Reviewing Hit Discovery Literature for Difficult Targets: Glutathione Transferase Omega-1 as an Example.

No abstract is available for this paper.

• Publication year

  2018

• Venue

  Journal of Medicinal Chemistry

• Publication date

  2018-04-13

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1021/acs.jmedchem.8b00318PMID 29652143
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Assay interference and off-target liabilities of reported histone acetyltransferase inhibitors

  2017cited by this paper
• Chemotherapy-Induced Ca2+ Release Stimulates Breast Cancer Stem Cell Enrichment.

  2017cited by this paper
• Seven Year Itch: Pan-Assay Interference Compounds (PAINS) in 2017—Utility and Limitations

  2017cited by this paper
• Upregulated glutathione transferase omega-1 correlates with progression of urinary bladder carcinoma

  2017cited by this paper
• PAIN-less identification and evaluation of small molecule inhibitors against protein tyrosine phosphatase 1B.

  2017cited by this paper
• GSTO1-1 plays a pro-inflammatory role in models of inflammation, colitis and obesity

  2017cited by this paper
• Dependency of a therapy-resistant state of cancer cells on a lipid peroxidase pathway

  2017cited by this paper
• Repurposing of Proton Pump Inhibitors as first identified small molecule inhibitors of endo-β-N-acetylglucosaminidase (ENGase) for the treatment of NGLY1 deficiency, a rare genetic disease.

  2017cited by this paper
• A functional drug re-purposing screening identifies carfilzomib as a drug preventing 17β-estradiol: ERα signaling and cell proliferation in breast cancer cells

  2017cited by this paper
• High-Throughput Screening Using Mass Spectrometry within Drug Discovery.

  2016cited by this paper
• Mechanistic evaluation and transcriptional signature of a glutathione S-transferase omega 1 inhibitor

  2016cited by this paper
• Can you teach old drugs new tricks?

  2016cited by this paper
• Small molecules, big targets: drug discovery faces the protein–protein interaction challenge

  2016cited by this paper
• Using Protein-Confined Proximity To Determine Chemical Reactivity.

  2016cited by this paper
• Structure, function and disease relevance of Omega-class glutathione transferases

  2016cited by this paper
• Feeling Nature's PAINS: Natural Products, Natural Product Drugs, and Pan Assay Interference Compounds (PAINS).

  2016cited by this paper
• Specificity of Protein Covalent Modification by the Electrophilic Proteasome Inhibitor Carfilzomib in Human Cells*

  2016cited by this paper
• Structural understanding of the recycling of oxidized ascorbate by dehydroascorbate reductase (OsDHAR) from Oryza sativa L. japonica

  2016cited by this paper
• Proteome-wide covalent ligand discovery in native biological systems

  2016cited by this paper
• AlphaScreen selectivity assay for β-catenin/B-cell lymphoma 9 inhibitors.

  2015cited by this paper
• The promise and peril of chemical probes.

  2015cited by this paper
• A small-molecule inhibitor of the NLRP3 inflammasome for the treatment of inflammatory diseases

  2015cited by this paper
• Identification of Novel Inhibitors of Organic Anion Transporting Polypeptides 1B1 and 1B3 (OATP1B1 and OATP1B3) Using a Consensus Vote of Six Classification Models

  2015cited by this paper
• PAINS in the Assay: Chemical Mechanisms of Assay Interference and Promiscuous Enzymatic Inhibition Observed during a Sulfhydryl-Scavenging HTS

  2015cited by this paper
• Genomic instability and cellular stress in organ biopsies and peripheral blood lymphocytes from patients with colorectal cancer and predisposing pathologies

  2015cited by this paper
• Members of the Chloride Intracellular Ion Channel Protein Family Demonstrate Glutaredoxin-Like Enzymatic Activity

  2015cited by this paper
• GSTO1-1 modulates metabolism in macrophages activated through the LPS and TLR4 pathway

  2015cited by this paper
• Quantification and visualization of glutathione S-transferase omega 1 in cells using inductively coupled plasma mass spectrometry (ICP-MS) and fluorescence microscopy

  2015cited by this paper
• The discovery of first-in-class drugs: origins and evolution

  2014cited by this paper
• Identification of Natural Compound Carnosol as a Novel TRPA1 Receptor Agonist

  2014cited by this paper
• Identification of glutathione S-transferase omega 1 (GSTO1) protein as a novel tumor-associated antigen and its autoantibody in human esophageal squamous cell carcinoma

  2014cited by this paper
• Carnosic acid inhibits TLR4-MyD88 signaling pathway in LPS-stimulated 3T3-L1 adipocytes

  2014cited by this paper
• Glutathione transferase omega 1 is required for the lipopolysaccharide-stimulated induction of NADPH oxidase 1 and the production of reactive oxygen species in macrophages.

  2014cited by this paper
• The role of ligand efficiency metrics in drug discovery

  2014cited by this paper
• Chemical and computational methods for the characterization of covalent reactive groups for the prospective design of irreversible inhibitors.

