SCREENING OF ANTIVIRAL COMPOUNDS TARGETED TO THE HIV-1 gp41 CORE STRUCTURE

摘要

A method for the screening of antiviral compounds targeted to the HIV- 1 gp41 core structure comprising capturing polyclonal antibodies from an animal other than a mouse directed against a trimer of a heterodimer containing an N- peptide and a C- peptide onto a solid- phase, mixing a compound to be tested with an N- peptide and then adding a C- peptide, adding the resultant mixture to the resultant polyclonal antibody coated solid- phase and then removing unbound peptides and unbound compound, adding a monoclonal antibody directed against the trimer of a heterodimer containing an N- peptide and a C- peptide and measuring the antibody binding of the monoclonal antibody. A method for inhibiting HIV- 1 virus replication or infectivity in a patient by administering to the patient an antiviral compound targeted to the HIV- 1 gp41 core structure selected from the group consisting of 7- [6- phenylamino- 4[4- [(3,5- disulfo- 8- hydroxynaphthyl)azo]- 2- methoxy- 5- methyl- phenylamino]- 1,3,5- triazine- 2- yl]- 4- hydroxy- 3- [(2- methoxy- 5- sulfophenyl)azo]- 2- naphthalene sulfonic acid and 5- [(4- chloro- 6- phenylamino- 1,3,5- triazine- 2- yl)- aminol]- 4- hydroxy- 3- (4- methyl- 5- sulfophenyl)azo]- 2,7- naphthalene disulfonic acid.