Insight from Linker Investigations: Discovery of a Novel Phenylbenzothiazole Necroptosis Inhibitor Targeting Receptor-Interacting Protein Kinase 1 (RIPK1) from a Phenoxybenzothiazole Compound with Dual RIPK1/3 Targeting Activity

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

(2023) Danni Quan et al.   Journal of Medicinal Chemistry

Regulatory T cell and macrophage crosstalk in acute lung injury: future perspectives

(2023) Tianshu Guan et al.   Cell Death Discovery

Cpd‐42 Alleviates Acute Kidney Injury via Targeting RIPK3‐mediated Necroptosis

(2023) Xiao‐yan He et al.   BRITISH JOURNAL OF PHARMACOLOGY

Receptor-interacting protein kinase 1 (RIPK1) inhibitor: a review of the patent literature (2018-present)

(2023) Lijuan Xu et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Protective Effect of a Novel RIPK1 Inhibitor, Compound 4–155, in Systemic Inflammatory Response Syndrome and Sepsis

(2023) Zhong-Yi Ling et al.   INFLAMMATION

Targeting Receptor-Interacting Protein Kinase 1 by Novel Benzothiazole Derivatives: Treatment of Acute Lung Injury through the Necroptosis Pathway

(2023) Xinqi Zhang et al.   Journal of Medicinal Chemistry

Profiling of small‐molecule necroptosis inhibitors based on the subpockets of kinase–ligand interactions

(2023) Lijuan Xu et al.   MEDICINAL RESEARCH REVIEWS

Analysis on benzothiazole necroptosis inhibitors with chiral substitutions in the solvent-accessible region of RIP kinase domain

(2023) Hongming Shao et al.   BIOORGANIC CHEMISTRY

Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK

(2022) Li Ding et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

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

Profiling of the chemical space on the phenyl group of substituted benzothiazole RIPK3 inhibitors

(2022) Yue Xu et al.   BIOORGANIC CHEMISTRY

Discovery of a Trifluoromethoxy Cyclopentanone Benzothiazole Receptor-Interacting Protein Kinase 1 Inhibitor as the Treatment for Alzheimer’s Disease

(2022) Yi Sun et al.   Journal of Medicinal Chemistry

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

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

Renin–Angiotensin–Aldosterone System Inhibitors in Patients with Covid-19

(2020) Muthiah Vaduganathan et al.   NEW ENGLAND JOURNAL OF MEDICINE

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

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

Microglia-targeted candidates push the Alzheimer drug envelope

(2018) Asher Mullard   NATURE REVIEWS DRUG DISCOVERY

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

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

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

Programmed necrosis in inflammation: Toward identification of the effector molecules

(2016) D. Wallach et al.   SCIENCE

Necroptosis and its role in inflammation

(2015) Manolis Pasparakis et al.   NATURE

The diverse role of RIP kinases in necroptosis and inflammation

(2015) John Silke et al.   NATURE IMMUNOLOGY

RIPK1 and RIPK3: critical regulators of inflammation and cell death

(2015) Kim Newton   TRENDS IN CELL BIOLOGY

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

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

(2013) Zhenyu Cai et al.   NATURE CELL BIOLOGY

A Role of RIP3-Mediated Macrophage Necrosis in Atherosclerosis Development

(2013) Juan Lin et al.   Cell Reports

Many stimuli pull the necrotic trigger, an overview

(2011) N Vanlangenakker et al.   CELL DEATH AND DIFFERENTIATION

RIP Kinase-Dependent Necrosis Drives Lethal Systemic Inflammatory Response Syndrome

(2011) Linde Duprez et al.   IMMUNITY

Comprehensive analysis of kinase inhibitor selectivity

(2011) Mindy I Davis et al.   NATURE BIOTECHNOLOGY

Necroptosis as an alternative form of programmed cell death

(2010) Dana E Christofferson et al.   CURRENT OPINION IN CELL BIOLOGY

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

(2009) YoungSik Cho et al.   CELL

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