Document 0151
 DOCN  M95A0151
 TI    Antiherpetic activities of N-alpha-acetyl-nona-D-arginine amide acetate.
 DT    9510
 AU    Sumner-Smith M; Zheng Y; Zhang YP; Twist EM; Climie SC; Allelix
       Biopharmaceuticals Inc., Mississauga, Ontario, Canada.
 SO    Drugs Exp Clin Res. 1995;21(1):1-6. Unique Identifier : AIDSLINE
       MED/95317183
 AB    N-alpha-acetyl-nona-D-arginine amide acetate (ALX40-4C) was developed as
       a competitive inhibitor of the binding of the HIV Tat protein to its RNA
       target TAR, which is an intracellular interaction dependent on a short,
       arginine-rich sequence in Tat. ALX40-4C is a simple mimic of that
       domain, which is stabilised against enzymatic degradation through
       inclusion of D-amino acids and terminal protection. The drug inhibits
       HIV-1 in vitro and is currently being assessed in vivo. In the work
       reported here, potential activities of the compound against other
       viruses were examined. As expected, there was little or no activity
       against most viruses examined, except against some herpesviruses: HSV-1,
       HSV-2 and CMV. Maximal inhibition of HSV-1 in a plaque reduction assay
       required pre-incubation with the drug. Maximal inhibition of HCMV, which
       replicates more slowly than HSV-1, requires exposure to the compound
       within the first few hours of infection. It appears that the drug
       inhibits an early step in HSV and HCMV infection. Such a mechanism is
       consistent with that of other cationic, herpesvirus inhibitors.
 DE    Antiviral Agents/*PHARMACOLOGY  Cytomegalovirus/*DRUG EFFECTS
       Herpesvirus 1, Human/*DRUG EFFECTS  Herpesvirus 2, Human/DRUG EFFECTS
       Oligopeptides/*PHARMACOLOGY  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).