Discovery of Clinical Candidate GDC-8264, a Novel, Potent and Selective RIP1 Inhibitor for Amelioration of Tissue Damage and the Treatment of Inflammatory Diseases.
Sign Up to like & getrecommendations! Published in 2025 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.5c01891
Abstract: Receptor-interacting protein 1 (RIP1) is a critical regulator of inflammatory cell death induced by diverse stimuli including TNF family ligands and ischemic injury. As such, the inhibition of RIP1 with small molecule kinase inhibitors is… read more here.
Keywords: rip1; tissue damage; inflammatory; gdc 8264 ... See more keywords
RIP1 inhibition blocks inflammatory diseases but not tumor growth or metastases
Sign Up to like & getrecommendations! Published in 2019 at "Cell Death and Differentiation"
DOI: 10.1038/s41418-019-0347-0
Abstract: The kinase RIP1 acts in multiple signaling pathways to regulate inflammatory responses and it can trigger both apoptosis and necroptosis. Its kinase activity has been implicated in a range of inflammatory, neurodegenerative, and oncogenic diseases.… read more here.
Keywords: rip1 inhibition; rip1; inhibition blocks; tumor growth ... See more keywords
TNF Signaling through RIP1 Kinase Enhances SN38-Induced Death in Colon Adenocarcinoma
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DOI: 10.1158/1541-7786.mcr-16-0329
Abstract: Elucidation of TNF-directed mechanisms for cell death induction and maintenance of tumor growth has revealed a role for receptor-interacting protein kinases 1 and 3 (RIPK1/RIP1 and RIPK3/RIP3), components of the necrosome complex, as determinants of… read more here.
Keywords: death; tnf; tnf signaling; colon ... See more keywords
Cooperative inhibition of RIP1-mediated NF-κB signaling by cytomegalovirus-encoded deubiquitinase and inactive homolog of cellular ribonucleotide reductase large subunit
Sign Up to like & getrecommendations! Published in 2017 at "PLoS Pathogens"
DOI: 10.1371/journal.ppat.1006423
Abstract: Several viruses have been found to encode a deubiquitinating protease (DUB). These viral DUBs are proposed to play a role in regulating innate immune or inflammatory signaling. In human cytomegalovirus (HCMV), the largest tegument protein… read more here.
Keywords: inactive homolog; infection; cytomegalovirus; rip1 mediated ... See more keywords
RIP1 is a central signaling protein in regulation of TNF-α/TRAIL mediated apoptosis and necroptosis during Newcastle disease virus infection
Sign Up to like & getrecommendations! Published in 2017 at "Oncotarget"
DOI: 10.18632/oncotarget.17970
Abstract: Newcastle disease virus (NDV) is an oncolytic virus which selectively replicates in tumor cells and exerts anti-tumor cytotoxic activity by promoting cell death. In this study, we focus on characterization of the underlying mechanisms of… read more here.
Keywords: tnf trail; infection; rip1; apoptosis ... See more keywords
RIP1 Perturbation Induces Chondrocyte Necroptosis and Promotes Osteoarthritis Pathogenesis via Targeting BMP7
Sign Up to like & getrecommendations! Published in 2021 at "Frontiers in Cell and Developmental Biology"
DOI: 10.3389/fcell.2021.638382
Abstract: Osteoarthritis (OA) is a highly prevalent and debilitating joint disorder that characterized by progressive destruction of articular cartilage. There is no effective disease-modifying therapy for the condition due to limited understanding of the molecular mechanisms… read more here.
Keywords: chondrocyte necroptosis; necroptosis; pathogenesis; rip1 perturbation ... See more keywords
Induction of Breast Cancer Cell Apoptosis by TRAIL and Smac Mimetics: Involvement of RIP1 and cFLIP
Sign Up to like & getrecommendations! Published in 2022 at "Current Issues in Molecular Biology"
DOI: 10.3390/cimb44100327
Abstract: Smac mimetics are a group of compounds able to facilitate cell death in cancer cells. TNF-related apoptosis-inducing ligand (TRAIL) is a death receptor ligand currently explored in combination with Smac mimetics. The molecular mechanisms determining… read more here.
Keywords: trail; cell; smac mimetics; apoptosis ... See more keywords