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

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

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

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

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

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

Ubiquitination of RIPK1 regulates its activation mediated by TNFR1 and TLRs signaling in distinct manners

(2020) Xingyan Li et al.   Nature Communications

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

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

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

Cleavage of RIPK1 by caspase-8 is crucial for limiting apoptosis and necroptosis

(2019) Kim Newton et al.   NATURE

Small-Molecule Inhibitors of Necroptosis: Current Status and Perspectives

(2019) Chunlin Zhuang 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

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

(2018) Wei Wang et al.   CANCER CELL

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

RIPK1-RIPK3-MLKL-dependent necrosis promotes the aging of mouse male reproductive system

(2017) Dianrong Li et al.   eLife

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

Control of Life-or-Death Decisions by RIP1 Kinase

(2013) Dana E Christofferson et al.   Annual Review of Physiology

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

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

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

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

(2012) Liming Sun et al.   CELL

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

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

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

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