Axonal and Myelin Neuroprotection by the Peptoid BN201 in Brain Inflammation.
Pablo VillosladaGemma VilaValeria ColafrancescoBeatriz MorenoBegoña Fernandez-DiezRaquel VazquezInna PertsovskayaIrati ZubizarretaIrene Pulido-ValdeolivasJoaquin MesseguerGloria Vendrell-NavarroJose Maria FradeNoelia López-SánchezMeritxell TeixidoErnest GiraltMar MassoJason C DugasDmitri LeonoudakisKaren D Lariosa-WillinghamLawrence SteinmanAngel MesseguerPublished in: Neurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics (2020)
The development of neuroprotective therapies is a sought-after goal. By screening combinatorial chemical libraries using in vitro assays, we identified the small molecule BN201 that promotes the survival of cultured neural cells when subjected to oxidative stress or when deprived of trophic factors. Moreover, BN201 promotes neuronal differentiation, the differentiation of precursor cells to mature oligodendrocytes in vitro, and the myelination of new axons. BN201 modulates several kinases participating in the insulin growth factor 1 pathway including serum-glucocorticoid kinase and midkine, inducing the phosphorylation of NDRG1 and the translocation of the transcription factor Foxo3 to the cytoplasm. In vivo, BN201 prevents axonal and neuronal loss, and it promotes remyelination in models of multiple sclerosis, chemically induced demyelination, and glaucoma. In summary, we provide a new promising strategy to promote neuroaxonal survival and remyelination, potentially preventing disability in brain diseases.
Keyphrases
- induced apoptosis
- cerebral ischemia
- oxidative stress
- multiple sclerosis
- growth factor
- white matter
- transcription factor
- small molecule
- cell cycle arrest
- diabetic rats
- spinal cord injury
- type diabetes
- brain injury
- signaling pathway
- endoplasmic reticulum stress
- subarachnoid hemorrhage
- resting state
- blood brain barrier
- pi k akt
- endothelial cells
- tyrosine kinase
- optic nerve
- protein kinase
- free survival
- metabolic syndrome
- insulin resistance
- weight loss
- heat shock