E. Sergienko

J. Millán, E. Sergienko, W. C. O'Neill, 2015, Journal of bone and mineral research : the official journal of the American Society for Bone and Mineral Research.

TGR5 contributes to hepatic cystogenesis in rodents with polycystic liver diseases through cyclic adenosine monophosphate/Gαs signaling

N. LaRusso, T. Chung, E. Sergienko, 2017, Hepatology.

TGR 5 contributes to hepatic cystogenesis in rodents with polycystic liver diseases via cAMP / G α s signaling Short title : TGR 5 in hepatic cystogenesis

N. LaRusso, T. Chung, E. Sergienko, 2017 .

Catalytic acid-base groups in yeast pyruvate decarboxylase. 2. Insights into the specific roles of D28 and E477 from the rates and stereospecificity of formation of carboligase side products.

E. Sergienko, F. Jordan, 2001, Biochemistry.

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.

T. Chung, M. Hedrick, E. Sergienko, 2012, Bioorganic & medicinal chemistry letters.

Identification of a selective inhibitor of murine intestinal alkaline phosphatase (ML260) by concurrent ultra-high throughput screening against human and mouse isozymes.

T. Chung, Brock T Brown, M. Hedrick, 2014, Bioorganic & medicinal chemistry letters.

Molecular Inhibitor of QSOX1 Suppresses Tumor Growth In Vivo

D. Mukhopadhyay, D. Faigel, T. Ho, 2019, Molecular Cancer Therapeutics.

Table 1, Listing of all Assays and AIDs for this project

Susanne Heynen-Genel, Shenghua Shi, Thomas D.Y. Chung, 2010 .

Versatile Assays for High Throughput Screening for Activators or Inhibitors of Intracellular Proteases and Their Cellular Regulators

John Calvin Reed, H. Hayashi, E. Sergienko, 2009, PloS one.

Table 4, Probe and Analog Submissions to MLSMR (BioFocus DPI) for Gli-Sufu Antagonist ML340

Santhi Ganji, Ian Pass, Robert Ardecky, 2014 .

Small-molecule antagonists of Gli function

Tram A. Ngo, Jennifer K. T. Casabar, T. Chung, 2014 .

NRF2 mediates melanoma addiction to GCDH by modulating apoptotic signalling

E. Ruppin, E. Sergienko, Z. Ronai, 2022, Nature Cell Biology.

Functional Antagonists of EBI-2

M. Jackson, T. Chung, Brock T Brown, 2015 .

pCAP-based peptide substrates: the new tool in the box of tyrosine phosphatase assays.

N. Bottini, T. Chung, E. Sergienko, 2014, Methods.

High-throughput screening based identification of small molecule antagonists of integrin CD11b/CD18 ligand binding.

Brock T Brown, M. Hedrick, E. Sergienko, 2010, Biochemical and biophysical research communications.

Screening for Selective Ligands for GPR55 - Antagonists

M. Caron, T. Chung, M. Hedrick, 2011 .

Discovery of small molecule positive allosteric modulators of thesecretin receptor

E. Sergienko, L. Miller, Sirkku Pollari, 2021 .

Development of a Testing Funnel for Identification of Small-Molecule Modulators Targeting Secretin Receptors

Brock T Brown, E. Sergienko, L. Miller, 2020, SLAS discovery : advancing life sciences R & D.

Screening for positive allosteric modulators of cholecystokinin type 1 receptor potentially useful for management of obesity

E. Sergienko, L. Miller, K. Harikumar, 2022, SLAS discovery : advancing life sciences R & D.

Optimization of a Urea-containing Series of Nicotinamide Phosphoribosyltransferase (NAMPT) Activators.

M. Jackson, E. Sergienko, S. Gardell, 2021, Bioorganic & medicinal chemistry letters.

Discovery 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.

E. Sergienko, M. Yokoyama, S. Gardell, 2021, Bioorganic & medicinal chemistry letters.

High-Throughput Fluorescence Polarization Assay for Chemical Library Screening against Anti-Apoptotic Bcl-2 Family Member Bfl-1

John Calvin Reed, T. Chung, X. Chan, 2012, Journal of biomolecular screening.

