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Author Details

Eduard Sergienko
Cancer Center, Sanford Burnham Prebys Medical Discovery Institute
1992
77
29
PMIDPaper TitleJournal TitlePublished Year
36837653Mechanism of Action and Structure-Activity Relationships of Tetracyclic Small Molecules Acting as Universal Positive Allosteric Modulators of the Cholecystokinin Receptor.Membranes (Basel)2023
37406115Melanoma-intrinsic NR2F6 activity regulates antitumor immunity.Sci Adv2023
36050469NRF2 mediates melanoma addiction to GCDH by modulating apoptotic signalling.Nat Cell Biol2022
35850480Screening for positive allosteric modulators of cholecystokinin type 1 receptor potentially useful for management of obesity.SLAS Discov2022
32749201Development of a Testing Funnel for Identification of Small-Molecule Modulators Targeting Secretin Receptors.SLAS Discov2021
33545115Discovery of small molecule positive allosteric modulators of the secretin receptor.Biochem Pharmacol2021
33887438Discovery of 1-[2-(1-methyl-1H-pyrazol-5-yl)-[1,2,4]triazolo[1,5-a]pyridin-6-yl]-3-(pyridin-4-ylmethyl)urea as a potent NAMPT (nicotinamide phosphoribosyltransferase) activator with attenuated CYP inhibition.Bioorg Med Chem Lett2021
33798699Optimization of a urea-containing series of nicotinamide phosphoribosyltransferase (NAMPT) activators.Bioorg Med Chem Lett2021
34950108Discovery of a Positive Allosteric Modulator of Cholecystokinin Action at CCK1R in Normal and Elevated Cholesterol.Front Endocrinol (Lausanne)2021
33414172Serine-Threonine Kinase TAO3-Mediated Trafficking of Endosomes Containing the Invadopodia Scaffold TKS5α Promotes Cancer Invasion and Tumor Growth.Cancer Res2021
31575656Molecular Inhibitor of QSOX1 Suppresses Tumor Growth <i>In Vivo</i>.Mol Cancer Ther2020
31953320A cellular target engagement assay for the characterization of SHP2 (PTPN11) phosphatase inhibitors.J Biol Chem2020
30581133Allosteric Inhibition of Ubiquitin-like Modifications by a Class of Inhibitor of SUMO-Activating Enzyme.Cell Chem Biol2019
30771432Identification and characterization of small molecule inhibitors of the ubiquitin ligases Siah1/2 in melanoma and prostate cancer cells.Cancer Lett2019
30969758Novel Antimycobacterial Compounds Suppress NAD Biogenesis by Targeting a Unique Pocket of NaMN Adenylyltransferase.ACS Chem Biol2019
29174347Discovery of 5-((5-chloro-2-methoxyphenyl)sulfonamido)nicotinamide (SBI-425), a potent and orally bioavailable tissue-nonspecific alkaline phosphatase (TNAP) inhibitor.Bioorg Med Chem Lett2018
28543567TGR5 contributes to hepatic cystogenesis in rodents with polycystic liver diseases through cyclic adenosine monophosphate/Gαs signaling.Hepatology2017
28244987Capzimin is a potent and specific inhibitor of proteasome isopeptidase Rpn11.Nat Chem Biol2017
28592560Ectopic calcification in pseudoxanthoma elasticum responds to inhibition of tissue-nonspecific alkaline phosphatase.Sci Transl Med2017
27105284p97 Composition Changes Caused by Allosteric Inhibition Are Suppressed by an On-Target Mechanism that Increases the Enzyme's ATPase Activity.Cell Chem Biol2016
27316992Time-Resolved Fluorescence Assays.Methods Mol Biol2016
25520375Dual-specificity phosphatase 3 deficiency or inhibition limits platelet activation and arterial thrombosis.Circulation2015
26158899Ebselen inhibits QSOX1 enzymatic activity and suppresses invasion of pancreatic and renal cancer cell lines.Oncotarget2015
26075913TRAIL-Based High Throughput Screening Reveals a Link between TRAIL-Mediated Apoptosis and Glutathione Reductase, a Key Component of Oxidative Stress Response.PLoS One2015
25631047Mycobacterial nicotinate mononucleotide adenylyltransferase: structure, mechanism, and implications for drug discovery.J Biol Chem2015
25719760Design of high-throughput screening assays and identification of a SUMO1-specific small molecule chemotype targeting the SUMO-interacting motif-binding surface.ACS Comb Sci2015
25428889Pathophysiological role of vascular smooth muscle alkaline phosphatase in medial artery calcification.J Bone Miner Res2015
23886911pCAP-based peptide substrates: the new tool in the box of tyrosine phosphatase assays.Methods2014
25124115Design, synthesis and evaluation of benzoisothiazolones as selective inhibitors of PHOSPHO1.Bioorg Med Chem Lett2014
24412070Identification of a selective inhibitor of murine intestinal alkaline phosphatase (ML260) by concurrent ultra-high throughput screening against human and mouse isozymes.Bioorg Med Chem Lett2014
23023104Identification and characterization of novel human glucose-6-phosphate dehydrogenase inhibitors.J Biomol Screen2013
