Structure-Based Design of Novel Alkynyl Thio-Benzoxazepinone Receptor-Interacting Protein Kinase-1 Inhibitors: Extending the Chemical Space from the Allosteric to ATP Binding Pockets

Targeting Necroptosis as a Promising Therapy for Alzheimer’s Disease

(2022) Wenli Zhao et al.   ACS Chemical Neuroscience

Investigation on the chemical space of the substituted triazole thio-benzoxazepinone RIPK1 inhibitors

(2022) Yanan Hao et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

The regulation of necroptosis by ubiquitylation

(2022) Yiliang Chen et al.   APOPTOSIS

Structure-based optimizations of a necroptosis inhibitor (SZM594) as novel protective agents of acute lung injury

(2021) Lijuan Xu et al.   CHINESE CHEMICAL LETTERS

Structure-based bioisosterism design of thio-benzoxazepinones as novel necroptosis inhibitors

(2021) Chunnian Xia et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Necroptosis: A Novel Pathway in Neuroinflammation

(2021) Ziyu Yu et al.   Frontiers in Pharmacology

Discovery of a cooperative mode of inhibiting RIPK1 kinase

(2021) Huyan Meng et al.   Cell Discovery

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

(2021) Xiangbo Yang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Ligand-based substituent-anchoring design of selective receptor-interacting protein kinase 1 necroptosis inhibitors for ulcerative colitis therapy

(2021) Jing Zhu et al.   Acta Pharmaceutica Sinica B

Targeting necroptosis in anticancer therapy: mechanisms and modulators

(2020) Ying Wu et al.   Acta Pharmaceutica Sinica B

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

Radiosensitization of human pancreatic cancer by piperlongumine analogues

(2020) Hao Ma et al.   CHINESE CHEMICAL LETTERS

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

(2019) Xiaofei Chen et al.   BRITISH JOURNAL OF PHARMACOLOGY

RIP1 inhibition blocks inflammatory diseases but not tumor growth or metastases

(2019) Snahel Patel et al.   CELL DEATH AND DIFFERENTIATION

N-(7-Cyano-6-(4-fluoro-3-(2-(3-(trifluoromethyl)phenyl)acetamido)phenoxy)benzo[d]thiazol-2-yl)cyclopropanecarboxamide (TAK-632) Analogues as Novel Necroptosis Inhibitors by Targeting Receptor-Interacting Protein Kinase 3 (RIPK3): Synthesis, Structure–Activity Relationships, and in Vivo Efficacy

(2019) Hao Zhang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identification of a RIP1 Kinase Inhibitor Clinical Candidate (GSK3145095) for the Treatment of Pancreatic Cancer

(2019) Philip A. Harris et al.   ACS Medicinal Chemistry Letters

Small-Molecule Inhibitors of Necroptosis: Current Status and Perspectives

(2019) Chunlin Zhuang et al.   JOURNAL OF MEDICINAL CHEMISTRY

RIP kinase 1–dependent endothelial necroptosis underlies systemic inflammatory response syndrome

(2018) Matija Zelic et al.   JOURNAL OF CLINICAL INVESTIGATION

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

TBK1 Suppresses RIPK1-Driven Apoptosis and Inflammation during Development and in Aging

(2018) Daichao Xu et al.   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

RIPK1 mediates a disease-associated microglial response in Alzheimer’s disease

(2017) Dimitry Ofengeim et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

RIPK1 mediates axonal degeneration by promoting inflammation and necroptosis in ALS

(2016) Yasushi Ito et al.   SCIENCE

Activation of Necroptosis in Multiple Sclerosis

(2015) Dimitry Ofengeim et al.   Cell Reports

Activity of Protein Kinase RIPK3 Determines Whether Cells Die by Necroptosis or Apoptosis

(2014) K. Newton et al.   SCIENCE

Interferon-induced RIP1/RIP3-mediated necrosis requires PKR and is licensed by FADD and caspases

(2013) R. J. Thapa et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

RIP Kinase-Dependent Necrosis Drives Lethal Systemic Inflammatory Response Syndrome

(2011) Linde Duprez et al.   IMMUNITY

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

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

(2011) Sam I. McNeal et al.   SHOCK

Tumor necrosis factor-mediated cell death: to break or to burst, that’s the question

(2010) Franky Van Herreweghe et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

Circulating mitochondrial DAMPs cause inflammatory responses to injury

(2010) Qin Zhang et al.   NATURE

Phosphorylation-Driven Assembly of the RIP1-RIP3 Complex Regulates Programmed Necrosis and Virus-Induced Inflammation

(2009) YoungSik Cho et al.   CELL

Identification of RIP1 kinase as a specific cellular target of necrostatins

(2008) Alexei Degterev et al.   Nature Chemical Biology