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

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

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Targeting necroptosis in anticancer therapy: mechanisms and modulators

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

The Bcr-Abl inhibitor GNF-7 inhibits necroptosis and ameliorates acute kidney injury by targeting RIPK1 and RIPK3 kinases

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

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Radiosensitization of human pancreatic cancer by piperlongumine analogues

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Ulcerative colitis

(2020) Taku Kobayashi et al.   Nature Reviews Disease Primers

Hallmarks of Health

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Discovery of bardoxolone derivatives as novel orally active necroptosis inhibitors

(2020) Yuanyuan Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

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

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Targeting RIPK1 for the treatment of human diseases

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

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Small-Molecule Inhibitors of Necroptosis: Current Status and Perspectives

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Necroptosis promotes cell-autonomous activation of proinflammatory cytokine gene expression

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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

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Ulcerative colitis

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RIPK1 and RIPK3 Kinases Promote Cell-Death-Independent Inflammation by Toll-like Receptor 4

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DNA-Encoded Library Screening Identifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors

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Necroptosis and its role in inflammation

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The diverse role of RIP kinases in necroptosis and inflammation

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Necroptosis Is Active in Children With Inflammatory Bowel Disease and Contributes to Heighten Intestinal Inflammation

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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

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

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

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Apoptosis, necrosis and necroptosis: cell death regulation in the intestinal epithelium

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RIP Kinase-Dependent Necrosis Drives Lethal Systemic Inflammatory Response Syndrome

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

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

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Receptor Interacting Protein Kinase-3 Determines Cellular Necrotic Response to TNF-α

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Identification of RIP1 kinase as a specific cellular target of necrostatins

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