p(HGNC:BACE1, frag("67_78"))

Entity

Name

BACE1

Namespace

hgnc

Namespace Version

20180906

Namespace URL

https://raw.githubusercontent.com/pharmacome/terminology/b46b65c3da259b6e86026514dfececab7c22a11b/external/hgnc-names.belns

Neither, BI-1 nor, BI-3, nor any of the other peptides used in this study, induced any changes of full-length APP levels. They also did not affect the level of b-actin. PubMed:17293005

Neither, BI-1 nor, BI-3, nor any of the other peptides used in this study, induced any changes of full-length APP levels. They also did not affect the level of b-actin. PubMed:17293005

These results suggest that BACE1 derived peptides do not directly inhibit BACE activities in vitro when the fluorogenic peptides are used as a substrate. PubMed:17293005

BI-1 treatment dose-dependently inhibited the release of both sAPPa and sAPPb in the conditioned medium (Figs. 2A and 3A). The 50% inhibitory concentrations (IC50) of BI-1 were about 1.5 mM for sAPPa and 0.9 mM for APPb, respectively. But BI-2, which is mainly composed of the core region BACE1 69–73, did not show the inhibitory effects PubMed:17293005

Taken together, these results show that BI-1 and BI-3 not only selectively reduce the level of APPbeta but also lead to the accumulation of APPalpha in cells with no change of full-length APP level. PubMed:17293005

BI-1 treatment dose-dependently inhibited the release of both sAPPa and sAPPb in the conditioned medium (Figs. 2A and 3A). The 50% inhibitory concentrations (IC50) of BI-1 were about 1.5 mM for sAPPa and 0.9 mM for APPb, respectively. But BI-2, which is mainly composed of the core region BACE1 69–73, did not show the inhibitory effects PubMed:17293005

Surprisingly, BI-1 treatment resulted in a drastic, dose-dependent increase in the level of intracellular APPa (Figs. 2A and 3A). BI-3 also induced the accumulation of intracellular APPa until the concentration of BI-3 was raised to 12.5 mM; however, treatment of BI-3 with 25 mM decreased the level of intracellular APPa. PubMed:17293005

Taken together, these results show that BI-1 and BI-3 not only selectively reduce the level of APPbeta but also lead to the accumulation of APPalpha in cells with no change of full-length APP level. PubMed:17293005

BI-1 treatment effectively reduced Ab 40 levels (IC50 = 0.06 mM) in the conditioned medium. BI-3 also inhibited Ab 40 production (IC50 = 0.2 mM), although the effective concentrations were relatively high compared to those of BI-1. PubMed:17293005