Antiviral activity and cross-resistance profile of P-1946, a novel human immunodeficiency virus type 1 protease inhibitor.
The HIV protease inhibitor P-1946 is a member of a novel family of l-Lysine derivatives. The compound is a specific HIV-1 protease inhibitor that has potent and selective in vitro antiviral activity (EC50 152 nM) against a range of isolates resistant to commercially available protease inhibitors. The presence of at least four primary and four secondary drug resistance mutations is required to achieve greater than four-fold resistance to P-1946. P-1946's favorable resistance profile makes it a good lead for the development of new agents active against existing PI-resistant virus in treatment-experienced patient.
Sévigny
G
G
Procyon Biopharma Inc., Montreal, Canada.
Stranix
B
B
Tian
B
B
Dubois
A
A
Sauvé
G
G
Petropoulos
C
C
Lie
Y
Y
Hellmann
N
N
Conway
B
B
Yelle
J
J
D002460:Cell Line; D024882:Drug Resistance, Viral; D016333:HIV Protease / Q000737:chemistry / Q000378:metabolism; D017320:HIV Protease Inhibitors / Q000494:pharmacology*; D015497:HIV-1 / Q000187:drug effects* / Q000201:enzymology / Q000502:physiology; D006801:Humans; D007211:Indoles / Q000494:pharmacology*; D008239:Lysine / Q000031:analogs & derivatives; D013449:Sulfonamides / Q000494:pharmacology*; D014779:Virus Replication / Q000187:drug effects
D017320:HIV Protease Inhibitors; D007211:Indoles; C512203:P 1946; D013449:Sulfonamides; D016333:HIV Protease; D008239:Lysine