 receptor (GLP-1R) function: allosteric rescue of loss of function mutation. Mol Pharmacol. 2011, 80(3), 486-497.Link to article.

Leach K, Davey AE, Felder CC, Sexton PM, Christopoulos A. The role of transmembrane domain 3 (TMIII) in the actions of orthosteric, allosteric and atypical agonists of the M4 muscarinic acetylcholine receptor. Mol. Pharmacol. 2011, 79(5), 855-865. Link to article.

Lim J, Taoka B, Otte RD, Spencer K, Dinsmore CJ, Altman MD, Chan G, Rosenstein C, Sharma S, Su H-P, Szewczak AA, Xu L, Yin H, Zugay-Murphy J, Marshall CG, Young JR. Discovery of 1-Amino-5H-pyrido[4,3-b]indol-4-carboxamide Inhibitors of Janus Kinase 2 (JAK2) for the Treatment of Myeloproliferative Disorders. J. Med. Chem. 2011, 54(20):7334-49. Link to article.

Masiero M, Minuzzo S, Pusceddu I, Moserle L, Persano L, Agnusdei V, Tosello V, Basso G, Amadori A, Indraccolo S. Notch3-mediated regulation of MKP-1 levels promotes survival of T acute lymphoblastic leukemia cells. Leukemia. 2011, 25(4):588-598. Link to article.

Mole D, Gagliano T, Gentilin E, Tagliati F, Pasquali C, Ambrosio M-R, Pansini G, Uberti EC, Zatelli MC. Targeting protein kinase C by enzastaurin restrains proliferation and secretion in human pancreatic endocrine tumors. Endocr Relat Cancer. 201, 18, 439-450. Link to article.

Schenkel LB, Huang X, Cheng A, Deak HL, Doherty E, Emkey R, Gu Y, Gunaydin H, Kim JL, Lee J, Loberg R, Olivieri P, Pistillo J, Tang J, Wan Q, Wang HL, Wang SW, Wells MC, Wu B, Yu V, Liu L, Geuns-Meyer S. Discovery of potent and highly selective thienopyridine Janus kinase 2 inhibitors. J Med Chem. 201; 54(24), 8440-8450. Link to article.

Schinske KA, Nyati S, Khan AP, Williams TM, Johnson TD, Ross BD, Perez-Tomas R, Rehemtulla A. Novel Kinase Inhibitor of FADD Phosphorylation Chemosensitizes through the Inhibition of NF-κB. Mol cancer Ther. 2011, 10(10):1807-17. Link to article.

Shibata M-A, Iinuma M, Morimoto J, Kurose H, Akamatsu K, Okuno Y, Akao Y Otsuki Y. alpha-Mangostin extracted from the pericarp of the mangosteen (Garcinia mangostana Linn) reduces tumor growth and lymph node metastasis in an immunocompetent xenograft model of metastatic mammary cancer carrying a p53 mutation. BMC Medicine. 2011, 9, 69. Link to article.

Smith NJ, Ward RJ, Stoddart LA, Hudson BD, Kostenis E, Ulven T, Morris JC, Trankle C, Tikhonova IG, Adams DR, Milligan G. Extracellular Loop 2 Of The Free Fatty Acid Receptor 2 Mediates Allosterism Of A Phenylacetamide Ago-Allosteric Modulator. Mol Pharmacol. 2011, 80 (1), 163-173. Link to article.

Suratman S, Leach K, Sexton PM, FelderCC, Loiacono RE, Christopoulos A. Impact of species variability and “probe-dependence” on the detection and in vivo validation of allosteric modulation at the M4 muscarinic acetylcholine receptor. Brit. J. Pharmacol. 2011, 162(7), 1659-1670. Link to article.

Uitdehaag JC, Sünnen CM, van Doornmalen AM, de Rouw N, Oubrie A, Azevedo R, Ziebell M, Nickbarg E, Karstens WJ, Ruygrok S. Multidimensional Profiling of CSF1R Screening Hits and Inhibitors: Assessing Cellular Activity, Target Residence Time, and Selectivity in a Higher Throughput Way. J Biomol Screen. 2011, 16(9):1007-17. Link to article.

Van Allera GS , Carsona JD, Tangb W, Pengb H, Zhaob L, Copelanda RA, Tumminoa PJ, Luob L. Epigallocatechin gallate (EGCG), a major component of green tea, is a dual phosphoinositide-3-kinase/mTOR inhibitor. Biochem. Biophys. Res. Comm. 2011, 406(2):194-199. Link to article.

Ward RJ, Pediani JD, Milligan G. Ligand-induced internalisation of the orexin OX1 and cannabinoid CB1 receptors assessed via N-terminal SNAP and CLIP-tagging. Brit. J. Pharmacol. 2011, 162(6), 1439-1452. Link to article.

Wu C-H, Huang H-W, Huang S-M, Lin J-A, Yeh C-T, Yen G-C. AGE-induced interference of glucose uptake and transport as a possible cause of insulin resistance in adipocytes. J. Agric. Food Chem. 2011, 59 (14), 7978–7984. Link to article.

Zhao G, Li W, Chen D, Henry JR, Li H, Chen Z, Zia-Ebrahimi M, Bloem L, Zhai Y, Huss K, Peng S-B, McCann DJ. Novel, Selective Inhibitor of Fibroblast Growth Factor Receptors That Shows A Potent Broad-spectrum of Anti-tumor Activity in Several Tumor Xenograft Models. Mol Cancer Ther. 2011, 10:2200. Link to article.

Zou S, El-Hage N, Podhaizer EM, Knapp PE, Hauser KF. PTEN gene silencing prevents HIV-1 gp120IIIB-induced degeneration of striatal neurons. J. Neurovirol. 2011, 17(1), 41-49. Link to article.

Last updated: November 2011