Identification of the Raf kinase inhibitor TAK‐632 and its analogues as potent inhibitors of necroptosis by targeting RIPK1 and RIPK3

Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design

(2018) Nicholas A. Meanwell   JOURNAL OF MEDICINAL CHEMISTRY

Origin and Consequences of Necroinflammation

(2018) Maysa Sarhan et al.   PHYSIOLOGICAL REVIEWS

Phenytoin inhibits necroptosis

(2018) Anne von Mässenhausen et al.   Cell Death & Disease

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

The IUPHAR/BPS Guide to PHARMACOLOGY in 2018: updates and expansion to encompass the new guide to IMMUNOPHARMACOLOGY

(2017) Simon D Harding et al.   NUCLEIC ACIDS RESEARCH

Sorafenib tosylate inhibits directly necrosome complex formation and protects in mouse models of inflammation and tissue injury

(2017) Sofie Martens et al.   Cell Death & Disease

Generation of small molecules to interfere with regulated necrosis

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

Fluorination methods for drug discovery and development

(2016) Paul Richardson   Expert Opinion on Drug Discovery

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

Necroptosis in development, inflammation and disease

(2016) Ricardo Weinlich et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Applications of Fluorine in Medicinal Chemistry

(2015) Eric P. Gillis et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

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

(2014) Christopher P. Dillon et al.   CELL

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

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

Antitumor Activity of the Selective Pan-RAF Inhibitor TAK-632 in BRAF Inhibitor-Resistant Melanoma

(2013) A. Nakamura et al.   CANCER RESEARCH

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

Discovery of a Selective Kinase Inhibitor (TAK-632) Targeting Pan-RAF Inhibition: Design, Synthesis, and Biological Evaluation of C-7-Substituted 1,3-Benzothiazole Derivatives

(2013) Masanori Okaniwa et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2013) Zhenyu Cai et al.   NATURE CELL BIOLOGY

Structural Basis of RIP1 Inhibition by Necrostatins

(2013) Tian Xie et al.   STRUCTURE

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

(2012) Liming Sun et al.   CELL

The Role of Src Kinase in Macrophage-Mediated Inflammatory Responses

(2012) Se Eun Byeon et al.   MEDIATORS OF INFLAMMATION

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

Animal research: Reporting in vivo experiments: The ARRIVE guidelines

(2010) Carol Kilkenny et al.   BRITISH JOURNAL OF PHARMACOLOGY

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

Target identification using drug affinity responsive target stability (DARTS)

(2009) B. Lomenick et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Identification of RIP1 kinase as a specific cellular target of necrostatins

(2008) Alexei Degterev et al.   Nature Chemical Biology