Generation of small molecules to interfere with regulated necrosis

Glutathione and Thioredoxin Antioxidant Pathways Synergize to Drive Cancer Initiation and Progression

(2015) Isaac S. Harris et al.   CANCER CELL

The Free Radical Scavenger NecroX-7 Attenuates Acute Graft-versus-Host Disease via Reciprocal Regulation of Th1/Regulatory T Cells and Inhibition of HMGB1 Release

(2015) Keon-Il Im et al.   JOURNAL OF IMMUNOLOGY

A RIPK3–Caspase 8 Complex Mediates Atypical Pro–IL-1β Processing

(2015) Kenta Moriwaki et al.   JOURNAL OF IMMUNOLOGY

The indole derivative NecroX-7 improves nonalcoholic steatohepatitis inob/obmice through suppression of mitochondrial ROS/RNS and inflammation

(2015) Hyo Kyun Chung et al.   LIVER INTERNATIONAL

PARP inhibitors: A new era of targeted therapy

(2015) Shifalika Tangutoori et al.   MATURITAS

Poly(ADP-ribosylation) and neurodegenerative disorders

(2015) Davide Alessandro Basello et al.   MITOCHONDRION

Necroptosis and its role in inflammation

(2015) Manolis Pasparakis et al.   NATURE

Ferroptosis as a p53-mediated activity during tumour suppression

(2015) Le Jiang et al.   NATURE

The diverse role of RIP kinases in necroptosis and inflammation

(2015) John Silke et al.   NATURE IMMUNOLOGY

A cytosolic heat shock protein 90 and cochaperone CDC37 complex is required for RIP3 activation during necroptosis

(2015) Dianrong Li et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

A cellular screen identifies ponatinib and pazopanib as inhibitors of necroptosis

(2015) A Fauster et al.   Cell Death & Disease

Structure Guided Design of Potent and Selective Ponatinib-Based Hybrid Inhibitors for RIPK1

(2015) Malek Najjar et al.   Cell Reports

Necroptosis Interfaces with MOMP and the MPTP in Mediating Cell Death

(2015) Jason Karch et al.   PLoS One

Exploration of Type II Binding Mode: A Privileged Approach for Kinase Inhibitor Focused Drug Discovery?

(2014) Zheng Zhao et al.   ACS Chemical Biology

Poly(ADP-ribose): A signaling molecule in different paradigms of cell death

(2014) Francesca Aredia et al.   BIOCHEMICAL PHARMACOLOGY

RIPK1 Regulates RIPK3-MLKL-Driven Systemic Inflammation and Emergency Hematopoiesis

(2014) James A. Rickard et al.   CELL

RIPK1 Blocks Early Postnatal Lethality Mediated by Caspase-8 and RIPK3

(2014) Christopher P. Dillon et al.   CELL

Regulation of Ferroptotic Cancer Cell Death by GPX4

(2014) Wan Seok Yang et al.   CELL

Distinct roles of RIP1–RIP3 hetero- and RIP3–RIP3 homo-interaction in mediating necroptosis

(2014) X-N Wu et al.   CELL DEATH AND DIFFERENTIATION

Toll-like Receptor-mediated Down-regulation of the Deubiquitinase Cylindromatosis (CYLD) Protects Macrophages from Necroptosis in Wild-derived Mice

(2014) Stephen A. Schworer et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Cutting Edge: RIPK1 Kinase Inactive Mice Are Viable and Protected from TNF-Induced Necroptosis In Vivo

(2014) Apostolos Polykratis et al.   JOURNAL OF IMMUNOLOGY

Cutting Edge: RIP1 Kinase Activity Is Dispensable for Normal Development but Is a Key Regulator of Inflammation in SHARPIN-Deficient Mice

(2014) S. B. Berger et al.   JOURNAL OF IMMUNOLOGY

RIP3 Induces Apoptosis Independent of Pronecrotic Kinase Activity

(2014) Pratyusha Mandal et al.   MOLECULAR CELL

RIPK1 ensures intestinal homeostasis by protecting the epithelium against apoptosis

(2014) Nozomi Takahashi et al.   NATURE

RIPK1 maintains epithelial homeostasis by inhibiting apoptosis and necroptosis

(2014) Marius Dannappel et al.   NATURE

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

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

Necroptosis

(2014) Andreas Linkermann et al.   NEW ENGLAND JOURNAL OF MEDICINE

Poly(ADP-ribose) polymerase-dependent energy depletion occurs through inhibition of glycolysis

(2014) S. A. Andrabi et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Activation of the pseudokinase MLKL unleashes the four-helix bundle domain to induce membrane localization and necroptotic cell death

(2014) Joanne M. Hildebrand et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Caspase-8 and RIP kinases regulate bacteria-induced innate immune responses and cell death

