Triterpene derivatives that block entry of human immunodeficiency virus type 1 into cells.
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.
Mayaux
J F
JF
Rhône Poulenc Rorer S.A., Centre de Recherche de Vitry-Alfortville, Vitry Sur Seine, France.
Bousseau
A
A
Pauwels
R
R
Huet
T
T
Hénin
Y
Y
Dereu
N
N
Evers
M
M
Soler
F
F
Poujade
C
C
De Clercq
E
E
D000998:Antiviral Agents; D015704:CD4 Antigens / Q000378:metabolism; D002460:Cell Line; D015658:HIV Infections / Q000517:prevention & control*; D015497:HIV-1 / Q000472:pathogenicity*; D008561:Membrane Fusion; D053978:Pentacyclic Triterpenes; D013329:Structure-Activity Relationship; D014315:Triterpenes / Q000737:chemistry / Q000494:pharmacology*; D000094062:Betulinic Acid
D000998:Antiviral Agents; D015704:CD4 Antigens; D053978:Pentacyclic Triterpenes; D014315:Triterpenes; D000094062:Betulinic Acid