Discovery of potent necroptosis inhibitors targeting RIPK1 kinase activity for the treatment of inflammatory disorder and cancer metastasis

Discovery of potent and novel smoothened antagonists via structure-based virtual screening and biological assays

(2018) Wenfeng Lu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

RIP kinases as modulators of inflammation and immunity

(2018) Sudan He et al.   NATURE IMMUNOLOGY

RIP1 Kinase Drives Macrophage-Mediated Adaptive Immune Tolerance in Pancreatic Cancer

(2018) Wei Wang et al.   CANCER CELL

Necroptosis and RIPK1-mediated neuroinflammation in CNS diseases

(2018) Junying Yuan et al.   NATURE REVIEWS NEUROSCIENCE

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

MLKL forms disulfide bond-dependent amyloid-like polymers to induce necroptosis

(2017) Shuzhen Liu et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

RIPK1/RIPK3 promotes vascular permeability to allow tumor cell extravasation independent of its necroptotic function

(2017) Kay Hänggi et al.   Cell Death & Disease

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

Tumour-cell-induced endothelial cell necroptosis via death receptor 6 promotes metastasis

(2016) Boris Strilic et al.   NATURE

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

The ubiquitin-modifying enzyme A20 restricts ubiquitination of the kinase RIPK3 and protects cells from necroptosis

(2015) Michio Onizawa et al.   NATURE IMMUNOLOGY

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

(2015) Malek Najjar et al.   Cell Reports

RIP3, a kinase promoting necroptotic cell death, mediates adverse remodelling after myocardial infarction

(2014) Mark Luedde et al.   CARDIOVASCULAR RESEARCH

RIPK1 both positively and negatively regulates RIPK3 oligomerization and necroptosis

(2014) S Orozco et al.   CELL DEATH AND DIFFERENTIATION

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

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

(2014) Huayi Wang et al.   MOLECULAR CELL

Necroptosis in health and diseases

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

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

(2013) Xin Chen et al.   CELL RESEARCH

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

(2013) Zhenyu Cai et al.   NATURE CELL BIOLOGY

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

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

Rip1 (Receptor-interacting protein kinase 1) mediates necroptosis and contributes to renal ischemia/reperfusion injury

(2012) Andreas Linkermann et al.   KIDNEY INTERNATIONAL

Mixed lineage kinase domain-like is a key receptor interacting protein 3 downstream component of TNF-induced necrosis

(2012) J. Zhao et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

RIP Kinase-Dependent Necrosis Drives Lethal Systemic Inflammatory Response Syndrome

(2011) Linde Duprez et al.   IMMUNITY

Synopsis of Some Recent Tactical Application of Bioisosteres in Drug Design

(2011) Nicholas A. Meanwell   JOURNAL OF MEDICINAL CHEMISTRY

The Ripoptosome, a Signaling Platform that Assembles in Response to Genotoxic Stress and Loss of IAPs

(2011) Tencho Tenev et al.   MOLECULAR CELL

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

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

Escape from Flatland: Increasing Saturation as an Approach to Improving Clinical Success

(2009) Frank Lovering et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2009) D.-W. Zhang et al.   SCIENCE

Identification of RIP1 kinase as a specific cellular target of necrostatins

(2008) Alexei Degterev et al.   Nature Chemical Biology