Synthetic peptides for neutralising the infectiosity of the AIDS VIRUS (HIV)

摘要

The invention relates to phenylalanine-containing peptides with the brief formula: R1-aa1-Tyr-Ile-aa4-aa5-Val-aa7-aa8-aa9-R2, where the radical R1 corresponds either to a hydrogen atom or R3. The radical R2 corresponds to a hydrogen group or a group which is the same as or different from R3, where R3 is an oligopeptide which contains 2 to 10 amino acid residues; aa1 is Tyr or Phe, aa4 is Cys or Phe, aa5 is Glu or Phe, aa7 is Glu or Phe, aa8 is Asp or Phe and aa9 is Gln, Glu or a single bond between aa8 and R2, with at least one of the groups aa1, aa4, aa5, aa7 and aa8 being Phe. The preferred structures are those in which R1 = H and R2 = OH and in which the peptide is readily soluble in water. These peptides can be used for inhibition of the infectiosity of the AIDS Virus. These peptides have possible therapeutic uses, not only for the actual AIDS disorder but also for disturbing concomitant manifestations of AIDS. They could be useful for bringing to a standstill the advance of the disorder in asymptomatic HIV-seropositive people. Accordingly, they may be effective for prophylaxis of infection in people in risk groups who may possibly come into contact with the virus, and in the newborn children of seropositive mothers. These peptides can be prepared synthetically by the solid-phase method of Merrifield or by genetic engineering methods.