Eduard Sergienko

Summary

Affiliation: The Burnham Institute
Country: USA

Publications

  1. pmc 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
  2. pmc 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
  3. doi request reprint 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. pmc 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. pmc Design, synthesis and evaluation of benzoisothiazolones as selective inhibitors of PHOSPHO1
    Yalda Bravo
    Cell Death and Survival Networks Research Program, NCI Designated Cancer Center, Sanford Burnham Medical Research Institute, 10901 North Torrey Pines Road, La Jolla, CA 92037, USA Conrad Prebys Center for Chemical Genomics, Sanford Burnham Medical Research Institute, 10901 North Torrey Pines Road, La Jolla, CA 92037, USA
    Bioorg Med Chem Lett 24:4308-11. 2014
  6. pmc 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
  7. pmc 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
  8. pmc 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. doi request reprint 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
  10. pmc Identification of a selective inhibitor of murine intestinal alkaline phosphatase (ML260) by concurrent ultra-high throughput screening against human and mouse isozymes
    Robert J Ardecky
    Sanford Burnham Medical Research Institute, La Jolla, CA 92037, United States
    Bioorg Med Chem Lett 24:1000-4. 2014

Collaborators

  • Jose Luis Millan
  • Thomas D Y Chung
  • Nicholas D P Cosford
  • Gregory P Roth
  • Anthony B Pinkerton
  • Li Yang
  • Matthew D Petroski
  • Andrei L Osterman
  • Jian Xu
  • Jonathan Kaunitz
  • Ekaterina V Bobkova
  • Ricardo G Correa
  • Hideki Hayashi
  • Fu Yue Zeng
  • Tomas Mustelin
  • Lutz Tautz
  • Russell Dahl
  • Ying Su
  • Brock Brown
  • Dayong Zhai
  • Chen Ting Ma
  • Yalda Bravo
  • Michael Hedrick
  • Layton H Smith
  • Justin Rascon
  • Stefan Vasile
  • John C Reed
  • Nam Gu Her
  • Irina A Rodionova
  • Robert J Ardecky
  • Stephanie M Stanford
  • Tina Kiffer-Moreira
  • Raveendra Panickar Dhanya
  • Patrick R Maloney
  • Paul Diaz
  • Derek Stonich
  • Michael Vicchiarelli
  • Sonoko Narisawa
  • Chih Wen Shu
  • Shyama Sidique
  • Kenneth W Yip
  • Khatereh Motamedchaboki
  • Yang Wei
  • Julia I Toth
  • Alexander E Aleshin
  • Eric J Rubin
  • Christopher P Locher
  • Harmon J Zuccola
  • Marat D Kazanov
  • Leonardo Sorci
  • Colin Farquharson
  • Santhi Ganji
  • Marc F Hoylaerts
  • Nunzio Bottini
  • Shenghua Shi
  • Caitlin E Karver
  • Rhushikesh A Kulkarni
  • Anita Forster
  • Carlton Gasior
  • Divya Krishnamurthy
  • Eveline Bruenger
  • Santhi Reddy Ganji
  • Craig Rosenstein
  • Fl├ívia Godoy Iano
  • Peter Teriete
  • Ian Pass
  • Anton Cheltsov
  • Logan M Walker
  • Amy M Barrios
  • Jiwen Zou
  • Pooi San Lee
  • Pasha Khan
  • Hung Nguyen
  • Kevin Nguyen
  • Xochella Chan
  • Paulo Godoi
  • Monika Milewski
  • Eliot Sugarman
  • Jena Diwan
  • Chaofang Jin
  • Arianna Mangravita Novo
  • Linda Li
  • Palak Gosalia
  • Alka Mehta
  • Andrew Hurder
  • Eigo Suyama
  • Hudson H Freeze
  • Renata Sano
  • Vandana Sharma
  • Charitha Madiraju

Detail Information

Publications17

  1. pmc 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...
  2. pmc 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
    ....
  3. doi request reprint 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. pmc 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. pmc Design, synthesis and evaluation of benzoisothiazolones as selective inhibitors of PHOSPHO1
    Yalda Bravo
    Cell Death and Survival Networks Research Program, NCI Designated Cancer Center, Sanford Burnham Medical Research Institute, 10901 North Torrey Pines Road, La Jolla, CA 92037, USA Conrad Prebys Center for Chemical Genomics, Sanford Burnham Medical Research Institute, 10901 North Torrey Pines Road, La Jolla, CA 92037, USA
    Bioorg Med Chem Lett 24:4308-11. 2014
    ..On the basis of its overall profile the benzoisothiazolone analogue 2q was selected as MLPCN probe ML086. ..
  6. pmc 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...
  7. pmc 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...
  8. pmc 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. doi request reprint 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
    ....
  10. pmc Identification of a selective inhibitor of murine intestinal alkaline phosphatase (ML260) by concurrent ultra-high throughput screening against human and mouse isozymes
    Robert J Ardecky
    Sanford Burnham Medical Research Institute, La Jolla, CA 92037, United States
    Bioorg Med Chem Lett 24:1000-4. 2014
    ..High throughput screening and subsequent SAR efforts generated a potent inhibitor of dIAP, ML260, with specificity for the Akp3-, compared to the Akp5- and Akp6-encoded mouse isozymes...
  11. pmc 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...
  12. pmc 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...
  13. pmc p97 Composition Changes Caused by Allosteric Inhibition Are Suppressed by an On-Target Mechanism that Increases the Enzyme's ATPase Activity
    Nam Gu Her
    Tumor Initiation and Maintenance Program, NCI Designated Cancer Center, Sanford Burnham Prebys Medical Discovery Institute, 10901 North Torrey Pines Road, La Jolla, CA 92037, USA
    Cell Chem Biol 23:517-28. 2016
    ..Collectively, these findings identify cofactor-p97 interactions sensitive to p97 inhibition and reveal a new on-target mechanism to suppress the cytotoxicity of NMS-873. ..
  14. pmc Mycobacterial nicotinate mononucleotide adenylyltransferase: structure, mechanism, and implications for drug discovery
    Irina A Rodionova
    From the Sanford Burnham Medical Research Institute, La Jolla, California 92037
    J Biol Chem 290:7693-706. 2015
    ..These findings point to a possible new strategy for designing inhibitors that lock the enzyme in the inactive over-closed conformation...
  15. pmc pCAP-based peptide substrates: the new tool in the box of tyrosine phosphatase assays
    Stephanie M Stanford
    Division of Cellular Biology, La Jolla Institute for Allergy and Immunology, La Jolla, CA 92037, USA
    Methods 65:165-74. 2014
    ..Finally the use of pCAP can expand the range of phosphatase assays, facilitating the investigation of multiphosphorylated peptides and providing an in-gel assay for phosphatase activity. ..
  16. pmc 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;..
  17. doi request reprint 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...