Adam B Weinglass

Summary

Affiliation: Merck Research Laboratories
Country: USA

Publications

  1. ncbi A high-capacity membrane potential FRET-based assay for the sodium-coupled glucose co-transporter SGLT1
    Adam B Weinglass
    Department of Ion Channels, Merck Research Laboratories, Rahway, NJ 07065, USA
    Assay Drug Dev Technol 6:255-62. 2008
  2. ncbi Technologies for transporter drug discovery
    Adam B Weinglass
    Merck Research Laboratories, Department of Ion Channels, Rahway, New Jersey 07065, USA
    Channels (Austin) 2:312-21. 2008
  3. ncbi Extracellular loop C of NPC1L1 is important for binding to ezetimibe
    Adam B Weinglass
    Departments of Ion Channels, Medicinal Chemistry, and Pharmacology, Merck Research Laboratories, P O Box 2000, Rahway, NJ 07065, USA
    Proc Natl Acad Sci U S A 105:11140-5. 2008
  4. ncbi Madin-Darby canine kidney II cells: a pharmacologically validated system for NPC1L1-mediated cholesterol uptake
    Adam B Weinglass
    Department of Ion Channels, Merck Research Laboratories, P O Box 2000, Rahway, NJ 07065, USA
    Mol Pharmacol 73:1072-84. 2008
  5. ncbi ProTx-II, a selective inhibitor of NaV1.7 sodium channels, blocks action potential propagation in nociceptors
    William A Schmalhofer
    Department of Ion Channels, Merck Research Laboratories, Rahway, NJ 07065 0900, USA
    Mol Pharmacol 74:1476-84. 2008
  6. ncbi Characterization of Kir1.1 channels with the use of a radiolabeled derivative of tertiapin
    John P Felix
    Department of Ion Channels, Merck Research Laboratories, Post Office Box 2000, Rahway, New Jersey 07065, USA
    Biochemistry 45:10129-39. 2006
  7. ncbi Exploring the role of a unique carboxyl residue in EmrE by mass spectrometry
    Adam B Weinglass
    Howard Hughes Medical Institute, Department of Physiology, Molecular Biology Institute, University of California Los Angeles, 90095 1662, USA
    J Biol Chem 280:7487-92. 2005
  8. ncbi Sugar recognition by the lactose permease of Escherichia coli
    José Luis Vázquez-Ibar
    Department of Physiology and Microbiology, Molecular Biology Institute, Howard Hughes Medical Institute, Los Angeles, CA 90095 1662, USA
    J Biol Chem 279:49214-21. 2004
  9. ncbi In vitro synthesis of lactose permease to probe the mechanism of membrane insertion and folding
    Shushi Nagamori
    Howard Hughes Medical Institute and Departments of Physiology and Microbiology, Immunology, and Molecular Genetics, Molecular Biology Institute, UCLA, Los Angeles, California 90095-1662, USA
    J Biol Chem 278:14820-6. 2003
  10. ncbi Binding of enzyme IIAGlc, a component of the phosphoenolpyruvate:sugar phosphotransferase system, to the Escherichia coli lactose permease
    Melissa Sondej
    Howard Hughes Medical Institute, Department of Physiology, University of California Los Angeles, Los Angeles, California 90095 1662, USA
    Biochemistry 41:5556-65. 2002

