Identification of a novel class of RIP1/RIP3 dual inhibitors that impede cell death and inflammation in mouse abdominal aortic aneurysm models

Dabrafenib, an inhibitor of RIP3 kinase-dependent necroptosis, reduces ischemic brain injury

(2018) Hsiao-Huei Chen et al.   Neural Regeneration Research

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

Genetic Inhibition of Receptor Interacting Protein Kinase-1 Reduces Cell Death and Improves Functional Outcome After Intracerebral Hemorrhage in Mice

(2017) Sevda Lule et al.   STROKE

Complex Pathologic Roles of RIPK1 and RIPK3: Moving Beyond Necroptosis

(2017) Kelby W. Wegner et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Progress towards a public chemogenomic set for protein kinases and a call for contributions

(2017) David H. Drewry et al.   PLoS One

Inhibition of Receptor-Interacting Protein Kinase 1 with Necrostatin–1s ameliorates disease progression in elastase-induced mouse abdominal aortic aneurysm model

(2017) Qiwei Wang et al.   Scientific Reports

Hypoxia-inducible factor-1 alpha is involved in RIP-induced necroptosis caused by in vitro and in vivo ischemic brain injury

(2017) Xiao-Sa Yang et al.   Scientific Reports

Necroptosis and Inflammation

(2016) Kim Newton et al.   Annual Review of Biochemistry

K45A mutation of RIPK1 results in poor necroptosis and cytokine signaling in macrophages, which impacts inflammatory responses in vivo

(2016) B Shutinoski et al.   CELL DEATH AND DIFFERENTIATION

RIPK3 deficiency or catalytically inactive RIPK1 provides greater benefit than MLKL deficiency in mouse models of inflammation and tissue injury

(2016) K Newton et al.   CELL DEATH AND DIFFERENTIATION

The Role of the PERK/eIF2α/ATF4/CHOP Signaling Pathway in Tumor Progression During Endoplasmic Reticulum Stress

(2016) W. Rozpedek et al.   CURRENT MOLECULAR MEDICINE

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

CaMKII is a RIP3 substrate mediating ischemia- and oxidative stress–induced myocardial necroptosis

(2016) Ting Zhang et al.   NATURE MEDICINE

Regulated necrosis: disease relevance and therapeutic opportunities

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

Targeting macrophage necroptosis for therapeutic and diagnostic interventions in atherosclerosis

(2016) D. Karunakaran et al.   Science Advances

Characterization of RIPK3-mediated phosphorylation of the activation loop of MLKL during necroptosis

(2015) D A Rodriguez et al.   CELL DEATH AND DIFFERENTIATION

Receptor-Interacting Protein Kinase 3 Contributes to Abdominal Aortic Aneurysms via Smooth Muscle Cell Necrosis and Inflammation

(2015) Q. Wang et al.   CIRCULATION RESEARCH

Thrombospondin-1 (TSP1) Contributes to the Development of Vascular Inflammation by Regulating Monocytic Cell Motility in Mouse Models of Abdominal Aortic AneurysmNovelty and Significance

(2015) Zhenjie Liu et al.   CIRCULATION RESEARCH

RIP3-mediated necrotic cell death accelerates systematic inflammation and mortality

(2015) Lingjun Meng et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

RIPK1 and RIPK3: critical regulators of inflammation and cell death

(2015) Kim Newton   TRENDS IN CELL BIOLOGY

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

Activation of Necroptosis in Multiple Sclerosis

(2015) Dimitry Ofengeim et al.   Cell Reports

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

(2014) James A. Rickard 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

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

(2014) Apostolos Polykratis et al.   JOURNAL OF IMMUNOLOGY

RIP3 Induces Apoptosis Independent of Pronecrotic Kinase Activity

(2014) Pratyusha Mandal et al.   MOLECULAR CELL

RNA viruses promote activation of the NLRP3 inflammasome through a RIP1-RIP3-DRP1 signaling pathway

(2014) Xiaqiong Wang et al.   NATURE IMMUNOLOGY

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

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

Monocyte Chemoattractant Protein-1 (MCP-1) Regulates Macrophage Cytotoxicity in Abdominal Aortic Aneurysm

(2014) Qiwei Wang et al.   PLoS One

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

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

Sequence Determinants of a Specific Inactive Protein Kinase Conformation

(2013) Sanjay B. Hari et al.   CHEMISTRY & BIOLOGY

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

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

Regulation of RIP1 kinase signalling at the crossroads of inflammation and cell death

(2013) Dimitry Ofengeim et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Profile of the GSK Published Protein Kinase Inhibitor Set Across ATP-Dependent and-Independent Luciferases: Implications for Reporter-Gene Assays

(2013) Patricia Dranchak et al.   PLoS One

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

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

Discovery of 7-Methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a Potent and Selective First-in-Class Inhibitor of Protein Kinase R (PKR)-like Endoplasmic Reticulum Kinase (PERK)

(2012) Jeffrey M. Axten et al.   JOURNAL OF MEDICINAL CHEMISTRY

Accelerated aneurysmal dilation associated with apoptosis and inflammation in a newly developed calcium phosphate rodent abdominal aortic aneurysm model

(2012) Dai Yamanouchi et al.   JOURNAL OF VASCULAR SURGERY

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

(2011) Sharon Biton et al.   CELL

Effects of Caspase Inhibitor on Angiotensin II-Induced Abdominal Aortic Aneurysm in Apolipoprotein E–Deficient Mice

(2010) Dai Yamanouchi et al.   ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY

Type-II Kinase Inhibitor Docking, Screening, and Profiling Using Modified Structures of Active Kinase States

(2008) Irina Kufareva et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identification of RIP1 kinase as a specific cellular target of necrostatins

(2008) Alexei Degterev et al.   Nature Chemical Biology