A cellular screen identifies ponatinib and pazopanib as inhibitors of necroptosis

SLC38A9 is a component of the lysosomal amino acid sensing machinery that controls mTORC1

(2015) Manuele Rebsamen et al.   NATURE

Necroptosis and its role in inflammation

(2015) Manolis Pasparakis et al.   NATURE

TAK1 control of cell death

(2014) S R Mihaly et al.   CELL DEATH AND DIFFERENTIATION

RIP kinases: key decision makers in cell death and innate immunity

(2014) F Humphries et al.   CELL DEATH AND DIFFERENTIATION

TAK1 kinase switches cell fate from apoptosis to necrosis following TNF stimulation

(2014) Sho Morioka et al.   JOURNAL OF CELL BIOLOGY

RIP3 Induces Apoptosis Independent of Pronecrotic Kinase Activity

(2014) Pratyusha Mandal et al.   MOLECULAR CELL

Mixed Lineage Kinase Domain-like Protein MLKL Causes Necrotic Membrane Disruption upon Phosphorylation by RIP3

(2014) Huayi Wang et al.   MOLECULAR CELL

Stereospecific targeting of MTH1 by (S)-crizotinib as an anticancer strategy

(2014) Kilian V. M. Huber et al.   NATURE

Necroptosis

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

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

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

Activity of Protein Kinase RIPK3 Determines Whether Cells Die by Necroptosis or Apoptosis

(2014) K. Newton et al.   SCIENCE

A Plug Release Mechanism for Membrane Permeation by MLKL

(2014) Lijing Su et al.   STRUCTURE

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

RIPK3-Mediated Necroptosis Promotes Donor Kidney Inflammatory Injury and Reduces Allograft Survival

(2013) A. Lau et al.   AMERICAN JOURNAL OF TRANSPLANTATION

Necroptosis in Immunity and Ischemia-Reperfusion Injury

(2013) A. Linkermann et al.   AMERICAN JOURNAL OF TRANSPLANTATION

Control of Life-or-Death Decisions by RIP1 Kinase

(2013) Dana E Christofferson et al.   Annual Review of Physiology

Crosstalk between apoptosis, necrosis and autophagy

(2013) Vassiliki Nikoletopoulou et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

Programmed necrosis, not apoptosis, is a key mediator of cell loss and DAMP-mediated inflammation in dsRNA-induced retinal degeneration

(2013) Y Murakami 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

Necroptosis: The Release of Damage-Associated Molecular Patterns and Its Physiological Relevance

(2013) Agnieszka Kaczmarek et al.   IMMUNITY

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

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

Plasma membrane translocation of trimerized MLKL protein is required for TNF-induced necroptosis

(2013) Zhenyu Cai et al.   NATURE CELL BIOLOGY

A Phase 2 Trial of Ponatinib in Philadelphia Chromosome–Positive Leukemias

(2013) J.E. Cortes et al.   NEW ENGLAND JOURNAL OF MEDICINE

Two independent pathways of regulated necrosis mediate ischemia-reperfusion injury

(2013) A. Linkermann et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

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

(2013) D. M. Molina et al.   SCIENCE

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

A Role of RIP3-Mediated Macrophage Necrosis in Atherosclerosis Development

(2013) Juan Lin et al.   Cell Reports

Inhibition of RIP1-dependent necrosis prevents adverse cardiac remodeling after myocardial ischemia–reperfusion in vivo

(2012) Martinus I. F. J. Oerlemans et al.   BASIC RESEARCH IN CARDIOLOGY

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

(2012) Liming Sun et al.   CELL

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

(2012) Jixi Li et al.   CELL

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

Pazopanib for metastatic soft-tissue sarcoma (PALETTE): a randomised, double-blind, placebo-controlled phase 3 trial

(2012) Winette TA van der Graaf et al.   LANCET

Ponatinib in Refractory Philadelphia Chromosome–Positive Leukemias

(2012) Jorge E. Cortes et al.   NEW ENGLAND JOURNAL OF MEDICINE

Programmed Cell Death in Animal Development and Disease

(2011) Yaron Fuchs et al.   CELL

An integrated approach to dissecting oncogene addiction implicates a Myb-coordinated self-renewal program as essential for leukemia maintenance

(2011) J. Zuber et al.   GENES & DEVELOPMENT

Comprehensive analysis of kinase inhibitor selectivity

(2011) Mindy I Davis et al.   NATURE BIOTECHNOLOGY

Dedifferentiation, transdifferentiation and reprogramming: three routes to regeneration

(2011) Chris Jopling et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Toll-like receptors activate programmed necrosis in macrophages through a receptor-interacting kinase-3-mediated pathway

(2011) S. He et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Virus Inhibition of RIP3-Dependent Necrosis

(2010) Jason W. Upton et al.   Cell Host & Microbe

Pazopanib in Renal Cell Carcinoma

(2010) J. E. Ward et al.   CLINICAL CANCER RESEARCH

Pazopanib in Locally Advanced or Metastatic Renal Cell Carcinoma: Results of a Randomized Phase III Trial

(2010) Cora N. Sternberg et al.   JOURNAL OF CLINICAL ONCOLOGY

Modeling Contaminants in AP-MS/MS Experiments

(2010) Mathieu Lavallée-Adam et al.   JOURNAL OF PROTEOME RESEARCH

AP24534, a Pan-BCR-ABL Inhibitor for Chronic Myeloid Leukemia, Potently Inhibits the T315I Mutant and Overcomes Mutation-Based Resistance

(2009) Thomas O'Hare et al.   CANCER CELL

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

Phase I Trial of Pazopanib in Patients with Advanced Cancer

(2009) H. I. Hurwitz et al.   CLINICAL CANCER RESEARCH

DAI/ZBP1 recruits RIP1 and RIP3 through RIP homotypic interaction motifs to activate NF-κB

(2009) Manuele Rebsamen et al.   EMBO REPORTS

Efficacy and Safety of Pazopanib in Patients With Metastatic Renal Cell Carcinoma

(2009) Thomas E. Hutson et al.   JOURNAL OF CLINICAL ONCOLOGY

Target profiling of small molecules by chemical proteomics

(2009) Uwe Rix et al.   Nature Chemical Biology

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

(2009) D.-W. Zhang et al.   SCIENCE

Discovery of 5-[[4-[(2,3-Dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a Novel and Potent Vascular Endothelial Growth Factor Receptor Inhibitor†

(2008) Philip A. Harris et al.   JOURNAL OF MEDICINAL CHEMISTRY

Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells

(2008) L L Remsing Rix et al.   LEUKEMIA

Target spectrum of the BCR-ABL inhibitors imatinib, nilotinib and dasatinib

(2008) Oliver Hantschel et al.   LEUKEMIA & LYMPHOMA

Identification of RIP1 kinase as a specific cellular target of necrostatins

(2008) Alexei Degterev et al.   Nature Chemical Biology