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PEPTIDE EXHIBITING, IN PARTICULAR AN ANTI-HIV ACTIVITY, METHOD FOR THE PREPARATION THEREOF AND A PHARMACEUTICAL COMPOSITION CONTAINING SAID PEPTIDE
PEPTIDE EXHIBITING, IN PARTICULAR AN ANTI-HIV ACTIVITY, METHOD FOR THE PREPARATION THEREOF AND A PHARMACEUTICAL COMPOSITION CONTAINING SAID PEPTIDE
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机译:尤其是抗HIV活性的肽的显示方法及其制备方法和包含所述肽的药物组合物
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摘要
The invention relates to a multi-branched peptide which exhibits, in particular an anti-HIV activity and comprising at least two identical or different peptidic branches, wherein the peptide sequence of each branch (i) is derived from a consensus sequence of a native endoproteolytic cleavage area gp 160 of a HIV-I virus envelop, the cleavage site upstream of each said peptide sequence is modified with respect the cleavage site upstream of the native endoproteolytic cleavage area in such a way that the antifusogenic activity is improved with respect to a peptide construct activity corresponding to the endoproteolytic cleavage area and the activity range thereof is extended, (ii) comprises from 5 to 25 types of amino acids from which at least two types of basic amino acids are situated in the upstream cleavage site, (iii) said basic amino acids on the upstream site location are situated at a distance more than t amino acids from a lysine core. Said peptide comprises at least one pattern of formula (I) with two identical or different peptide branches a1 and a2, wherein b1 is a disubstituted molecule and is characterised in that at least one of a1 or a2 comprises a sequence consecutively containing from 3 to 8 Arginine or Lysine, preferably from 4 to 6, with in N terminal a sequence from 0 to 6 amino acids, preferably from 2 to 4 and in C terminal a sequence from 2 to 12 amino acids, preferably from 4 to 9 bonding the sequence in interest with b1.
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