Patent ID: 6150088
Filing Date: 2000-11-21
Classification: A61K,C07K,C12N

Abstract:
A method of producing a drug which inhibits interaction of two components of the core of fusion-active HIV-1 envelope gp41, wherein the two components are referred to as N36 peptide trimer and C34 peptide, respectively, comprising identifying a drug or designing a drug which fits into a cavity on the N36 peptide trimer which is:(a) lined by Leu-566 of the left N36 helix of FIG. 1 and Leu-565 of the right N36 helix of FIG. 1;(b) formed on the left side by sidechains from the left N36 helix, including residues (top to bottom) Val-570, Lys-574 (aliphatic portion) and Gln-577 of FIG. 1;(c) formed on the right side by residues Leu-568, Trp-571 and Gly-572 of the right N36 helix of FIG. 1; and(d) composed on its floor of Thr-569, Ile-573 and Leu-576 of FIG. 1 and which inhibits interaction of the N36 peptide trimer and the C34 peptide of the core of fusion-active HIV-1 envelope gp41, thereby producing a drug which inhibits interaction of the two components of fusion-active HIV-1 envelope gp41.