Sibiriline, a new small chemical inhibitor of receptor-interacting protein kinase 1, prevents immune-dependent hepatitis

Discovery of a Highly Potent, Selective, and Metabolically Stable Inhibitor of Receptor-Interacting Protein 1 (RIP1) for the Treatment of Systemic Inflammatory Response Syndrome

(2017) Yan Ren et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases

(2017) Philip A. Harris et al.   JOURNAL OF MEDICINAL CHEMISTRY

Generation of small molecules to interfere with regulated necrosis

(2016) Alexei Degterev et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

Necroptosis inhibitors as therapeutic targets in inflammation mediated disorders - a review of the current literature and patents

(2016) Spandana Rajendra Kopalli et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

The pseudokinase MLKL mediates programmed hepatocellular necrosis independently of RIPK3 during hepatitis

(2016) Claudia Günther et al.   JOURNAL OF CLINICAL INVESTIGATION

DNA-Encoded Library Screening Identifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors

(2016) Philip A. Harris et al.   JOURNAL OF MEDICINAL CHEMISTRY

Regulated necrosis: disease relevance and therapeutic opportunities

(2016) Marcus Conrad et al.   NATURE REVIEWS DRUG DISCOVERY

RIPK1 protects from TNF-α-mediated liver damage during hepatitis

(2016) Aveline Filliol et al.   Cell Death & Disease

Necroptosis is a key pathogenic event in human and experimental murine models of non-alcoholic steatohepatitis

(2015) Marta B. Afonso et al.   CLINICAL SCIENCE

A cellular screen identifies ponatinib and pazopanib as inhibitors of necroptosis

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

Role of necroptosis in the pathogenesis of solid organ injury

(2015) H Zhao 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

A positive feedback loop between RIP3 and JNK controls non-alcoholic steatohepatitis

(2014) J. Gautheron et al.   EMBO Molecular Medicine

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

(2014) Huayi Wang et al.   MOLECULAR CELL

Regulated necrosis: the expanding network of non-apoptotic cell death pathways

(2014) Tom Vanden Berghe et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

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

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

Necrostatin-1 protects against reactive oxygen species (ROS)-induced hepatotoxicity in acetaminophen-induced acute liver failure

(2014) Kenji Takemoto et al.   FEBS Open Bio

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

Synthesis, docking and pharmacological evaluation of novel indole based potential atypical antipsychotics

(2013) Alka Bali et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Receptor interacting protein kinase 3 is a critical early mediator of acetaminophen-induced hepatocyte necrosis in mice

(2013) Anup Ramachandran et al.   HEPATOLOGY

The Pseudokinase MLKL Mediates Necroptosis via a Molecular Switch Mechanism

(2013) James M. Murphy et al.   IMMUNITY

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

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

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

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

Absence of receptor interacting protein kinase 3 prevents ethanol-induced liver injury

(2012) Sanjoy Roychowdhury et al.   HEPATOLOGY

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

RIP Kinase-Dependent Necrosis Drives Lethal Systemic Inflammatory Response Syndrome

(2011) Linde Duprez et al.   IMMUNITY

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

(2011) Andrew Oberst et al.   NATURE

The application of Stille cross-coupling reactions with multiple nitrogen containing heterocycles

(2011) Roland Selig et al.   TETRAHEDRON

Hepatocyte Death: A Clear and Present Danger

(2010) Harmeet Malhi et al.   PHYSIOLOGICAL REVIEWS

TNF-α Induces Two Distinct Caspase-8 Activation Pathways

(2008) Lai Wang et al.   CELL

Identification of RIP1 kinase as a specific cellular target of necrostatins

(2008) Alexei Degterev et al.   Nature Chemical Biology