23860657High-throughput screening for protein tyrosine phosphatase activity modulators.Methods Mol Biol2013
23860652Modulators of intestinal alkaline phosphatase.Methods Mol Biol2013
23860653New activity assays for ENPP1 with physiological substrates ATP and ADP.Methods Mol Biol2013
23860649A method for direct assessment of tissue-nonspecific alkaline phosphatase (TNAP) inhibitors in blood samples.Methods Mol Biol2013
23860645Phosphatase high-throughput screening assay design and selection.Methods Mol Biol2013
22156224High-throughput fluorescence polarization assay for chemical library screening against anti-apoptotic Bcl-2 family member Bfl-1.J Biomol Screen2012
23010269Discovery of 4-oxo-6-((pyrimidin-2-ylthio)methyl)-4H-pyran-3-yl 4-nitrobenzoate (ML221) as a functional antagonist of the apelin (APJ) receptor.Bioorg Med Chem Lett2012
22813531Discovery of a Plasmodium falciparum glucose-6-phosphate dehydrogenase 6-phosphogluconolactonase inhibitor (R,Z)-N-((1-ethylpyrrolidin-2-yl)methyl)-2-(2-fluorobenzylidene)-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazine-6-carboxamide (ML276) that reduces parasite growth in vitro.J Med Chem2012
22737280Discovery of Small Molecule Kappa Opioid Receptor Agonist and Antagonist Chemotypes through a HTS and Hit Refinement Strategy.ACS Chem Neurosci2012
22496096High-throughput screening for small-molecule inhibitors of plasmodium falciparum glucose-6-phosphate dehydrogenase 6-phosphogluconolactonase.J Biomol Screen2012
22070201Inhibition of hematopoietic protein tyrosine phosphatase augments and prolongs ERK1/2 and p38 activation.ACS Chem Biol2012
22034497TR-FRET-based high-throughput screening assay for identification of UBC13 inhibitors.J Biomol Screen2012
21245471High-throughput fluorescence assay for small-molecule inhibitors of autophagins/Atg4.J Biomol Screen2011
21802003Discovery and characterization of 2-aminobenzimidazole derivatives as selective NOD1 inhibitors.Chem Biol2011
21539312Potent, selective, and orally available benzoisothiazolone phosphomannose isomerase inhibitors as probes for congenital disorder of glycosylation Ia.J Med Chem2011
21503265Inhibition of the Hematopoietic Protein Tyrosine Phosphatase by Phenoxyacetic Acids.ACS Med Chem Lett2011
20031422Design and synthesis of selective inhibitors of placental alkaline phosphatase.Bioorg Med Chem2010
20933419Inhibition of Bfl-1 with N-aryl maleimides.Bioorg Med Chem Lett2010
20657462Assay format as a critical success factor for identification of novel inhibitor chemotypes of tissue-nonspecific alkaline phosphatase from high-throughput screening.Molecules2010
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Collaborators

Sanford Burnham Prebys Medical Discovery Institute
Co-authored papers 15
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Co-authored papers 14
Sanford Burnham Prebys Medical Discovery Institute
Co-authored papers 6
Cancer Center, Sanford Burnham Prebys Medical Discovery Institute
Co-authored papers 5
Chugai Pharmaceutical Co.
Co-authored papers 4
Sanford Burnham Prebys Medical Discovery Institute
Co-authored papers 3
Cancer Center, Sanford Burnham Prebys Medical Discovery Institute
Co-authored papers 3
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Co-authored papers 3
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Co-authored papers 2
Sanford Burnham Prebys Medical Discovery Institute
Co-authored papers 2
Co-authored papers 2
National Research Center for Preventive Medicine (NRCPM)
Co-authored papers 2
National Cancer Institute
Co-authored papers 2
Oregon Health and Science University
Co-authored papers 2
Mayo Clinic Arizona
Co-authored papers 2
University of California at San Diego
Co-authored papers 2
The Rockefeller University
Co-authored papers 2
Purdue University
Co-authored papers 2
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Oregon Health and Science University
Co-authored papers 1
Sungkyunkwan University
Co-authored papers 1
Institute for Data Science and Computing, University of Miami
Co-authored papers 1
Sanford Burnham Prebys Medical Discovery Institute
Co-authored papers 1
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University of British Columbia
Co-authored papers 1
Cancer Center, Sanford Burnham Prebys Medical Discovery Institute
Co-authored papers 1
Oregon Health & Science University, University of California Berkeley
Co-authored papers 1
Mayo Clinic Jacksonville
Co-authored papers 1
Ellen and Ronald Caplan Cancer Center, The Wistar Institute
Co-authored papers 1