p(RGD:Cdk5)

Entity

Name

Cdk5

Namespace

rgd

Namespace Version

20181021

Namespace URL

https://raw.githubusercontent.com/pharmacome/terminology/f2f993e599694ab5ce989cc39d789a499f75db99/external/rgd-names.belns

Tau Modifications Sections of NESTOR

Small molecules in the diaminothiazole class are potent Tau kinase inhibitors that target CDK5 and GSK3β. Lead compounds from the series have IC50 values toward CDK5/p25 and GSK3β in the low nanomolar range and no observed toxicity in the therapeutic dose range. Neuronal protective effects and decreased PHF-1 immunoreactivity were observed in two animal models, 3×Tg-AD and CK-p25. Treatment nearly eliminated Sarkosyl-insoluble Tau with the most prominent effect on the phosphorylation at Ser-404. Treatment also induced the recovery of memory in a fear conditioning assay. PubMed:23737518

Small molecules in the diaminothiazole class are potent Tau kinase inhibitors that target CDK5 and GSK3β. Lead compounds from the series have IC50 values toward CDK5/p25 and GSK3β in the low nanomolar range and no observed toxicity in the therapeutic dose range. Neuronal protective effects and decreased PHF-1 immunoreactivity were observed in two animal models, 3×Tg-AD and CK-p25. Treatment nearly eliminated Sarkosyl-insoluble Tau with the most prominent effect on the phosphorylation at Ser-404. Treatment also induced the recovery of memory in a fear conditioning assay. PubMed:23737518

Small molecules in the diaminothiazole class are potent Tau kinase inhibitors that target CDK5 and GSK3β. Lead compounds from the series have IC50 values toward CDK5/p25 and GSK3β in the low nanomolar range and no observed toxicity in the therapeutic dose range. Neuronal protective effects and decreased PHF-1 immunoreactivity were observed in two animal models, 3×Tg-AD and CK-p25. Treatment nearly eliminated Sarkosyl-insoluble Tau with the most prominent effect on the phosphorylation at Ser-404. Treatment also induced the recovery of memory in a fear conditioning assay. PubMed:23737518

p39, but not p35, is selectively upregulated by histone acetylation-mediated transcription, underlying the robust increase of Cdk5 activity during rat and mouse neuronal differentiation. Loss of p39 attenuates Cdk5 activity in neurons and preferentially affects phosphorylation of specific Cdk5 targets, leading to aberrant axonal growth and impaired dendritic spine and synapse formation. PubMed:27807169

In NGF-exposed PC12 cells, Egr-1 activates Cdk5 to promote phosphorylation of tau and inactivates PP1 via phosphorylation. Cdk5 phosphorylates Ser(396/404) directly. By phosphorylating and inactivating PP1, Cdk5 promotes tau phosphorylation at Ser(262) indirectly. PubMed:21489990

In NGF-exposed PC12 cells, Egr-1 activates Cdk5 to promote phosphorylation of tau and inactivates PP1 via phosphorylation. Cdk5 phosphorylates Ser(396/404) directly. By phosphorylating and inactivating PP1, Cdk5 promotes tau phosphorylation at Ser(262) indirectly. PubMed:21489990

In NGF-exposed PC12 cells, Egr-1 activates Cdk5 to promote phosphorylation of tau and inactivates PP1 via phosphorylation. Cdk5 phosphorylates Ser(396/404) directly. By phosphorylating and inactivating PP1, Cdk5 promotes tau phosphorylation at Ser(262) indirectly. PubMed:21489990

In NGF-exposed PC12 cells, Egr-1 activates Cdk5 to promote phosphorylation of tau and inactivates PP1 via phosphorylation. Cdk5 phosphorylates Ser(396/404) directly. By phosphorylating and inactivating PP1, Cdk5 promotes tau phosphorylation at Ser(262) indirectly. PubMed:21489990