(2014) D. Weng et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

RIP1 suppresses innate immune necrotic as well as apoptotic cell death during mammalian parturition

(2014) W. J. Kaiser et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Synchronized renal tubular cell death involves ferroptosis

(2014) Andreas Linkermann et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Necroptosis in health and diseases

(2014) Wen Zhou et al.   SEMINARS IN CELL & DEVELOPMENTAL BIOLOGY

Necroptosis: An emerging type of cell death in liver diseases

(2014) Waqar Khalid Saeed   WORLD JOURNAL OF GASTROENTEROLOGY

The B-RafV600E inhibitor dabrafenib selectively inhibits RIP3 and alleviates acetaminophen-induced liver injury

(2014) J-X Li et al.   Cell Death & Disease

MLKL Compromises Plasma Membrane Integrity by Binding to Phosphatidylinositol Phosphates

(2014) Yves Dondelinger et al.   Cell Reports

Insights into the evolution of divergent nucleotide-binding mechanisms among pseudokinases revealed by crystal structures of human and mouse MLKL

(2013) James M. Murphy et al.   BIOCHEMICAL JOURNAL

A novel necroptosis inhibitor—necrostatin-21 and its SAR study

(2013) Zhijie Wu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

RIPK3 contributes to TNFR1-mediated RIPK1 kinase-dependent apoptosis in conditions of cIAP1/2 depletion or TAK1 kinase inhibition

(2013) Y Dondelinger et al.   CELL DEATH AND DIFFERENTIATION

Translocation of mixed lineage kinase domain-like protein to plasma membrane leads to necrotic cell death

(2013) Xin Chen et al.   CELL RESEARCH

Mlkl knockout mice demonstrate the indispensable role of Mlkl in necroptosis

(2013) Jianfeng Wu et al.   CELL RESEARCH

TNF-induced necroptosis and PARP-1-mediated necrosis represent distinct routes to programmed necrotic cell death

(2013) Justyna Sosna et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

Necrosis-dependent and independent signaling of the RIP kinases in inflammation

(2013) Kenta Moriwaki et al.   CYTOKINE & GROWTH FACTOR REVIEWS

The Pseudokinase MLKL Mediates Necroptosis via a Molecular Switch Mechanism

(2013) James M. Murphy et al.   IMMUNITY

Toll-like Receptor 3-mediated Necrosis via TRIF, RIP3, and MLKL

(2013) William J. Kaiser et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Interferon-induced RIP1/RIP3-mediated necrosis requires PKR and is licensed by FADD and caspases

(2013) R. J. Thapa et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

HSP90 Inhibitors: Current Development and Potential in Cancer Therapy

(2013) Katerina Sidera et al.   Recent Patents on Anti-Cancer Drug Discovery

Structural Basis of RIP1 Inhibition by Necrostatins

(2013) Tian Xie et al.   STRUCTURE

Discovery of Small Molecule RIP1 Kinase Inhibitors for the Treatment of Pathologies Associated with Necroptosis

(2013) Philip A. Harris et al.   ACS Medicinal Chemistry Letters

Widespread Mitochondrial Depletion via Mitophagy Does Not Compromise Necroptosis

(2013) Stephen W.G. Tait et al.   Cell Reports

Structural Insights into RIP3-Mediated Necroptotic Signaling

(2013) Tian Xie et al.   Cell Reports

Fluorescence polarization assay for inhibitors of the kinase domain of receptor interacting protein 1

(2012) Jenny L. Maki et al.   ANALYTICAL BIOCHEMISTRY

An Indole Derivative Protects Against Acetaminophen-Induced Liver Injury by Directly Binding to N-Acetyl-p-Benzoquinone Imine in Mice

(2012) Ji-Hoon Park et al.   ANTIOXIDANTS & REDOX SIGNALING

Optimization of tricyclic Nec-3 necroptosis inhibitors for in vitro liver microsomal stability

(2012) Sungwoon Choi et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Advances in using PARP inhibitors to treat cancer

(2012) Shivaani Kummar et al.   BMC Medicine

NecroX-5 prevents hypoxia/reoxygenation injury by inhibiting the mitochondrial calcium uniporter

(2012) Vu Thi Thu et al.   CARDIOVASCULAR RESEARCH

Ferroptosis: An Iron-Dependent Form of Nonapoptotic Cell Death

(2012) Scott J. Dixon et al.   CELL

Mixed Lineage Kinase Domain-like Protein Mediates Necrosis Signaling Downstream of RIP3 Kinase

(2012) Liming Sun et al.   CELL

The Mitochondrial Phosphatase PGAM5 Functions at the Convergence Point of Multiple Necrotic Death Pathways

