Selective covalent targeting of GPX4 using masked nitrile-oxide electrophiles

Selective and reversible modification of kinase cysteines with chlorofluoroacetamides

(2019) Naoya Shindo et al.   Nature Chemical Biology

Diacylfuroxans Are Masked Nitrile Oxides That Inhibit GPX4 Covalently

(2019) John K. Eaton et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

The Nitro Group as a Masked Electrophile in Covalent Enzyme Inhibition

(2018) Sneha Ray et al.   ACS Chemical Biology

Crystal structure and functional characterization of selenocysteine-containing glutathione peroxidase 4 suggests an alternative mechanism of peroxide reduction

(2018) Astrid Borchert et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS

Multi-stage Differentiation Defines Melanoma Subtypes with Differential Vulnerability to Drug-Induced Iron-Dependent Oxidative Stress

(2018) Jennifer Tsoi et al.   CANCER CELL

FINO2 initiates ferroptosis through GPX4 inactivation and iron oxidation

(2018) Michael M. Gaschler et al.   Nature Chemical Biology

Resolving the Role of Lipoxygenases in the Initiation and Execution of Ferroptosis

(2018) Ron Shah et al.   ACS Central Science

Selenium-Encoded Isotopic Signature Targeted Profiling

(2018) Jinjun Gao et al.   ACS Central Science

Discovery and Characterization of the Potent and Highly Selective (Piperidin-4-yl)pyrido[3,2-d]pyrimidine Based in Vitro Probe BAY-885 for the Kinase ERK5

(2018) Duy Nguyen et al.   JOURNAL OF MEDICINAL CHEMISTRY

Drug-tolerant persister cancer cells are vulnerable to GPX4 inhibition

(2017) Matthew J. Hangauer et al.   NATURE

Dependency of a therapy-resistant state of cancer cells on a lipid peroxidase pathway

(2017) Vasanthi S. Viswanathan et al.   NATURE

Computational correction of copy number effect improves specificity of CRISPR–Cas9 essentiality screens in cancer cells

(2017) Robin M Meyers et al.   NATURE GENETICS

On the Mechanism of Cytoprotection by Ferrostatin-1 and Liproxstatin-1 and the Role of Lipid Peroxidation in Ferroptotic Cell Death

(2017) Omkar Zilka et al.   ACS Central Science

Metabolically Labile Fumarate Esters Impart Kinetic Selectivity to Irreversible Inhibitors

(2016) Balyn W. Zaro et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Proteome-wide covalent ligand discovery in native biological systems

(2016) Keriann M. Backus et al.   NATURE

Global survey of cell death mechanisms reveals metabolic regulation of ferroptosis

(2016) Kenichi Shimada et al.   Nature Chemical Biology

Peroxidation of polyunsaturated fatty acids by lipoxygenases drives ferroptosis

(2016) Wan Seok Yang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Systematic Study of the Glutathione (GSH) Reactivity of N-Arylacrylamides: 1. Effects of Aryl Substitution

(2015) Victor J. Cee et al.   JOURNAL OF MEDICINAL CHEMISTRY

Correlating chemical sensitivity and basal gene expression reveals mechanism of action

(2015) Matthew G Rees et al.   Nature Chemical Biology

Synthesis of furoxan derivatives: DABCO-mediated cascade sulfonylation/cyclization reaction of α-nitro-ketoximes

(2015) Jian-Qiang Zhao et al.   TETRAHEDRON

Harnessing Connectivity in a Large-Scale Small-Molecule Sensitivity Dataset

(2015) B. Seashore-Ludlow et al.   Cancer Discovery

Regulation of Ferroptotic Cancer Cell Death by GPX4

(2014) Wan Seok Yang et al.   CELL

Preparation of 13 or 9-Hydroperoxy-9Z,11E (9E,11E) or 10E,12Z (10E,12E)-Octadecadienoic Phosphatidylcholine Hydroperoxide

(2014) Shunji Kato et al.   Journal of Oleo Science

Ferrostatins Inhibit Oxidative Lipid Damage and Cell Death in Diverse Disease Models

(2014) Rachid Skouta et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Inactivation of the ferroptosis regulator Gpx4 triggers acute renal failure in mice

(2014) Jose Pedro Friedmann Angeli et al.   NATURE CELL BIOLOGY

Nitro drugs for the treatment of trypanosomatid diseases: past, present, and future prospects

(2014) Stephen Patterson et al.   TRENDS IN PARASITOLOGY

An Interactive Resource to Identify Cancer Genetic and Lineage Dependencies Targeted by Small Molecules

(2013) Amrita Basu et al.   CELL

Monitoring Drug Target Engagement in Cells and Tissues Using the Cellular Thermal Shift Assay

(2013) D. M. Molina et al.   SCIENCE

Ferroptosis: An Iron-Dependent Form of Nonapoptotic Cell Death

(2012) Scott J. Dixon et al.   CELL

Development of small-molecule probes that selectively kill cells induced to express mutant RAS

(2011) Michel Weïwer et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Elucidation of a Novel Bioactivation Pathway of a 3,4-Unsubstituted Isoxazole in Human Liver Microsomes: Formation of a Glutathione Adduct of a Cyanoacrolein Derivative after Isoxazole Ring Opening

(2010) J. Yu et al.   DRUG METABOLISM AND DISPOSITION

Benzothiazinones: Prodrugs That Covalently Modify the Decaprenylphosphoryl-β-d-ribose 2′-epimerase DprE1 ofMycobacterium tuberculosis

(2010) Claudia Trefzer et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Quantitative reactivity profiling predicts functional cysteines in proteomes

(2010) Eranthie Weerapana et al.   NATURE

Glucosinolate engineering identifies a γ-glutamyl peptidase

(2009) Fernando Geu-Flores et al.   Nature Chemical Biology

Synthetic Lethal Screening Identifies Compounds Activating Iron-Dependent, Nonapoptotic Cell Death in Oncogenic-RAS-Harboring Cancer Cells

(2008) Wan Seok Yang et al.   CHEMISTRY & BIOLOGY