Lusong Luo

Summary

Affiliation: GlaxoSmithKline Research and Development
Country: USA

Publications

  1. ncbi Epigallocatechin gallate (EGCG), a major component of green tea, is a dual phosphoinositide-3-kinase/mTOR inhibitor
    Glenn S Van Aller
    Department of Cancer Research, GlaxoSmithKline, Collegeville, PA 19426, USA
    Biochem Biophys Res Commun 406:194-9. 2011
  2. ncbi Characterization of PI3K class IA isoforms with regulatory subunit p55alpha using a scintillation proximity assay
    Glenn S Van Aller
    Department of Enzymology and Mechanistic Pharmacology, Oncology CEDD, GlaxoSmithKline, Collegeville, PA 19426, USA
    Anal Biochem 383:311-5. 2008
  3. ncbi Biochemical characterization of human HIF hydroxylases using HIF protein substrates that contain all three hydroxylation sites
    Melissa B Pappalardi
    Department of Cancer Research, GlaxoSmithKline, Collegeville, PA 19426, USA
    Biochem J 436:363-9. 2011
  4. ncbi Effects of oncogenic p110alpha subunit mutations on the lipid kinase activity of phosphoinositide 3-kinase
    Jeffrey D Carson
    Department of Enzymology and Mechanistic Pharmacology, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, PA 19426, USA
    Biochem J 409:519-24. 2008
  5. ncbi Biochemical characterization of human prolyl hydroxylase domain protein 2 variants associated with erythrocytosis
    Melissa B Pappalardi
    Department of Enzymology and Mechanistic Pharmacology, Oncology CEDD, GlaxoSmithKline, Collegeville, Pennsylvania 19426, USA
    Biochemistry 47:11165-7. 2008
  6. ncbi Conformation-dependent ligand regulation of ATP hydrolysis by human KSP: activation of basal hydrolysis and inhibition of microtubule-stimulated hydrolysis by a single, small molecule modulator
    Lusong Luo
    Department of Enzymology and Mechanistic Pharmacology, GlaxoSmithKline, Collegeville, Pennsylvania 19426, USA
    J Am Chem Soc 130:7584-91. 2008
  7. ncbi ATP-competitive inhibitors of the mitotic kinesin KSP that function via an allosteric mechanism
    Lusong Luo
    Department of Enzymology and Mechanistic Pharmacology, Oncology CEDD, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA
    Nat Chem Biol 3:722-6. 2007
  8. ncbi Characterization of an exosite binding inhibitor of matrix metalloproteinase 13
    Lata T Gooljarsingh
    Department of Enzymology and Mechanistic Pharmacology, GlaxoSmithKline Pharmaceuticals, Collegeville, Pennsylvania 19426, USA
    Protein Sci 17:66-71. 2008
  9. ncbi Novel ATP-competitive kinesin spindle protein inhibitors
    Cynthia A Parrish
    Department of Medicinal Chemistry, Oncology Center of Excellence for Drug Discovery, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA
    J Med Chem 50:4939-52. 2007
  10. ncbi Mechanism of inhibition of human KSP by monastrol: insights from kinetic analysis and the effect of ionic strength on KSP inhibition
    Lusong Luo
    Department of Enzymology and Mechanistic Pharmacology, MMPD CEDD, GlaxoSmithKline, Collegeville, Pennsylvania 19426, USA
    Biochemistry 43:15258-66. 2004

