Eduard Sergienko

Summary

Affiliation: The Burnham Institute
Country: USA

Publications

  1. ncbi Identification and characterization of novel tissue-nonspecific alkaline phosphatase inhibitors with diverse modes of action
    Eduard Sergienko
    Conrad Prebys Center for Chemical Genomics, Burnham Institute for Medical Research, La Jolla, California 92037, USA
    J Biomol Screen 14:824-37. 2009
  2. ncbi High-throughput screening of tissue-nonspecific alkaline phosphatase for identification of effectors with diverse modes of action
    Eduard A Sergienko
    Conrad Prebys Center for Chemical Genomics, Sanford Burnham Medical Research Institute, La Jolla, California, USA
    Nat Protoc 5:1431-9. 2010
  3. ncbi High-throughput fluorescence polarization assay for chemical library screening against anti-apoptotic Bcl-2 family member Bfl-1
    Dayong Zhai
    Sanford Burnham Medical Research Institute, Program on Apoptosis and Cell Death Research, La Jolla, CA 92037, USA
    J Biomol Screen 17:350-60. 2012
  4. ncbi Design and synthesis of pyrazole derivatives as potent and selective inhibitors of tissue-nonspecific alkaline phosphatase (TNAP)
    Shyama Sidique
    Burnham Center for Chemical Genomics, Burnham Institute for Medical Research, La Jolla, CA 92037, USA
    Bioorg Med Chem Lett 19:222-5. 2009
  5. ncbi Inhibition of hematopoietic protein tyrosine phosphatase augments and prolongs ERK1/2 and p38 activation
    Eduard Sergienko
    Infectious and Inflammatory Disease Center, Sanford Burnham Medical Research Institute, La Jolla, California 92037, United States
    ACS Chem Biol 7:367-77. 2012
  6. ncbi Assay format as a critical success factor for identification of novel inhibitor chemotypes of tissue-nonspecific alkaline phosphatase from high-throughput screening
    Thomas D Y Chung
    Conrad Prebys Center for Chemical Genomics, Sanford Burnham Medical Research Institute, La Jolla, CA 92037, USA
    Molecules 15:3010-37. 2010
  7. ncbi High-throughput fluorescence assay for small-molecule inhibitors of autophagins/Atg4
    Chih Wen Shu
    Sanford Burnham Medical Research Institute, Program on Apoptosis and Cell Death Research, and Conrad Prebys Center for Chemical Genomics, La Jolla, CA 92037, USA
    J Biomol Screen 16:174-82. 2011
  8. ncbi Potent, selective, and orally available benzoisothiazolone phosphomannose isomerase inhibitors as probes for congenital disorder of glycosylation Ia
    Russell Dahl
    Apoptosis and Cell Death Research Program, Conrad Prebys Center for Chemical Genomics, Sanford Burnham Medical Research Institute, 10901 North Torrey Pines Road, La Jolla, California 92037, United States
    J Med Chem 54:3661-8. 2011
  9. ncbi Discovery of 4-oxo-6-((pyrimidin-2-ylthio)methyl)-4H-pyran-3-yl 4-nitrobenzoate (ML221) as a functional antagonist of the apelin (APJ) receptor
    Patrick R Maloney
    Conrad Prebys Center for Chemical Genomics, Sanford Burnham Medical Research Institute, 6400 Sanger Road, Orlando, FL 32827, USA
    Bioorg Med Chem Lett 22:6656-60. 2012
  10. ncbi Discovery and characterization of 2-aminobenzimidazole derivatives as selective NOD1 inhibitors
    Ricardo G Correa
    Sanford Burnham Medical Research Institute, La Jolla, CA 92037, USA
    Chem Biol 18:825-32. 2011

Collaborators

  • Thomas D Y Chung
  • Jose Luis Millan
  • Nicholas D P Cosford
  • Li Yang
  • Hideki Hayashi
  • Anthony B Pinkerton
  • Fu Yue Zeng
  • Lutz Tautz
  • Tomas Mustelin
  • Ekaterina V Bobkova
  • Dayong Zhai
  • Ying Su
  • Brock Brown
  • John C Reed
  • Russell Dahl
  • Patrick R Maloney
  • Michael Hedrick
  • Paul Diaz
  • Derek Stonich
  • Justin Rascon
  • Layton H Smith
  • Michael Vicchiarelli
  • Gregory P Roth
  • Chih Wen Shu
  • Ricardo G Correa
  • Stefan Vasile
  • Motti Gerlic
  • Shyama Sidique
  • Kenneth W Yip
  • Andrew Hurder
  • Monika Milewski
  • Eigo Suyama
  • Alka Mehta
  • Jena Diwan
  • Palak Gosalia
  • Hung Nguyen
  • Kevin Nguyen
  • Chaofang Jin
  • Linda Li
  • Arianna Mangravita Novo
  • Pasha Khan
  • Eliot Sugarman
  • Xochella Chan
  • Paulo Godoi
  • Vandana Sharma
  • Yalda Bravo
  • Paul W Diaz
  • Mie Ichikawa
  • Arianna Mangravita-Novo
  • Kate Welsh
  • Roberto Spreafico
  • Salvatore Albani
  • Nadav Askari
  • Charitha Madiraju
  • Pasha M Khan
  • Gavin Magnuson
  • Hudson H Freeze
  • Renata Sano
  • Raveendra Panickar Dhanya
  • Sonoko Narisawa
  • Robert Ardecky
  • Arnold Satterthwait
  • Jason F Cellitti
  • Paulo H C Godoi
  • Xochella Garcia
  • Ya Chen
  • Michael Cuddy

