Viral infection inhibitor targeting integrase n-terminal domain

Details Viral infection inhibitor targeting integrase n-terminal domain Viral infection inhibitor targeting integrase n-terminal domain

C - Chemistry, Metallurgy

12

N

C12N 15/52 (2006.01) A61K 31/7088 (2006.01) A61K 39/21 (2006.01) A61K 48/00 (2006.01) A61P 31/18 (2006.01) C07K 14/16 (2006.01) C12N 9/00 (2006.01) C12N 9/12 (2006.01) C12N 15/00 (2006.01) C12N 15/49 (2006.01) C12N 15/54 (2006.01)

Patent

CA 2372456

The object of the present invention is to provide a screening method of a new integrase inhibitor being able to inhibit an HIV infection before the reverse transcription step and having a pharmaceutical site of action totally different from those of traditional integrase inhibitors, a new integrase inhibitor being obtainable by the screening method, and pharmaceutical constituents containing the integrase inhibitor and DNA encoding the integrase inhibitor being greatly expected as new remedies for AIDS. A peptide which specifically binds to a peptide at N-terminal domain of retroviral integrase was screened by phage display method, and as a result of the screening, a peptide being able to inhibit the infection and the proliferation of retroviruses such as HIV-1 before the reverse transcription reaction is obtained.

L'invention porte sur un procédé de recherche automatique d'un nouvel inhibiteur de l'intégrase totalement différent des inhibiteurs d'intégrase traditionnels dans un point fonctionnel d'un médicament, procédé selon lequel il est possible d'inhiber l'infection due au VIH avant de passer à l'étape de la transcription inverse. L'invention porte également sur de nouveaux inhibiteurs de l'intégrase obtenus à l'aide du procédé de recherche automatique précité ; sur des compositions médicinales contenant ces inhibiteurs d'intégrase ou l'ADN les codant et envisagées comme nouveaux remèdes contre le SIDA. L'invention porte encore sur l'obtention d'un peptide inhibant l'infection et la prolifération d'un rétrovirus (VIH, etc.) avant la transcription inverse par recherche automatique selon une méthode d'expression à la surface des phages d'un peptide se liant spécifiquement à la région à extrémité terminale N d'une intégrase de rétrovirus.

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