Document 0041
 DOCN  M9460041
 TI    Triterpene derivatives that block entry of human immunodeficiency virus
       type 1 into cells.
 DT    9408
 AU    Mayaux JF; Bousseau A; Pauwels R; Huet T; Henin Y; Dereu N; Evers M;
       Soler F; Poujade C; De Clercq E; et al; Rhone Poulenc Rorer S.A., Centre
       de Recherche de; Vitry-Alfortville, Vitry Sur Seine, France.
 SO    Proc Natl Acad Sci U S A. 1994 Apr 26;91(9):3564-8. Unique Identifier :
       AIDSLINE MED/94224780
 AB    A series of triterpene compounds characterized by a stringent
       structure-activity relationship were identified as potent and selective
       inhibitors of human immunodeficiency virus type 1 (HIV-1) replication.
       Currently studied botulinic derivatives have 50% inhibitory
       concentrations (IC50) against HIV-1 strain IIIB/LAI in the 10 nM range
       in several cellular infection assays but are inactive against HIV-2.
       These compounds did not significantly inhibit the in vitro activities of
       several purified HIV-1 enzymes. Rather, they appeared to block virus
       infection at a postbinding, envelope-dependent step involved in the
       fusion of the virus to the cell membrane.
 DE    Antigens, CD4/METABOLISM  *Antiviral Agents  Cell Line  HIV
       Infections/*PREVENTION & CONTROL  HIV-1/*PATHOGENICITY  Membrane Fusion
       Structure-Activity Relationship  Support, Non-U.S. Gov't
       Triterpenes/CHEMISTRY/*PHARMACOLOGY  JOURNAL ARTICLE

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