Peptide derivative fusion inhibitors of HIV infection
AssigneeFrontier Biotechnologies, Co., Ltd.
InventorsDong Xie, He Jiang
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Abstract
This invention relates to gp41 peptide derivatives that are inhibitors of viral infection and/or exhibit antifusogenic properties. In particular, this invention relates to gp41 derivatives having inhibiting activity against human immunodeficiency virus (HIV) and simian immunodeficiency virus (SIV) with enhanced duration of action for the treatment of the respective viral infections.
Claims36
An isolated FB005, FB006 or FB066 peptide comprising the sequence of SEQ ID NO:1, SEQ ID NO:2 or SEQ ID NO:3, respectively.
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An isolated, modified peptide selected from the group consisting of:
- (a) SEQ ID NO:1;
- (b) SEQ ID NO:2;
- (c) SEQ ID NO:3;
- and
- (d) SEQ ID NO:7,
- and having at least one substituted amino acid residue at a predetermined position in the peptide sequence, wherein the at least one substituted amino acid residue is a hydrophilic amino acid residue, a hydrophobic amino acid residue, an amino acid residue having a propensity to form alpha helices, a D-isomer of one of the naturally occurring L-amino acids, or a non-naturally occurring amino acid residue.
An isolated, derivatized peptide selected from the group consisting of:
- (a) the FB005M peptide of SEQ ID NO:8;
- (b) the FB005CM peptide of SEQ ID NO:9;
- (c) the FB006M peptide of SEQ ID NO:10;
- (d) the FB007M peptide of SEQ ID NO:11;
- (e) the FB010M peptide of SEQ ID NO:12;
- (f) the FB010KM peptide of SEQ ID NO:13;
- (g) the FB066M peptide of SEQ ID NO:14;
- and
- (h) the FB066KM peptide of SEQ ID NO:15.
An isolated, derivatized peptide selected from the group consisting of:
- (a) SEQ ID NO:1;
- (b) SEQ ID NO:2;
- (c) SEQ ID NO:3;
- and
- (d) SEQ ID NO:7,
- wherein predetermined amino acid residues in the peptide sequence are derivatized by conjugating a coupling group to said predetermined amino acid residues.
An isolated, derivatized peptide consisting of the sequence of SEQ ID NO:
- 3, wherein the peptide is modified by replacing glutamic acid at position 13 with a lysine and attaching a coupling group to the lysine, or derivatized by conjugating a coupling group to a lysine added at the C-terminus.
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A method of making an antiviral conjugate comprising mixing derivatized variant gp41 peptide(s) with blood components and allowing the formation of covalent bonds between derivatized variant gp41 peptide and blood components.
A method for the generation of peptides having anti-viral, virostatic or anti-fusogenic activity comprising:
- (a) screening a viral virulence protein(s) to identify sequences thereof having alpha-helical forming propensities;
- (b) designing an altered peptide by modifying or derivatizing at least one amino acid residue(s) of said identified sequence;
- (c) synthesizing said altered peptides;
- and
- (d) testing said peptides to verify anti-viral, virostatic or anti-fusogenic activity.
Dependencies are inferred from the claim text.