title: Lipid raft-like liposomes used for targeted delivery of a chimeric entry-inhibitor peptide with anti-HIV-1 activity.
abstract: The work reports the design and synthesis of a chimeric peptide that is composed of the peptide sequences of two entry inhibitors which target different sites of HIV-1 gp41. The chimeric peptide offers the advantage of targeting two gp41 regions simultaneously: the fusion peptide and the loop both of which are membrane active and participate in the membrane fusion process. We therefore use lipid raft-like liposomes as a tool to specifically direct the chimeric inhibitor peptide to the membrane domains where the HIV-1 envelope protein is located. Moreover, the liposomes that mimic the viral membrane composition protect the chimeric peptide against proteolytic digestion thereby increasing the stability of the peptide. The described liposome preparations are suitable nanosystems for managing hydrophobic entry-inhibitor peptides as putative therapeutics.
authors: Unit of Synthesis and Biomedical Applications of Peptides, IQAC-CSIC, Barcelona, Spain. Electronic address: mariajose.gomara@iqac.csic.es.
authors: María José
authors: MJ
authors: Gómara
authors: Unit of Synthesis and Biomedical Applications of Peptides, IQAC-CSIC, Barcelona, Spain.
authors: Ignacio
authors: I
authors: Pérez-Pomeda
authors: AIDS Research Unit, Institut d'Investigacions Biomèdiques August Pi i Sunyer; HIVACAT, Barcelona, Spain; Infectious Diseases Unit, HIVACAT, Hospital Clinic, Barcelona, Spain.
authors: José María
authors: JM
authors: Gatell
authors: AIDS Research Unit, Institut d'Investigacions Biomèdiques August Pi i Sunyer; HIVACAT, Barcelona, Spain.
authors: Victor
authors: V
authors: Sánchez-Merino
authors: AIDS Research Unit, Institut d'Investigacions Biomèdiques August Pi i Sunyer; HIVACAT, Barcelona, Spain.
authors: Eloisa
authors: E
authors: Yuste
authors: Unit of Synthesis and Biomedical Applications of Peptides, IQAC-CSIC, Barcelona, Spain. Electronic address: isabel.haro@iqac.csic.es.
authors: Isabel
authors: I
authors: Haro
mesh_terms: D000595:Amino Acid Sequence; D015700:HIV Envelope Protein gp41; D015658:HIV Infections / Q000188:drug therapy*; D015497:HIV-1; D006801:Humans; D008055:Lipids; D008081:Liposomes; D010455:Peptides
chemical_list: D015700:HIV Envelope Protein gp41; D008055:Lipids; D008081:Liposomes; D010455:Peptides
keywords: Chimeric peptide; Entry inhibitor peptide; HIV-1; Lipid raft-like liposomes; Targeted delivery