Antiviral inhibition of capsid proteins

Details Antiviral inhibition of capsid proteins Antiviral inhibition of capsid proteins

C - Chemistry, Metallurgy

12

Q

C12Q 1/70 (2006.01) A61K 31/17 (2006.01) A61K 31/277 (2006.01) A61K 31/341 (2006.01) A61P 31/18 (2006.01) C07D 307/52 (2006.01) G01N 33/569 (2006.01) C07K 14/16 (2006.01) C12Q 1/18 (2006.01)

Patent

CA 2483227

Methods for evaluating the antiviral activity of test compounds are provided. Further aspects of the methods involve the retroviral capsid protein of HIV-1. In another aspect, methods of reducing mortality associated with AIDS with a compound that binds to the apical cleft near the C-terminal end of the N- terminal domain of the HIV-1 capsid protein are provided. Derivatives of CAP- 1, CAP-2, CAP-3, CAP-4, CAP-5, CAP-6 and CAP-7 are described that bind to the apical cleft of the N-terminal domain of the HIV-1 capsid protein and inhibit proper assembly of the core particle.

L'invention concerne des procédés permettant d'évaluer l'activité antivirale de composés d'essai. D'autres aspects de ces procédés font intervenir la protéine capsidique rétrovirale du VIH-1. Un autre aspect de l'invention concerne des procédés destinés à réduire la mortalité liée au SIDA au moyen d'un composé qui se lie à la fente apicale à proximité de l'extrémité C-terminale du domaine N-terminal de la protéine capsidique du VIH-1. L'invention concerne en outre des dérivés de CAP-1, CAP-2, CAP-3, CAP-4, CAP-5, CAP-6 et CAP-7 qui se lient à la fente apicale du domaine N-terminal de la protéine capsidique du VIH-1 et inhibent un assemblage correct des particules capsidiques.

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