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Target intelligence / Profile preview
E3 ubiquitin-protein ligase pellino homolog 1 (Pellino1)
- Target
- Pellino1
- Molecular classification
- Enzyme, E3 ubiquitin ligase, Signal transducer
01
Overview
Pellino1 is an E3 ubiquitin ligase that regulates protein ubiquitination, primarily via K48- and K63-linked chains, impacting signal transduction in immune and inflammatory pathways such as Toll-like receptor, interleukin-1 receptor, and NF-κB signaling. It modulates cell death processes and DNA damage responses, acting as a crucial hub in inflammation, immune tolerance, and cancer development. Pellino1 is implicated in autoimmune diseases (like multiple sclerosis and lupus), infections, and many cancers, making it a validated therapeutic target with ongoing research focused on modulating its E3 ligase activity for disease treatment[1][2][3][4][5][7].
- Other names
- Peli1Pellino E3 ubiquitin ligase 1E3 ubiquitin-protein ligase pellino homolog 1
02
Mechanism of action
Inhibition or modulation of Pellino1 can regulate inflammatory pathways, proinflammatory cytokine production, macrophage migration, and survival/proliferation of cancer cells by interfering with substrate protein ubiquitination[3][4].
03
Biological functions
UbiquitinationSignal transductionImmune responseInflammation regulationCell death (apoptosis, necroptosis, pyroptosis)DNA damage responseCell survival
04
Disease associations
CancerInflammationAutoimmune diseaseInfectionColitisInflammation-related cancer (such as colitis-associated cancer)Neurodegenerative disease (multiple sclerosis)Systemic lupus erythematosus
05
Safety considerations
Targeting Pellino1 could disrupt normal immune and DNA repair functions, leading to risks of immune dysregulation or impaired DNA damage responses[2][3][4].
06
Interacting drugs
None well-established; experimental inhibitors could disrupt Pellino1-STAT3 interactions or target E3 ubiquitin ligase activity[4][3].
07
Biomarkers
Elevated Pellino1 expression in inflammatory diseases and certain cancers may serve as a biomarker for disease prognosis or therapeutic response[3][4].
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