DUSP3 Phosphatase Deficiency or Inhibition Limit Platelet Activation and Arterial Thrombosis Running title: Musumeci et al.; DUSP3, a new player in arterial thrombosis

T. Mustelin, T. Chung, E. Théâtre, 2014 .

Identification and Characterization of Novel Human Glucose-6-Phosphate Dehydrogenase Inhibitors

S. Rahlfs, K. Becker, M. Hedrick, 2013, Journal of biomolecular screening.

Table 1, SAR results generated using analogue-by-catalogue (ABC)

Layton H. Smith, Thomas D.Y. Chung, Eduard Sergienko, 2010 .

Ectopic calcification in pseudoxanthoma elasticum responds to inhibition of tissue-nonspecific alkaline phosphatase

E. Chew, H. Dietz, W. Gahl, 2017, Science Translational Medicine.

Spectroscopic evidence for participation of the 1',4'-imino tautomer of thiamin diphosphate in catalysis by yeast pyruvate decarboxylase.

Frank Jordan, Eduard Sergienko, Zhen Zhang, 2002, Bioorganic chemistry.

Design and synthesis of selective inhibitors of placental alkaline phosphatase.

T. Chung, J. Cashman, J. Millán, 2010, Bioorganic & medicinal chemistry.

Discovery 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.

Stefan Vasile, Eigo Suyama, Michael Vicchiarelli, 2012, Journal of medicinal chemistry.

Design and synthesis of pyrazole derivatives as potent and selective inhibitors of tissue-nonspecific alkaline phosphatase (TNAP).

Brock T Brown, J. Millán, E. Sergienko, 2009, Bioorganic & medicinal chemistry letters.

Structural and kinetic analysis of catalysis by a thiamin diphosphate-dependent enzyme, benzoylformate decarboxylase.

Frank Jordan, Asim K Bera, George L Kenyon, 2003, Biochemistry.

Catalytic acid-base groups in yeast pyruvate decarboxylase. 3. A steady-state kinetic model consistent with the behavior of both wild-type and variant enzymes at all relevant pH values.

E. Sergienko, F. Jordan, 2001, Biochemistry.

Catalytic acid-base groups in yeast pyruvate decarboxylase. 1. Site-directed mutagenesis and steady-state kinetic studies on the enzyme with the D28A, H114F, H115F, and E477Q substitutions.

E. Sergienko, K. Tittmann, F. Jordan, 2001, Biochemistry.

Assay Format as a Critical Success Factor for Identification of Novel Inhibitor Chemotypes of Tissue-Nonspecific Alkaline Phosphatase from High-Throughput Screening

T. Chung, J. Millán, E. Sergienko, 2010, Molecules.

Discovery of 5-((5-chloro-2-methoxyphenyl)sulfonamido)nicotinamide (SBI-425), a potent and orally bioavailable tissue-nonspecific alkaline phosphatase (TNAP) inhibitor.

M. Jackson, J. Millán, E. Sergienko, 2018, Bioorganic & medicinal chemistry letters.

Discovery and validation of a series of aryl sulfonamides as selective inhibitors of tissue-nonspecific alkaline phosphatase (TNAP).

Brock T Brown, J. Millán, E. Sergienko, 2009, Journal of medicinal chemistry.

Identification and Characterization of Novel Tissue-Nonspecific Alkaline Phosphatase Inhibitors with Diverse Modes of Action

X. Chan, Brock T Brown, J. Millán, 2009, Journal of biomolecular screening.

Design, synthesis and evaluation of benzoisothiazolones as selective inhibitors of PHOSPHO1.

J. Millán, E. Sergienko, N. Cosford, 2014, Bioorganic & medicinal chemistry letters.

Modulators of intestinal alkaline phosphatase.

E. Sergienko, E. Bobkova, T. Kiffer-Moreira, 2013, Methods in molecular biology.

A method for direct assessment of tissue-nonspecific alkaline phosphatase (TNAP) inhibitors in blood samples.

E. Sergienko, Chen-Ting Ma, Qing Sun, 2013, Methods in molecular biology.

High-throughput screening of tissue-nonspecific alkaline phosphatase for identification of effectors with diverse modes of action

J. Millán, E. Sergienko, 2010, Nature Protocols.

Melanoma Addiction to GCDH is Mediated by NRF2 Tumor Suppressor Function

E. Ruppin, E. Sergienko, Z. Ronai, 2021 .

Dual-Specificity Phosphatase 3 Deficiency or Inhibition Limits Platelet Activation and Arterial Thrombosis

T. Mustelin, T. Chung, E. Théâtre, 2014, Circulation.

Discovery of Small Molecule Kappa Opioid Receptor Agonist and Antagonist Chemotypes through a HTS and Hit Refinement Strategy.