  2014cited by this paper
• Chemistry: Chemical con artists foil drug discovery

  2014cited by this paper
• High-Throughput Screen of Natural Product Libraries for Hsp90 Inhibitors

  2014cited by this paper
• Promiscuity and selectivity in covalent enzyme inhibition: a systematic study of electrophilic fragments.

  2014cited by this paper
• Drug discovery considerations in the development of covalent inhibitors.

  2014cited by this paper
• Pyridoxylamine reactivity kinetics as an amine based nucleophile for screening electrophilic dermal sensitizers.

  2014cited by this paper
• A Role for Glutathione Transferase Omega 1 (GSTO1-1) in the Glutathionylation Cycle

  2013cited by this paper
• Glutathione transferases, regulators of cellular metabolism and physiology.

  2013cited by this paper
• A Cell-Free Fluorometric High-Throughput Screen for Inhibitors of Rtt109-Catalyzed Histone Acetylation

  2013cited by this paper
• Abbott Physicochemical Tiering (APT)--a unified approach to HTS triage.

  2012cited by this paper
• An inhibitor of glutathione S-transferase omega 1 that selectively targets apoptotic cells.

  2012cited by this paper
• Using Functional Signatures to Identify Repositioned Drugs for Breast, Myelogenous Leukemia and Prostate Cancer

  2012cited by this paper
• Large Scale Prediction and Testing of Drug Activity on Side-Effect Targets

  2012cited by this paper
• S-Glutathionylation signaling in cell biology: progress and prospects.

  2012cited by this paper
• Structural insights into the dehydroascorbate reductase activity of human omega-class glutathione transferases.

  2012cited by this paper
• Potent and selective inhibitors of glutathione S-transferase omega 1 that impair cancer drug resistance.

  2011cited by this paper
• Protoapigenone, a natural derivative of apigenin, induces mitogen-activated protein kinase-dependent apoptosis in human breast cancer cells associated with induction of oxidative stress and inhibition of glutathione S-transferase π

  2011cited by this paper
• Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor.

  2011cited by this paper
• The resurgence of covalent drugs

  2011cited by this paper
• Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain

  2011cited by this paper
• The Cytokine Release Inhibitory Drug CRID3 Targets ASC Oligomerisation in the NLRP3 and AIM2 Inflammasomes

  2011cited by this paper
• Synopsis of some recent tactical application of bioisosteres in drug design.

  2011cited by this paper
• Profiling the NIH Small Molecule Repository for Compounds That Generate H2O2 by Redox Cycling in Reducing Environments

  2010cited by this paper
• Glutathione transferases as mediators of signaling pathways involved in cell proliferation and cell death

  2010cited by this paper
• Glutathione transferase omega 1-1 (GSTO1-1) plays an anti-apoptotic role in cell resistance to cisplatin toxicity.

  2010cited by this paper
• Drug- and Lead-likeness, Target Class, and Molecular Diversity Analysis of 7.9 Million Commercially Available Organic Compounds Provided by 29 Suppliers

  2010cited by this paper
• Quantitative analyses of aggregation, autofluorescence, and reactivity artifacts in a screen for inhibitors of a thiol protease.

  2010cited by this paper
• New substructure filters for removal of pan assay interference compounds (PAINS) from screening libraries and for their exclusion in bioassays.

  2010cited by this paper
• Polymorphisms in Glutathione S-Transferase Omega-1 Gene and Increased Risk of Sporadic Alzheimer Disease

  2010cited by this paper
• Apparent activity in high-throughput screening: origins of compound-dependent assay interference.

  2010cited by this paper
• The art of the chemical probe.

  2010cited by this paper
• Isozyme-specific fluorescent inhibitor of glutathione s-transferase omega 1.

  2010cited by this paper
• Observations on screening-based research and some concerning trends in the literature.

  2010cited by this paper
• An Azido-Biotin Reagent for Use in the Isolation of Protein Adducts of Lipid-derived Electrophiles by Streptavidin Catch and Photorelease*

  2009cited by this paper
• The antioxidant glutathione in the fish cell lines EPC and BCF-2: response to model pro-oxidants as measured by three different fluorescent dyes.

  2009cited by this paper
• Substrate-Free High-Throughput Screening Identifies Selective Inhibitors for Uncharacterized Enzymes

  2009cited by this paper
• Escape from flatland: increasing saturation as an approach to improving clinical success.

  2009cited by this paper
• Protein S-glutathionylation: a regulatory device from bacteria to humans.

  2009cited by this paper
• Flow cytometric determination of intracellular non-protein thiols in Leishmania promastigotes using 5-chloromethyl fluorescein diacetate.

  2009cited by this paper
• Recent developments in fragment-based drug discovery.

  2008cited by this paper
• S-(4-Nitrophenacyl)glutathione is a specific substrate for glutathione transferase omega 1-1.