Detail Information

Publications12

  1. ncbi Identification and characterization of novel tissue-nonspecific alkaline phosphatase inhibitors with diverse modes of action
    Eduard Sergienko
    Conrad Prebys Center for Chemical Genomics, Burnham Institute for Medical Research, La Jolla, California 92037, USA
    J Biomol Screen 14:824-37. 2009
    ....
  2. ncbi High-throughput screening of tissue-nonspecific alkaline phosphatase for identification of effectors with diverse modes of action
    Eduard A Sergienko
    Conrad Prebys Center for Chemical Genomics, Sanford Burnham Medical Research Institute, La Jolla, California, USA
    Nat Protoc 5:1431-9. 2010
    ..This protocol provides a method of screening TNAP that is 1,000-fold more sensitive and 10-fold faster than a conventional colorimetric assay with p-nitrophenyl phosphate...
  3. ncbi High-throughput fluorescence polarization assay for chemical library screening against anti-apoptotic Bcl-2 family member Bfl-1
    Dayong Zhai
    Sanford Burnham Medical Research Institute, Program on Apoptosis and Cell Death Research, La Jolla, CA 92037, USA
    J Biomol Screen 17:350-60. 2012
    ..Collectively, these findings demonstrate the feasibility of using the HTS assay for discovery of selective chemical inhibitors of Bfl-1...
  4. ncbi Design and synthesis of pyrazole derivatives as potent and selective inhibitors of tissue-nonspecific alkaline phosphatase (TNAP)
    Shyama Sidique
    Burnham Center for Chemical Genomics, Burnham Institute for Medical Research, La Jolla, CA 92037, USA
    Bioorg Med Chem Lett 19:222-5. 2009
    ..A representative of the series was characterized in kinetic studies and determined to have a mode of inhibition not previously observed for TNAP inhibitors...
  5. ncbi Inhibition of hematopoietic protein tyrosine phosphatase augments and prolongs ERK1/2 and p38 activation
    Eduard Sergienko
    Infectious and Inflammatory Disease Center, Sanford Burnham Medical Research Institute, La Jolla, California 92037, United States
    ACS Chem Biol 7:367-77. 2012
    ..Our results warrant future studies with this probe compound that may establish HePTP as a new drug target for acute leukemic conditions...
  6. ncbi Assay format as a critical success factor for identification of novel inhibitor chemotypes of tissue-nonspecific alkaline phosphatase from high-throughput screening
    Thomas D Y Chung
    Conrad Prebys Center for Chemical Genomics, Sanford Burnham Medical Research Institute, La Jolla, CA 92037, USA
    Molecules 15:3010-37. 2010
    ..This illustrates the underappreciated impact of the underlying fundamental assay configuration on screening success, beyond mere signal generation and detection formats...
  7. ncbi High-throughput fluorescence assay for small-molecule inhibitors of autophagins/Atg4
    Chih Wen Shu
    Sanford Burnham Medical Research Institute, Program on Apoptosis and Cell Death Research, and Conrad Prebys Center for Chemical Genomics, La Jolla, CA 92037, USA
    J Biomol Screen 16:174-82. 2011
    ....
  8. ncbi Potent, selective, and orally available benzoisothiazolone phosphomannose isomerase inhibitors as probes for congenital disorder of glycosylation Ia
    Russell Dahl
    Apoptosis and Cell Death Research Program, Conrad Prebys Center for Chemical Genomics, Sanford Burnham Medical Research Institute, 10901 North Torrey Pines Road, La Jolla, California 92037, United States
    J Med Chem 54:3661-8. 2011
    ..The pharmacokinetic profile of a representative of this series (compound 19; ML089) was also assessed, demonstrating the potential of this series for in vivo efficacy when dosed orally in disease models...
  9. ncbi Discovery of 4-oxo-6-((pyrimidin-2-ylthio)methyl)-4H-pyran-3-yl 4-nitrobenzoate (ML221) as a functional antagonist of the apelin (APJ) receptor
    Patrick R Maloney
    Conrad Prebys Center for Chemical Genomics, Sanford Burnham Medical Research Institute, 6400 Sanger Road, Orlando, FL 32827, USA
    Bioorg Med Chem Lett 22:6656-60. 2012
    ..The synthetic methodology, development of structure-activity relationship (SAR), and initial in vitro pharmacologic characterization are also presented...
  10. ncbi Discovery and characterization of 2-aminobenzimidazole derivatives as selective NOD1 inhibitors
    Ricardo G Correa
    Sanford Burnham Medical Research Institute, La Jolla, CA 92037, USA
    Chem Biol 18:825-32. 2011
    ..Altogether, this inaugural class of inhibitors provides chemical probes for interrogating mechanisms regulating NOD1 activity and tools for exploring the roles of NOD1 in various infectious and inflammatory diseases...
  11. ncbi Versatile assays for high throughput screening for activators or inhibitors of intracellular proteases and their cellular regulators
    Hideki Hayashi
    Burnham Institute for Medical Research, La Jolla, California, USA
    PLoS ONE 4:e7655. 2009
    ..methods #entitystartx00026;..
  12. ncbi A TR3/Nur77 peptide-based high-throughput fluorescence polarization screen for small molecule Bcl-B inhibitors
    Kenneth W Yip
    Burnham Institute for Medical Research, La Jolla, California 92037, USA
    J Biomol Screen 13:665-73. 2008
    ..Experiments using Bcl-B overexpressing HeLa cells demonstrated that this compound induced Bcl-B-dependent cell death. The current FPA represents a screen that can identify noncanonical inhibitors of Bcl-2-family proteins...