Now showing items 1-4 of 4

    • 8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors. 

      Bavetsias, V; Lanigan, RM; Ruda, GF; Atrash, B; McLaughlin, MG; Tumber, A; Mok, NY; Le Bihan, Y-V; Dempster, S; Boxall, KJ; Jeganathan, F; Hatch, SB; Savitsky, P; Velupillai, S; Krojer, T; England, KS; Sejberg, J; Thai, C; Donovan, A; Pal, A; Scozzafava, G; Bennett, JM; Kawamura, A; Johansson, C; Szykowska, A; Gileadi, C; Burgess-Brown, NA; von Delft, F; Oppermann, U; Walters, Z; Shipley, J; Raynaud, FI; Westaway, SM; Prinjha, RK; Fedorov, O; Burke, R; Schofield, CJ; Westwood, IM; Bountra, C; Müller, S; van Montfort, RLM; Brennan, PE; Blagg, J (2016-02)
      We report the discovery of N-substituted 4-(pyridin-2-yl)thiazole-2-amine derivatives and their subsequent optimization, guided by structure-based design, to give 8-(1H-pyrazol-3-yl)pyrido[3,4-d]pyrimidin-4(3H)-ones, a ...
    • International Ring Trial of a High Resolution Targeted Metabolomics and Lipidomics Platform for Serum and Plasma Analysis. 

      Thompson, JW; Adams, KJ; Adamski, J; Asad, Y; Borts, D; Bowden, JA; Byram, G; Dang, V; Dunn, WB; Fernandez, F; Fiehn, O; Gaul, DA; Hühmer, AF; Kalli, A; Koal, T; Koeniger, S; Mandal, R; Meier, F; Naser, FJ; O'Neil, D; Pal, A; Patti, GJ; Pham-Tuan, H; Prehn, C; Raynaud, FI; Shen, T; Southam, AD; St John-Williams, L; Sulek, K; Vasilopoulou, CG; Viant, M; Winder, CL; Wishart, D; Zhang, L; Zheng, J; Moseley, MA (2019-11-08)
      A challenge facing metabolomics in the analysis of large human cohorts is the cross-laboratory comparability of quantitative metabolomics measurements. In this study, 14 laboratories analyzed various blood specimens using ...
    • Metabolomic changes of the multi (-AGC-) kinase inhibitor AT13148 in cells, mice and patients are associated with NOS regulation. 

      Pal, A; Asad, Y; Ruddle, R; Henley, AT; Swales, K; Decordova, S; Eccles, SA; Collins, I; Garrett, MD; De Bono, J; Banerji, U; Raynaud, FI (2020-04-13)
      INTRODUCTION:To generate biomarkers of target engagement or predictive response for multi-target drugs is challenging. One such compound is the multi-AGC kinase inhibitor AT13148. Metabolic signatures of selective signal ...
    • Modulation of Plasma Metabolite Biomarkers of the MAPK Pathway with MEK Inhibitor RO4987655: Pharmacodynamic and Predictive Potential in Metastatic Melanoma. 

      Ang, JE; Pal, A; Asad, YJ; Henley, AT; Valenti, M; Box, G; de Haven Brandon, A; Revell, VL; Skene, DJ; Venturi, M; Rueger, R; Meresse, V; Eccles, SA; de Bono, JS; Kaye, SB; Workman, P; Banerji, U; Raynaud, FI (2017-10)
      MAPK pathway activation is frequently observed in human malignancies, including melanoma, and is associated with sensitivity to MEK inhibition and changes in cellular metabolism. Using quantitative mass spectrometry-based ...