Potent and Selective RIPK1 Inhibitors Targeting Dual‐Pockets for the Treatment of Systemic Inflammatory Response Syndrome and Sepsis

Global, regional, and national sepsis incidence and mortality, 1990–2017: analysis for the Global Burden of Disease Study

(2020) Kristina E Rudd et al.   LANCET

Receptor-interacting protein kinase 1 (RIPK1) as a therapeutic target

(2020) Lauren Mifflin et al.   NATURE REVIEWS DRUG DISCOVERY

Glucocorticoids in Sepsis: To Be or Not to Be

(2020) Jolien Vandewalle et al.   Frontiers in Immunology

Discovery and Lead-Optimization of 4,5-Dihydropyrazoles as Mono-Kinase Selective, Orally Bioavailable and Efficacious Inhibitors of Receptor Interacting Protein 1 (RIP1) Kinase

(2019) Philip A. Harris et al.   JOURNAL OF MEDICINAL CHEMISTRY

Targeting RIPK1 for the treatment of human diseases

(2019) Alexei Degterev et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Tozasertib Analogues as Inhibitors of Necroptotic Cell Death

(2018) Sam Hofmans et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of 7-Oxo-2,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridine Derivatives as Potent, Orally Available, and Brain-Penetrating Receptor Interacting Protein 1 (RIP1) Kinase Inhibitors: Analysis of Structure–Kinetic Relationships

(2018) Masato Yoshikawa et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identification of 5-(2,3-Dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine Derivatives as a New Class of Receptor-Interacting Protein Kinase 1 (RIPK1) Inhibitors, Which Showed Potent Activity in a Tumor Metastasis Model

(2018) Yueshan Li et al.   JOURNAL OF MEDICINAL CHEMISTRY

Necroptosis and RIPK1-mediated neuroinflammation in CNS diseases

(2018) Junying Yuan et al.   NATURE REVIEWS NEUROSCIENCE

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

Necroptosis in neurodegenerative diseases: a potential therapeutic target

(2017) Shuo Zhang et al.   Cell Death & Disease

Necroptosis and Inflammation

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

The Third International Consensus Definitions for Sepsis and Septic Shock (Sepsis-3)

(2016) Mervyn Singer et al.   JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION

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

Classification of small molecule protein kinase inhibitors based upon the structures of their drug-enzyme complexes

(2016) Robert Roskoski   PHARMACOLOGICAL RESEARCH

Necroptosis and its role in inflammation

(2015) Manolis Pasparakis et al.   NATURE

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

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

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

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

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

Type I interferon induces necroptosis in macrophages during infection with Salmonella enterica serovar Typhimurium

(2012) Nirmal Robinson et al.   NATURE IMMUNOLOGY

RIP Kinase-Dependent Necrosis Drives Lethal Systemic Inflammatory Response Syndrome

(2011) Linde Duprez et al.   IMMUNITY

The Dual Functions of Receptor Interacting Protein 1 in Fas-Induced Hepatocyte Death During Sepsis

(2011) Sam I. McNeal et al.   SHOCK

Molecular mechanisms of necroptosis: an ordered cellular explosion

(2010) Peter Vandenabeele et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Identification of RIP1 kinase as a specific cellular target of necrostatins

(2008) Alexei Degterev et al.   Nature Chemical Biology