Abstract
Cell-penetrating peptides (CPP), which are short peptides that are capable of crossing the plasma membrane of a living cell, are under development as delivery vehicles for therapeutic agents that cannot themselves enter the cell. One well-studied CPP is the 10-amino acid peptide derived from the human immunodeficiency virus type 1 (HIV-1) Tat protein. In experiments to test the hypothesis that multiple cationic amino acids within Tat peptide confer antiviral activity against HIV-1, introduction of Tat peptide resulted in concentration-dependent inhibition of HIV-1 IIIB infection. Using Tat peptide variants containing arginine substitutions for two nonionic residues and two lysine residues, HIV-1 inhibition experiments demonstrated a direct relationship between cationic charge and antiviral potency. These studies of Tat peptide as an antiviral agent raise new questions about the role of Tat in HIV-1 replication and provide a starting point for the development of CPPs as novel HIV-1 inhibitors.
Highlights
Cell penetrating peptides (CPP) are short peptides that can efficiently cross the plasma membrane, which is otherwise a formidable barrier to many extracellular molecules [1,2,3]
human immunodeficiency virus type 1 (HIV-1)-susceptible P4-R5 MAGI indicator cells were exposed to HIV-1 strain IIIB (0.6 multiplicities of infection (MOI)) for 2 h while in the presence of half log concentrations of Tat peptide up to 1 mg/mL
Results presented in this paper demonstrate that Tat peptide, a CPP that is capable of delivering molecules intracellularly [1, 5] across living membranes, contains intrinsic antiviral activity against HIV-1 infection
Summary
Cell penetrating peptides (CPP) are short peptides that can efficiently cross the plasma membrane, which is otherwise a formidable barrier to many extracellular molecules [1,2,3]. Of the numerous peptides shown to have cell penetrating properties, a 10-amino acid (aa) peptide derived from the human immunodeficiency virus type 1 (HIV-1) Tat protein has been well studied as an effective CPP and an attractive drug delivery agent [5]. A multitude of studies have determined that the activity of the Tat peptide as a CPP involves interactions with the cellular membrane and cytoskeleton [7], and is influenced by numerous variables related to the peptide, the cargo, and extracellular conditions [4]
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