Active Cores of Peptide Triazole HIV-1 Entry Inhibitors
AssigneePhiladelphia Health & Education Corporation d/b/a Drexel University College of Medicine
InventorsIRWIN M. CHALKEN, UMASHANKARA MUDDEGOWDA, KARYN MCFADDEN
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Abstract
The invention provides a peptide triazole conjugate and derivatives thereof, and methods of its use. The invention also provides an antibody to the peptide triazole conjugate. The invention further provides a method of identifying an HIV-1 entry inhibitor candidate.
Claims33
A composition comprising a peptide triazole conjugate comprising a peptide component, wherein the peptide component consists essentially of the sequence X1X2X3NIPWX4 (SEQ ID No. 3), wherein:
- the sequence X1X2X3NIPWX4 is selected from the group consisting of SEQ ID No. 4 (INNIPWS), SEQ ID No. 5 (RINNIPWS), SEQ ID No. 7 (RINNIPW), SEQ ID No. 13 (INNIPW), SEQ ID No. 14 (NNIPWS), SEQ ID No. 15 (INIPWS) and SEQ ID No. 21 (NNIPW);
- the proline in SEQ ID No. 3 is modified according to Formula I:
- and
- R is a bulky aromatic group.
5-13. (canceled)
15-19. (canceled)
(canceled)
26-28. (canceled)
A method of treating HIV infection in an individual diagnosed therewith, the method comprising administering a therapeutically effective amount of a peptide triazole conjugate to the individual, wherein the peptide triazole conjugate comprises a peptide component, wherein the peptide component consists essentially of the sequence X1X2X3NIPWX4 (SEQ ID No. 3), wherein:
- the sequence X1X2X3NIPWX4 is selected from the group consisting of SEQ ID No. 4 (INNIPWS), SEQ ID No. 5 (RINNIPWS), SEQ ID No. 7 (RINNIPW), SEQ ID No. 13 (INNIPW), SEQ ID No. 14 (NNIPWS), SEQ ID No. 15 (INIPWS) and SEQ ID No. 21 (NNIPW);
- the proline in SEQ ID NO. 3 is modified according to Formula I:
- and
- R is a bulky aromatic group.
(canceled)
36-38. (canceled)
A method of reducing the risk of HIV infection in an individual at risk of HIV exposure, the method comprising administering to the individual a therapeutically effective amount of a pharmaceutical composition comprising a peptide triazole conjugate, wherein the peptide triazole conjugate comprises a peptide component, wherein the peptide component consists essentially of the sequence X1X2X3NIPWX4 (SEQ ID No. 3), wherein:
- the sequence X1X2X3NIPWX4 is selected from the group consisting of SEQ ID No. 4 (INNIPWS), SEQ ID No. 5 (RINNIPWS), SEQ ID No. 7 (RINNIPW), SEQ ID No. 13 (INNIPW), SEQ ID No. 14 (NNIPWS), SEQ ID No. 15 (INIPWS) and SEQ ID No. 21 (NNIPW);
- the proline in SEQ ID NO. 3 is modified according to Formula I:
- and
- R is a bulky aromatic group.
(canceled)
47-49. (canceled)
A method of isolating a viral envelope protein gp120 from a sample, the method comprising the steps of:
- contacting a solid phase matrix with a sample comprising gp120, wherein a peptide triazole conjugate is linked to the solid phase matrix,
- wherein the peptide triazole conjugate comprises a peptide component, wherein the peptide component consists essentially of the sequence X1X2X3NIPWX4 (SEQ ID No. 3), wherein:
- the sequence X1X2X3NIPWX4 is selected from the group consisting of SEQ ID No. 4 (INNIPWS), SEQ ID No. 5 (RINNIPWS), SEQ ID No. 7 (RINNIPW), SEQ ID No. 13 (INNIPW), SEQ ID No. 14 (NNIPWS), SEQ ID No. 15 (INIPWS) and SEQ ID No. 21 (NNIPW);
- the proline in SEQ ID NO. 3 is modified according to Formula I:
- and
- R is a bulky aromatic group,
- wherein the gp120 binds to the peptide triazole conjugate, thereby partitioning the sample into a bound phase and an unbound phase;
- and
- separating the unbound phase from the unbound phase, thereby isolating the gp120.
An antibody to a peptide triazole conjugate comprising a peptide component, wherein the peptide component consists essentially of the sequence X1X2X3NIPWX4 (SEQ ID No. 3), wherein:
- the sequence X1X2X3NIPWX4 is selected from the group consisting of SEQ ID No. 4 (INNIPWS), SEQ ID No. 5 (RINNIPWS), SEQ ID No. 7 (RINNIPW), SEQ ID No. 13 (INNIPW), SEQ ID No. 14 (NNIPWS), SEQ ID No. 15 (INIPWS) and SEQ ID No. 21 (NNIPW);
- the proline in SEQ ID NO. 3 is modified according to Formula I:
- and
- R is a bulky aromatic group.
Dependencies are inferred from the claim text.