Membrane permeability of scaffold peptides for potential use in orally administered anti-HIV drugs

In 2006, there were over 39 million people with Human Immunodeficiency Virus (HIV) worldwide, and 2.9 million HIV-related deaths. Currently, a cocktail of drugs administered via injection (HAART) has some efficacy in treating HIV, but does not eradicate HIV from infected individuals and has long-term side effects. In addition, drug-resistant variants of HIV are emerging. In an effort to help develop orally administered anti-HIV drugs, we examined membrane permeability of four scaffold peptides (synthesized by a researcher at Scripps Florida) into T-cells. One peptide (KE1-72A) entered cells with 100% efficiency; a second (KE1-72B) showed minimal cell penetration. Two other peptides (KE1-72C and KE1-72D), when chemically conjugated to an HIV fusion inhibitor, also showed minimal cell penetration. Further research is needed to determine whether the peptide KE1-72A may potentially be useful in orally delivered anti-HIV drugs.