Article ; Online: Arginine-rich membrane-permeable peptides are seriously toxic.
Pharmacology research & perspectives
2018 Volume 5, Issue 5
Abstract: The membrane-permeable peptides (MPP) such as undecapeptides TAT (YGRKKRRQRRR) and CTP (YGRRARRRRRR) have been receiving much attention for delivering various kinds of low membrane-permeability materials in vitro and in vivo. We have successfully used ... ...
Abstract | The membrane-permeable peptides (MPP) such as undecapeptides TAT (YGRKKRRQRRR) and CTP (YGRRARRRRRR) have been receiving much attention for delivering various kinds of low membrane-permeability materials in vitro and in vivo. We have successfully used MPP in carrying various proteins through blood-brain barrier (BBB) in treatment of many kinds of nervous diseases. However, people always concentrate their mind on the efficacy and the mechanism of permeation of the conjugates across BBB, but overlook the toxicity of the membrane-permeable peptide itself. Once we injected intravenously not very large amounts of gamma-aminobutyric acid-MPP (GABA-MPP) to the mice, to our great surprise, the mice died within seconds with seizure, whereas the GABA control mice well survived. Thus, the importance of the toxicity of MPPs and their conjugates comes into the field of our vision. The low LD |
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MeSH term(s) | Animals ; Arginine/chemistry ; Blood-Brain Barrier/drug effects ; Cell Membrane Permeability/drug effects ; Injections, Intravenous ; Lethal Dose 50 ; Mice ; Oligopeptides/chemistry ; Oligopeptides/metabolism ; Oligopeptides/toxicity ; Peptide Fragments/chemistry ; Peptide Fragments/toxicity ; Peptides/chemistry ; Peptides/toxicity ; Structure-Activity Relationship ; gamma-Aminobutyric Acid/administration & dosage ; tat Gene Products, Human Immunodeficiency Virus/chemistry ; tat Gene Products, Human Immunodeficiency Virus/toxicity |
Chemical Substances | Oligopeptides ; Peptide Fragments ; Peptides ; R11 peptide ; tat Gene Products, Human Immunodeficiency Virus ; tat peptide (47-57), Human immunodeficiency virus 1 ; gamma-Aminobutyric Acid (56-12-2) ; Arginine (94ZLA3W45F) |
Language | English |
Publishing date | 2018-01-03 |
Publishing country | United States |
Document type | Journal Article |
ZDB-ID | 2740389-0 |
ISSN | 2052-1707 ; 2052-1707 |
ISSN (online) | 2052-1707 |
ISSN | 2052-1707 |
DOI | 10.1002/prp2.334 |
Database | MEDical Literature Analysis and Retrieval System OnLINE |
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