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

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

Ring Closure Strategy Leads to Potent RIPK3 Inhibitors

(2021) Shuwei Wu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Enantiomeric profiling of a chiral benzothiazole necroptosis inhibitor

(2021) Jing Zhu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

(2021) Lijuan Xu et al.   CHINESE CHEMICAL LETTERS

Discovery of a cooperative mode of inhibiting RIPK1 kinase

(2021) Huyan Meng et al.   Cell Discovery

Human RIPK3 maintains MLKL in an inactive conformation prior to cell death by necroptosis

(2021) Yanxiang Meng et al.   Nature Communications

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

Inhibitors of RIP1 kinase: a patent review (2016–present)

(2020) Philip A. Harris   EXPERT OPINION ON THERAPEUTIC PATENTS

Discovery of a Potent RIPK3 Inhibitor for the Amelioration of Necroptosis-Associated Inflammatory Injury

(2020) Kaijiang Xia et al.   Frontiers in Cell and Developmental Biology

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 RIPK3 Type II Inhibitors Using High-Throughput Mechanistic Studies in Hit Triage

(2019) Amy C. Hart et al.   ACS Medicinal Chemistry Letters

Discovery of potent necroptosis inhibitors targeting RIPK1 kinase activity for the treatment of inflammatory disorder and cancer metastasis

(2019) Jue Hou et al.   Cell Death & Disease

DNL 104, a Centrally Penetrant RIPK 1 Inhibitor, Inhibits RIP 1 Kinase Phosphorylation in a Randomized Phase I Ascending Dose Study in Healthy Volunteers

(2019) Hendrika W. Grievink et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Small-Molecule Inhibitors of Necroptosis: Current Status and Perspectives

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

Tozasertib Analogues as Inhibitors of Necroptotic Cell Death

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

RIPK1-dependent cell death: a novel target of the Aurora kinase inhibitor Tozasertib (VX-680)

(2018) Sofie Martens et al.   Cell Death & Disease

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

ATP-Competitive MLKL Binders Have No Functional Impact on Necroptosis

(2016) Bin Ma et al.   PLoS One

A cellular screen identifies ponatinib and pazopanib as inhibitors of necroptosis

(2015) A Fauster et al.   Cell Death & Disease

The B-RafV600E inhibitor dabrafenib selectively inhibits RIP3 and alleviates acetaminophen-induced liver injury

(2014) J-X Li et al.   Cell Death & Disease

Through the “Gatekeeper Door”: Exploiting the Active Kinase Conformation

(2009) Fabio Zuccotto et al.   JOURNAL OF MEDICINAL CHEMISTRY