Document 0693
 DOCN  M9440693
 TI    CD4-modified synthetic peptides containing phenylalanine inhibit HIV-1
       infection in vitro.
 DT    9404
 AU    Lasarte JJ; Sarobe P; Golvano J; Prieto I; Civeira MP; Gullon A; Sarin
       PS; Prieto J; Borras-Cuesta F; Departamento de Medicina Interna,
       Facultad de Medicina,; Universidad de Navarra, Pamplona, Spain.
 SO    J Acquir Immune Defic Syndr. 1994 Feb;7(2):129-34. Unique Identifier :
       AIDSLINE MED/94133081
 AB    Phenylalanine-containing peptides from CD4 were synthesized based on
       chemical similarity with active CD4(81-92)-benzylated peptides. The
       synthetic peptide FYIFFVEDQKEEDD blocked the binding of gp120 to CD4 and
       inhibited 50% human immunodeficiency virus (HIV)-induced syncytia
       formation at a concentration (IC50) of approximately 40-50 microM and
       HIV p17 expression with an IC50 of approximately 67 microM. The peptide
       is not toxic to cells in vitro. Moreover, acute toxicity studies carried
       out in Swiss mice showed the peptide to be nontoxic at a dose of 2,000
       mg/kg. This phenylalanine-substituted CD4 peptide may prove to be useful
       in the treatment of AIDS.
 DE    Amino Acid Sequence  Animal  Antigens, CD4/METABOLISM  Binding,
       Competitive  Cell Line  Enzyme-Linked Immunosorbent Assay  Gene
       Products, gag/BIOSYNTHESIS/DRUG EFFECTS  Giant Cells/MICROBIOLOGY  HIV
       Antigens/BIOSYNTHESIS/DRUG EFFECTS  HIV Envelope Protein
       gp120/METABOLISM  HIV-1/*DRUG EFFECTS/PHYSIOLOGY  Mice  Molecular
       Sequence Data  Peptides/CHEMISTRY/CHEMICAL
       SYNTHESIS/*PHARMACOLOGY/TOXICITY  Phenylalanine/*CHEMISTRY  Recombinant
       Proteins/METABOLISM  Solubility  Support, Non-U.S. Gov't  JOURNAL
       ARTICLE

       SOURCE: National Library of Medicine.  NOTICE: This material may be
       protected by Copyright Law (Title 17, U.S.Code).