Collaborators

Detail Information

Publications13

  1. ncbi Epigallocatechin gallate (EGCG), a major component of green tea, is a dual phosphoinositide-3-kinase/mTOR inhibitor
    Glenn S Van Aller
    Department of Cancer Research, GlaxoSmithKline, Collegeville, PA 19426, USA
    Biochem Biophys Res Commun 406:194-9. 2011
    ..Our results suggest another important molecular mechanism for the anticancer activities of EGCG...
  2. ncbi Characterization of PI3K class IA isoforms with regulatory subunit p55alpha using a scintillation proximity assay
    Glenn S Van Aller
    Department of Enzymology and Mechanistic Pharmacology, Oncology CEDD, GlaxoSmithKline, Collegeville, PA 19426, USA
    Anal Biochem 383:311-5. 2008
    ..The simple, inexpensive, sensitive high-throughput nature of the SPA format has advanced our knowledge of isoform-specific enzymology and will facilitate the discovery of novel PI3K inhibitors...
  3. ncbi Biochemical characterization of human HIF hydroxylases using HIF protein substrates that contain all three hydroxylation sites
    Melissa B Pappalardi
    Department of Cancer Research, GlaxoSmithKline, Collegeville, PA 19426, USA
    Biochem J 436:363-9. 2011
    ..In addition, steady-state kinetic analyses show differential substrate selectivity for HIF and α-KG in reference to the three PHD isoforms and FIH...
  4. ncbi Effects of oncogenic p110alpha subunit mutations on the lipid kinase activity of phosphoinositide 3-kinase
    Jeffrey D Carson
    Department of Enzymology and Mechanistic Pharmacology, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, PA 19426, USA
    Biochem J 409:519-24. 2008
    ....
  5. ncbi Biochemical characterization of human prolyl hydroxylase domain protein 2 variants associated with erythrocytosis
    Melissa B Pappalardi
    Department of Enzymology and Mechanistic Pharmacology, Oncology CEDD, GlaxoSmithKline, Collegeville, Pennsylvania 19426, USA
    Biochemistry 47:11165-7. 2008
    ....
  6. ncbi Conformation-dependent ligand regulation of ATP hydrolysis by human KSP: activation of basal hydrolysis and inhibition of microtubule-stimulated hydrolysis by a single, small molecule modulator
    Lusong Luo
    Department of Enzymology and Mechanistic Pharmacology, GlaxoSmithKline, Collegeville, Pennsylvania 19426, USA
    J Am Chem Soc 130:7584-91. 2008
    ..Rather, this compound acts by driving a conformational change in the KSP motor domain and disrupts productive ATP turnover stimulated by MT. These findings provide a novel mechanism for targeting KSP and perhaps other mitotic kinesins...
  7. ncbi ATP-competitive inhibitors of the mitotic kinesin KSP that function via an allosteric mechanism
    Lusong Luo
    Department of Enzymology and Mechanistic Pharmacology, Oncology CEDD, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA
    Nat Chem Biol 3:722-6. 2007
    ..Cumulative data from generation of resistant cells, site-directed mutagenesis and photo-affinity labeling suggest that they compete with ATP binding via a novel allosteric mechanism...
  8. ncbi Characterization of an exosite binding inhibitor of matrix metalloproteinase 13
    Lata T Gooljarsingh
    Department of Enzymology and Mechanistic Pharmacology, GlaxoSmithKline Pharmaceuticals, Collegeville, Pennsylvania 19426, USA
    Protein Sci 17:66-71. 2008
    ..These studies elucidate the steric requirement for compounds that fit exclusively into the active site, a mandate for generating highly selective MMP13 inhibitors...
  9. ncbi Novel ATP-competitive kinesin spindle protein inhibitors
    Cynthia A Parrish
    Department of Medicinal Chemistry, Oncology Center of Excellence for Drug Discovery, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA
    J Med Chem 50:4939-52. 2007
    ....
  10. ncbi Mechanism of inhibition of human KSP by monastrol: insights from kinetic analysis and the effect of ionic strength on KSP inhibition
    Lusong Luo
    Department of Enzymology and Mechanistic Pharmacology, MMPD CEDD, GlaxoSmithKline, Collegeville, Pennsylvania 19426, USA
    Biochemistry 43:15258-66. 2004
    ....
  11. ncbi Demonstration of a genetic therapeutic index for tumors expressing oncogenic BRAF by the kinase inhibitor SB-590885
    Alastair J King
    Department of Oncology, MMPD CEDD, GlaxoSmithKline, Collegeville, Pennsylvania 19426, USA
    Cancer Res 66:11100-5. 2006
    ....
  12. ncbi An assay for Fe(II)/2-oxoglutarate-dependent dioxygenases by enzyme-coupled detection of succinate formation
    Lusong Luo
    Department of Enzymology and Mechanistic Pharmacology, MMPD CEDD, GlaxoSmithKline, Collegeville, PA 19426, USA
    Anal Biochem 353:69-74. 2006
    ..This assay is amenable to miniaturization and easily adapted to a format suitable for high-throughput screening; thus, it will be a valuable tool to study Fe(II)/2-oxoglutarate-dependent dioxygenases...
  13. ncbi A method for determining intracellular concentrations of enzyme substrates from a combination of competitive inhibition and mutagenesis studies
    Robert A Copeland
    Department of Enzymology and Mechanistic Pharmacology and Department of Oncology Biology, GlaxoSmithKline, 1250 S. Collegeville Road, Collegeville, PA 19426, USA
    Anal Biochem 337:351-3. 2005