  2008cited by this paper
• Polymorphism of glutathione transferase Omega 1 in a population exposed to a high environmental arsenic burden

  2008cited by this paper
• Pharmacology of proton pump inhibitors

  2008cited by this paper
• Fluorescence spectroscopic profiling of compound libraries.

  2008cited by this paper
• Development of a 384-Well Colorimetric Assay to Quantify Hydrogen Peroxide Generated by the Redox Cycling of Compounds in the Presence of Reducing Agents

  2008cited by this paper
• Discovery of small molecule agonists for the bombesin receptor subtype 3 (BRS-3) based on an omeprazole lead.

  2008cited by this paper
• Physiochemical drug properties associated with in vivo toxicological outcomes.

  2008cited by this paper
• Deletion of Glu155 causes a deficiency of glutathione transferase Omega 1-1 but does not alter sensitivity to arsenic trioxide and other cytotoxic drugs.

  2008cited by this paper
• Comprehensive mechanistic analysis of hits from high-throughput and docking screens against beta-lactamase.

  2008cited by this paper
• Zinc diethyldithiocarbamate allergenicity: potential haptenation mechanisms

  2008cited by this paper
• Toxicological evaluation of thiol-reactive compounds identified using a la assay to detect reactive molecules by nuclear magnetic resonance.

  2007cited by this paper
• Mass spectrometric techniques for label-free high-throughput screening in drug discovery.

  2007cited by this paper
• Identification of platinum-resistance associated proteins through proteomic analysis of human ovarian cancer cells and their platinum-resistant sublines.

  2007cited by this paper
• A high-throughput screen for aggregation-based inhibition in a large compound library.

  2007cited by this paper
• Designed Amyloid β Peptide Fibril—A Tool for High‐Throughput Screening of Fibril Inhibitors

  2007cited by this paper
• Glutathione transferase omega 1 catalyzes the reduction of S-(phenacyl)glutathiones to acetophenones.

  2007cited by this paper
• Recommendations for the Reduction of Compound Artifacts in Time-Resolved Fluorescence Resonance Energy Transfer Assays

  2007cited by this paper
• A Simple Assay for Detection of Small-Molecule Redox Activity

  2007cited by this paper
• Inhibition of human glutathione S-transferase omega by tocopherol succinate.

  2006cited by this paper
• Interpreting steep dose-response curves in early inhibitor discovery.

  2006cited by this paper
• Glutathione-S-transferase-omega [MMA(V) reductase] knockout mice: enzyme and arsenic species concentrations in tissues after arsenate administration.

  2006cited by this paper
• Derivation and validation of toxicophores for mutagenicity prediction.

  2005cited by this paper
• Nomenclature for mammalian soluble glutathione transferases.

  2005cited by this paper
• Potent activity of carfilzomib, a novel, irreversible inhibitor of the ubiquitin-proteasome pathway, against preclinical models of multiple myeloma.

  2005cited by this paper
• Characterization of the monomethylarsonate reductase and dehydroascorbate reductase activities of Omega class glutathione transferase variants: implications for arsenic metabolism and the age-at-onset of Alzheimer's and Parkinson's diseases

  2005cited by this paper
• Classification of drugs in absorption classes using the classification and regression trees (CART) methodology.

  2005cited by this paper

• β-Glucuronidase Acts as a Novel Nonantioxidative Target for Vitamin E.

  2025cites this paper
• Discovery of Potent, Allosteric GSTO1 Covalent Inhibitors with a New Binding Mode.

  2025cites this paper
• Development of potent glutathione transferase Omega-1 inhibitors with applications in inflammation and cancer therapy.

  2025cites this paper
• Glutathione S‐transferase omega class 1 (GSTO1)‐associated large extracellular vesicles are involved in tumor‐associated macrophage‐mediated cisplatin resistance in bladder cancer

  2024cites this paper
• Chemistry and biology of enzymes in protein glutathionylation.

  2023cites this paper
• Glutathione in Protein Redox Modulation through S-Glutathionylation and S-Nitrosylation

  2021cites this paper
• The Interaction of Human Glutathione Transferase GSTA1-1 with Reactive Dyes

  2021cites this paper
• Development of Benzenesulfonamide Derivatives as Potent Glutathione Transferase Omega-1 Inhibitors.

  2020cites this paper
• Structure-Based Design of N-(5-Phenylthiazol-2-yl)acrylamides as Novel and Potent Glutathione S-Transferase Omega 1 Inhibitors.

  2019cites this paper
• The mercapturic acid pathway

  2019cites this paper
• A cyclopropene electrophile that targets glutathione S-transferase omega-1 in cells.

  2019cites this paper
• Integrated phenotypic screening and activity-based protein profiling to reveal potential therapy targets of pancreatic cancer.

  2019cites this paper
• Risk Management in Early Discovery Medicinal Chemistry.

  2018cites this paper
• Glutathione Transferases: Potential Targets to Overcome Chemoresistance in Solid Tumors

  2018cites this paper
• Modeling Small-Molecule Reactivity Identifies Promiscuous Bioactive Compounds

  2018cites this paper