Compositions and methods for inhibition of hiv-1 infection

Details Compositions and methods for inhibition of hiv-1 infection Compositions and methods for inhibition of hiv-1 infection

A - Human Necessities

61

K

A61K 39/21 (2006.01) A61K 39/00 (2006.01) A61K 39/42 (2006.01) C07K 14/16 (2006.01) C07K 14/73 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2398521

This invention provides a composition which comprises an admixture of two compounds, wherein one compound retards attachment of HIV-1 to a CD4+ cell by retarding binding of HIV-1 gp120 envelope glycoprotein to CD4 on the surface of the CD4+ cell and the other compound retards gp41 from adopting a conformation capable of mediating fusion of HIV-1 to a CD4+ cell by binding noncovalently to an epitope on a gp41 fusion intermediate, wherein the relative mass ratio of the compounds in the admixture ranges from about 100:1 to about 1:100, the composition being effective to inhibit HIV-1 infection of the CD4+ cell. This invention also provides a method of inhibiting HIV-1 infection of CD4+ cell which comprises contacting the CD4+ cell with an amount of the above composition effective to inhibit HIV-1 infection of the CD4+ cell so as to thereby inhibit HIV-1 infection of the CD4+ cell.

L'invention concerne une composition comprenant un mélange de deux composés, l'un desdits composés retardant la fixation de VIH-1 sur une cellule CD4+ par retardement de la liaison de la glycoprotéine de l'enveloppe gp120 du VIH-1 avec la surface de la cellule CD4+, et l'autre composé retardant l'adoption par gp41 d'une conformation à médiation de fusion HIV-1/ cellule CD4+ par liaison non covalente avec un épitope sur un intermédiaire de fusion de gp41. Le rapport de masse relative des composés dans le mélange se situe entre environ 100/1 et 1/100, la composition étant efficace pour inhiber une infection à HIV-1 de la cellule CD4+. L'invention concerne également une méthode permettant d'inhiber une infection de la cellule CD4+ par le VIH-1, consistant à mettre la cellule CD4+ en contact avec une quantité de la composition précitée efficace pour inhiber une infection de la cellule CD4+ par le VIH-1.

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