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RIPK2 relays alarm signals from the NOD1 and NOD2 sensors that detect bacteria, switching on inflammation. It has been proposed as a cancer target both for its effects on immune cells and, in prostate cancer, for helping tumours spread; a RIPK2 inhibitor is in an early melanoma trial.
RIPK2 (chromosome 8q21.3) is a kinase that is the key effector of the NOD1 and NOD2 bacterial sensors: once recruited it is polyubiquitinated and becomes a scaffold for downstream signalling, modulating innate and adaptive immune responses (UniProt O43353). A 2022 Nature Communications study reported RIPK2 amplified or gained in about 65% of lethal metastatic castration-resistant prostate cancers, found that it stabilises c-Myc through MKK7, and showed that its knockout or inhibition reduced prostate cancer metastasis in models (Yan et al., doi:10.1038/s41467-022-28340-6). In OnCo, OPM-101 is an oral RIPK2 inhibitor that blocks the NOD2/RIPK2 pathway, which its developer says is designed to reprogram immune responses in cancer, in a phase 1 trial in melanoma.
In plain words · RIPK2 relays alarm signals from the NOD1 and NOD2 sensors that detect bacteria, switching on inflammation. It has been proposed as a cancer target both for its effects on immune cells and, in prostate cancer, for helping tumours spread; a RIPK2 inhibitor is in an early melanoma trial.
RIPK2 relays alarm signals from the NOD1 and NOD2 sensors that detect bacteria, switching on inflammation. It has been proposed as a cancer target both for its effects on immune cells and, in prostate cancer, for helping tumours spread; a RIPK2 inhibitor is in an early melanoma trial.
Serine/threonine/tyrosine kinase recruited to NOD1 and NOD2 through CARD-CARD interaction; it forms filaments and is polyubiquitinated by XIAP, BIRC2, BIRC3 and LUBAC, becoming a scaffold for downstream signalling (UniProt O43353).
1 product aims at RIPK2: small molecules. Kinases are switched on by binding ATP inside the cell, so most drugs are small molecules shaped to plug that ATP pocket.
Serine/threonine/tyrosine kinase recruited to NOD1 and NOD2 through CARD-CARD interaction; it forms filaments and is polyubiquitinated by XIAP, BIRC2, BIRC3 and LUBAC, becoming a scaffold for downstream signalling (UniProt O43353).
OPM-101 is an experimental oral small-molecule kinase inhibitor from Oncodesign Precision Medicine, in phase 1 trials for advanced melanoma resistant to anti-PD-1.
Query for this target: (TITLE:"RIPK2" OR ABSTRACT:"RIPK2" OR TITLE:"receptor interacting serine/threonine kinase 2" OR ABSTRACT:"receptor interacting serine/threonine kinase 2" OR TITLE:"RIP2" OR ABSTRACT:"RIP2" OR TITLE:"RICK" OR ABSTRACT:"RICK") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about RIPK2, not a curated reading list.
Shares Metastatic castration-resistant prostate cancer and the tag pipeline-gap-target.
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