(2012) Zhigao Wang et al.   CELL

The RIP1/RIP3 Necrosome Forms a Functional Amyloid Signaling Complex Required for Programmed Necrosis

(2012) Jixi Li et al.   CELL

TRAIL induces necroptosis involving RIPK1/RIPK3-dependent PARP-1 activation

(2012) S Jouan-Lanhouet et al.   CELL DEATH AND DIFFERENTIATION

Activity and specificity of necrostatin-1, small-molecule inhibitor of RIP1 kinase

(2012) A Degterev et al.   CELL DEATH AND DIFFERENTIATION

DAI/ZBP1/DLM-1 Complexes with RIP3 to Mediate Virus-Induced Programmed Necrosis that Is Targeted by Murine Cytomegalovirus vIRA

(2012) Jason W. Upton et al.   Cell Host & Microbe

Role of PARP Inhibitors in Cancer Biology and Therapy

(2012) D. Davar et al.   CURRENT MEDICINAL CHEMISTRY

αC helix displacement as a general approach for allosteric modulation of protein kinases

(2012) Lorenzo Palmieri et al.   DRUG DISCOVERY TODAY

Unknown

(2012) Andreas Linkermann et al.   MOLECULAR MEDICINE

Concise Drug Review: Pazopanib and Axitinib

(2012) R. M. J. M. van Geel et al.   ONCOLOGIST

NecroX-7 prevents oxidative stress-induced cardiomyopathy by inhibition of NADPH oxidase activity in rats

(2012) Joonghoon Park et al.   TOXICOLOGY AND APPLIED PHARMACOLOGY

A novel role for RIP1 kinase in mediating TNFα production

(2012) D E Christofferson et al.   Cell Death & Disease

Necrostatin-1 analogues: critical issues on the specificity, activity and in vivo use in experimental disease models

(2012) N Takahashi et al.   Cell Death & Disease

NEMO and RIP1 Control Cell Fate in Response to Extensive DNA Damage via TNF-α Feedforward Signaling

(2011) Sharon Biton et al.   CELL

PARP Inhibitor Treatment in Ovarian and Breast Cancer

(2011) Marcie K. Weil et al.   CURRENT PROBLEMS IN CANCER

RIP3 mediates the embryonic lethality of caspase-8-deficient mice

(2011) William J. Kaiser et al.   NATURE

Catalytic activity of the caspase-8–FLIPL complex inhibits RIPK3-dependent necrosis

(2011) Andrew Oberst et al.   NATURE

RIP1-Dependent and Independent Effects of Necrostatin-1 in Necrosis and T Cell Activation

(2011) YoungSik Cho et al.   PLoS One

NecroX as a novel class of mitochondrial reactive oxygen species and ONOO− scavenger

(2010) Hyoung Jin Kim et al.   ARCHIVES OF PHARMACAL RESEARCH

NAD+ Depletion Is Necessary and Sufficient forPoly(ADP-Ribose) Polymerase-1-Mediated Neuronal Death

(2010) C. C. Alano et al.   JOURNAL OF NEUROSCIENCE

Effect of Necrosis Modulator Necrox-7 on Hepatic Ischemia-Reperfusion Injury in Beagle Dogs

(2010) J.M. Choi et al.   TRANSPLANTATION PROCEEDINGS

Phosphorylation-Driven Assembly of the RIP1-RIP3 Complex Regulates Programmed Necrosis and Virus-Induced Inflammation

(2009) YoungSik Cho et al.   CELL

Receptor Interacting Protein Kinase-3 Determines Cellular Necrotic Response to TNF-α

(2009) Sudan He et al.   CELL

Necroptosis, necrosis and secondary necrosis converge on similar cellular disintegration features

(2009) T Vanden Berghe et al.   CELL DEATH AND DIFFERENTIATION

Mitochondrial Permeability Transition Pore Opening as a Promising Therapeutic Target in Cardiac Diseases

(2009) S. Javadov et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Inhibition of Poly(ADP-Ribose) Polymerase in Tumors fromBRCAMutation Carriers

(2009) Peter C. Fong et al.   NEW ENGLAND JOURNAL OF MEDICINE

RIP3, an Energy Metabolism Regulator That Switches TNF-Induced Cell Death from Apoptosis to Necrosis

(2009) D.-W. Zhang et al.   SCIENCE

Structure–activity relationship and liver microsome stability studies of pyrrole necroptosis inhibitors

(2008) Xin Teng et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Structure–activity relationship study of a novel necroptosis inhibitor, necrostatin-7

(2008) Weihong Zheng et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Identification of RIP1 kinase as a specific cellular target of necrostatins

(2008) Alexei Degterev et al.   Nature Chemical Biology