M. Caron, T. Chung, M. Hedrick, 2012, ACS chemical neuroscience.

p97 Composition Changes Caused by Allosteric Inhibition Are Suppressed by an On-Target Mechanism that Increases the Enzyme's ATPase Activity.

E. Sergienko, J. Toth, M. Petroski, 2016, Cell chemical biology.

Capzimin is a potent and specific inhibitor of proteasome isopeptidase Rpn11.

Seth M. Cohen, T. Chung, R. Deshaies, 2017, Nature chemical biology.

Discovery of small molecule positive allosteric modulators of the secretin receptor.

Brock T Brown, E. Sergienko, L. Miller, 2021, Biochemical pharmacology.

A cellular target engagement assay for the characterization of SHP2 (PTPN11) phosphatase inhibitors

D. Sheffler, E. Sergienko, N. Cosford, 2020, The Journal of Biological Chemistry.

A TR3/Nur77 Peptide-Based High-Throughput Fluorescence Polarization Screen for Small Molecule Bcl-B Inhibitors

John Calvin Reed, E. Sergienko, S. Vasile, 2008, Journal of biomolecular screening.

High-throughput screening for protein tyrosine phosphatase activity modulators.

E. Sergienko, L. Tautz, 2013, Methods in molecular biology.

Allosteric Inhibition of Ubiquitin-like Modifications by a Class of Inhibitor of SUMO-Activating Enzyme.

T. Chung, M. Fakih, Terry D. Lee, 2019, Cell chemical biology.

Discovery of a Positive Allosteric Modulator of Cholecystokinin Action at CCK1R in Normal and Elevated Cholesterol

P. Sexton, A. Christopoulos, E. Sergienko, 2021, Frontiers in Endocrinology.

Ebselen inhibits QSOX1 enzymatic activity and suppresses invasion of pancreatic and renal cancer cell lines

D. Faigel, T. Ho, E. Sergienko, 2015, Oncotarget.

Inhibition of Bfl-1 with N-aryl maleimides.

John Calvin Reed, J. Cashman, Brock T Brown, 2010, Bioorganic & medicinal chemistry letters.

Reconstituted NALP1 inflammasome reveals two-step mechanism of caspase-1 activation.

N. Volkmann, D. Hanein, John Calvin Reed, 2007, Molecular cell.

Yeast Pyruvate Decarboxylase: New Features of the Structure and Mechanism

E. Sergienko, F. Jordan, W. Furey, 2003 .

Inhibition of Hematopoietic Protein Tyrosine Phosphatase Augments and Prolongs ERK1/2 and p38 Activation

T. Mustelin, T. Chung, Li Yang, 2012, ACS chemical biology.

DUSP 3 Phosphatase Deficiency or Inhibition Limit Platelet Activation and Arterial Thrombosis

T. Mustelin, T. Chung, E. Théâtre, 2014 .

Functional Agonists of the Apelin (APJ) Receptor

T. Chung, M. Hedrick, E. Sergienko, 2013 .

High-Throughput Screening for Small-Molecule Inhibitors of Plasmodium falciparum Glucose-6-Phosphate Dehydrogenase 6-Phosphogluconolactonase

S. Rahlfs, K. Becker, M. Hedrick, 2012, Journal of biomolecular screening.

Background—A limitation of current antiplatelet therapies is their inability to separate thrombotic events from bleeding occurrences. A better understanding of the molecular mechanisms leading to platelet activation is important for the development of improved therapies. Recently, protein tyrosine p

T. Mustelin, T. Chung, E. Théâtre, 2015 .

Phosphatase high-throughput screening assay design and selection.

E. Sergienko, 2013, Methods in molecular biology.

Experimental Approaches to Rapid Identification, Profiling, and Characterization of Specific Biological Effects of DOS Compounds

E. Sergienko, S. Heynen-Genel, 2013 .

Triple hybrids of steroids, spiroketals, and oligopeptides as new biomolecular chimeras.

