Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: EC:2.3.1.108 (
TAT
)
2,389
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
A novel peptide
VIP
-
TAT
with a cell penetrating peptide
TAT
at the C-terminus of
VIP
was constructed and prepared using intein mediated purification with an affinity chitin-binding tag (IMPACT) system to enhance the brain uptake efficiency for the medical application in central nervous system. It was found by labeling
VIP
-
TAT
and
VIP
with fluorescein isothiocyanate (FITC) that the extension with
TAT
increased the brain uptake efficiency of
VIP
-
TAT
significantly. Then short-term and long-term treatment with scopolamine (Scop) was used to evaluate the effect of
VIP
-
TAT
or
VIP
on Scop induced amnesia. Both short-term and long-term administration of
VIP
-
TAT
inhibited the latent time reduction in step-through test induced by Scop significantly, but long-term administration of
VIP
aggravated the Scop induced amnesia. Long-term i.p. injection of
VIP
-
TAT
was shown to have positive effect by inhibiting the oxidative damage, apoptosis and the cholinergic system activity reduction that induced by Scop, while
VIP
exerted negative effect in brain opposite to that in periphery system. The in vitro data showed that
VIP
-
TAT
had not only protective but also proliferative effect on Neuro2a cells which was inhibited by PAC1 antagonist PACAP(6-38). Competition binding assay and cAMP assay confirmed that
VIP
-
TAT
had higher affinity and activation for PAC1 than
VIP
. So it was concluded that the significantly stronger protective effect of
VIP
-
TAT
against Scop induced amnesia than
VIP
was due to (1) the enhanced brain uptake efficiency of
VIP
-
TAT
and (2) the increased affinity and activation of
VIP
-
TAT
for receptor PAC1.
...
PMID:Novel peptide VIP-TAT with higher affinity for PAC1 inhibited scopolamine induced amnesia. 2508 67