Collaborators

Detail Information

Publications14

  1. ncbi A high-capacity membrane potential FRET-based assay for the sodium-coupled glucose co-transporter SGLT1
    Adam B Weinglass
    Department of Ion Channels, Merck Research Laboratories, Rahway, NJ 07065, USA
    Assay Drug Dev Technol 6:255-62. 2008
    ....
  2. ncbi Technologies for transporter drug discovery
    Adam B Weinglass
    Merck Research Laboratories, Department of Ion Channels, Rahway, New Jersey 07065, USA
    Channels (Austin) 2:312-21. 2008
    ..This review provides an update on potential transporter targets and evaluates the impact of available technologies to enable transporter screening, lead optimization and assessment of pharmacokinetics...
  3. ncbi Extracellular loop C of NPC1L1 is important for binding to ezetimibe
    Adam B Weinglass
    Departments of Ion Channels, Medicinal Chemistry, and Pharmacology, Merck Research Laboratories, P O Box 2000, Rahway, NJ 07065, USA
    Proc Natl Acad Sci U S A 105:11140-5. 2008
    ..Specifically, EZE binding to an extracellular site distinct from where cholesterol binds prevents conformational changes in NPC1L1 that are necessary for the translocation of cholesterol across the membrane...
  4. ncbi Madin-Darby canine kidney II cells: a pharmacologically validated system for NPC1L1-mediated cholesterol uptake
    Adam B Weinglass
    Department of Ion Channels, Merck Research Laboratories, P O Box 2000, Rahway, NJ 07065, USA
    Mol Pharmacol 73:1072-84. 2008
    ..From a mechanistic standpoint, these observations support the contention that EZE analogs and cholesterol share the same/overlapping binding site(s) or are tightly coupled through allosteric interactions...
  5. ncbi ProTx-II, a selective inhibitor of NaV1.7 sodium channels, blocks action potential propagation in nociceptors
    William A Schmalhofer
    Department of Ion Channels, Merck Research Laboratories, Rahway, NJ 07065 0900, USA
    Mol Pharmacol 74:1476-84. 2008
    ..Thus, the (125)I-ProTx-II binding assay, described here, offers a new tool in the search for novel Na(V)1.7-selective blockers...
  6. ncbi Characterization of Kir1.1 channels with the use of a radiolabeled derivative of tertiapin
    John P Felix
    Department of Ion Channels, Merck Research Laboratories, Post Office Box 2000, Rahway, New Jersey 07065, USA
    Biochemistry 45:10129-39. 2006
    ..1 channels and suggest its utility for identifying other Kir channel modulators...
  7. ncbi Exploring the role of a unique carboxyl residue in EmrE by mass spectrometry
    Adam B Weinglass
    Howard Hughes Medical Institute, Department of Physiology, Molecular Biology Institute, University of California Los Angeles, 90095 1662, USA
    J Biol Chem 280:7487-92. 2005
    ..Taken together with other biochemical data, the findings support a "time sharing" mechanism in which both Glu-14 residues in a dimer are involved in tetraphenylphosphonium and H(+) binding...
  8. ncbi Sugar recognition by the lactose permease of Escherichia coli
    José Luis Vázquez-Ibar
    Department of Physiology and Microbiology, Molecular Biology Institute, Howard Hughes Medical Institute, Los Angeles, CA 90095 1662, USA
    J Biol Chem 279:49214-21. 2004
    ....
  9. ncbi In vitro synthesis of lactose permease to probe the mechanism of membrane insertion and folding
    Shushi Nagamori
    Howard Hughes Medical Institute and Departments of Physiology and Microbiology, Immunology, and Molecular Genetics, Molecular Biology Institute, UCLA, Los Angeles, California 90095-1662, USA
    J Biol Chem 278:14820-6. 2003
    ..Furthermore, there is synergism between N(6) and the C-terminal half of permease during assembly, as opposed to assembly of the two halves as independent domains...
  10. ncbi Binding of enzyme IIAGlc, a component of the phosphoenolpyruvate:sugar phosphotransferase system, to the Escherichia coli lactose permease
    Melissa Sondej
    Howard Hughes Medical Institute, Department of Physiology, University of California Los Angeles, Los Angeles, California 90095 1662, USA
    Biochemistry 41:5556-65. 2002
    ....
  11. ncbi Manipulating conformational equilibria in the lactose permease of Escherichia coli
    Adam B Weinglass
    Howard Hughes Medical Institute, Department of Physiology, Molecular Biology Institute, Los Angeles, CA 90095 1662, USA
    J Mol Biol 315:561-71. 2002
    ..When the two sets of mutants are combined, the equilibrium between outwardly and inwardly facing conformations and thus protonation and H(+) transfer are restored...
  12. ncbi Integrating mass spectrometry into membrane protein drug discovery
    Adam B Weinglass
    Howard Hughes Medical Institute, Departments of Physiology and Microbiology and Molecular Genetics Molecular Biology Institute, University of California Los Angeles, Los Angeles, CA 90095 1662, USA
    Curr Opin Drug Discov Devel 7:589-99. 2004
    ....
  13. ncbi Elucidation of substrate binding interactions in a membrane transport protein by mass spectrometry
    Adam B Weinglass
    Department of Physiology, Molecular Biology Institute, University of California Los Angeles, Los Angeles, CA 90095 1662, USA
    EMBO J 22:1467-77. 2003
    ..The approach demonstrates that mass spectrometry can provide a powerful means of analyzing ligand interactions with integral membrane proteins...