P. Wipf, K. Vuori, E. Sergienko, 2009, Organic Letters.

TR-FRET-Based High-Throughput Screening Assay for Identification of UBC13 Inhibitors

Tram A. Ngo, John Calvin Reed, K. Welsh, 2012, Journal of biomolecular screening.

Design of high-throughput screening assays and identification of a SUMO1-specific small molecule chemotype targeting the SUMO-interacting motif-binding surface.

T. Chung, E. Sergienko, B. Blagg, 2015, ACS combinatorial science.

New activity assays for ENPP1 with physiological substrates ATP and ADP.

E. Sergienko, Chen-Ting Ma, 2013, Methods in molecular biology.

Potent, selective, and orally available benzoisothiazolone phosphomannose isomerase inhibitors as probes for congenital disorder of glycosylation Ia.

H. Freeze, Brock T Brown, M. Hedrick, 2011, Journal of medicinal chemistry.

Chemical Genomics: Basics of HTS Assay Design and Optimization

E. Sergienko, 2012 .

The Role of PHOSPHO1 in the Initiation of Skeletal Calcification

Nicholas Michael Hedrick, T. Chung, J. Rascon, 2010 .

Inhibition of the Hematopoietic Protein Tyrosine Phosphatase by Phenoxyacetic Acids.

T. Mustelin, T. Chung, X. Chan, 2011, ACS medicinal chemistry letters.

Small-Molecule Inhibitors of Vaccinia-H1-Related Phosphatase VHR

T. Mustelin, T. Chung, E. Sergienko, 2010 .

Probe Report Title : Small-Molecule Inhibitors of Vaccinia-H 1-Related Phosphatase VHR

E. Sergienko, S. Vasile, Mostofi, 2010 .

New model for activation of yeast pyruvate decarboxylase by substrate consistent with the alternating sites mechanism: demonstration of the existence of two active forms of the enzyme.

E. Sergienko, F. Jordan, 2002, Biochemistry.

Melanoma-intrinsic NR2F6 activity regulates anti-tumor immunity

E. Ruppin, R. Sears, M. Herlyn, 2022, bioRxiv.

High-Throughput Fluorescence Assay for Small-Molecule Inhibitors of Autophagins/Atg4

John Calvin Reed, K. Welsh, E. Sergienko, 2011, Journal of biomolecular screening.

Table 1, PubChem Assay Summaries for Probe project

Darren Finlay, Robert Ardecky, Thomas D.Y. Chung, 2010 .

Probing the CXCR6/CXCL16 Axis: Targeting Prevention of Prostate Cancer Metastasis

R. Taichman, T. Chung, M. Hedrick, 2014 .

Serine-Threonine Kinase TAO3-Mediated Trafficking of Endosomes Containing the Invadopodia Scaffold TKS5α Promotes Cancer Invasion and Tumor Growth

M. Abelman, S. McWeeney, E. Sergienko, 2021, Cancer Research.

Selective GPR35 Antagonists - Probe 3

M. Caron, T. Chung, E. Sergienko, 2011 .

Selective GPR35 Antagonists - Probes 1 & 2

M. Caron, T. Chung, E. Sergienko, 2010 .

Identification and characterization of small molecule inhibitors of the ubiquitin ligases Siah1/2 in melanoma and prostate cancer cells.

R. Liddington, M. Jackson, M. Gleave, 2019, Cancer letters.

Selective UBC 13 Inhibitors

Tram A. Ngo, J. Reed, T. Chung, 2014 .

Kinetic mechanism of the glycogen-phosphorylase-catalysed reaction in the direction of glycogen synthesis: co-operative interactions of AMP and glucose 1-phosphate during catalysis.

E. Sergienko, D. Srivastava, 1997, The Biochemical journal.

Discovery and characterization of 2-aminobenzimidazole derivatives as selective NOD1 inhibitors.

R. Spreafico, John Calvin Reed, Brock T Brown, 2011, Chemistry & biology.

Melanoma-intrinsic NR2F6 activity regulates antitumor immunity

E. Ruppin, R. Sears, M. Herlyn, 2023, Science advances.

High Throughput Screening Assays for NOD1 Inhibitors - Probe 2

John Calvin Reed, T. Chung, Brock T Brown, 2010 .