Inactivated pepsin fragments for modulating immune system activity against human malignant tumor cells

• US 8,067,531 B2
• Filed: 12/02/2008
• Issued: 11/29/2011
• Est. Priority Date: 11/12/2004
• Status: Active Grant

• Current Assignee: The Zhabilov Trust
• Original Assignee: The Zhabilov Trust
• Inventors: Zhabilov, Harry H.
• Primary Examiner(s): LI, BAO Q
• Application Number:
  US12/315,441
• Publication Number:
  US 20100143291A1
• Time in Patent Office: 1,092 Days
• Field of Search: None
• US Class Current: 530/300
• CPC Class Codes: A61K 2039/55533 IL-2
• CPC Class Codes: A61K 38/00 Medicinal preparations containing peptides peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00
• CPC Class Codes: A61K 39/001154 Enzymes
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: C07K 14/47 from mammals
• CPC Class Codes: C12N 2740/16111 concerning HIV env
• CPC Class Codes: G01N 2333/16 HIV-1, HIV-2

Abstract

Isolated anti-cancer peptides are disclosed which are characterized by the amino acid sequences TLTSGGGAIALPPSMAAPPLGPVAPLTGAIHAPTXG; TLSTATGGAIPPVAAMPPGLVAPTHGPAIHP; CCATSGPCGAVMILTPHLTA; MTLTTGSGAIAPAMPPGLPPHTGAIHAPM; and NXVPVSVEGYXQITLDSITX and a significant in vitro binding affinity for gp96. The peptides exhibit anti-tumor, anti-cancer activity in vivo. Also disclosed is an isolated antiviral peptide is characterized by the amino acid sequence GDEPLENYLDTEYF and a significant in vitro binding affinity for HIV-1 gp 120 and gp 41, and human CD4 cells. The peptide exhibits anti-retroviral activity in vivo, particularly anti-HIV-1 activity.

Claims

1. An isolated irreversibly inactivated anti-cancer pepsin characterized by the amino acid sequence of SEQ ID NO:

1.

2. A composition comprising the isolated irreversibly inactivated anti-cancer pepsin of claim 1, further comprising a carrier.

3. A composition for inferring immunity against malignant human cells, said composition comprising the composition of claim 2 combined with IL2.

4. A therapeutic composition comprising a complex of the isloated irreversibly inactivated anti-cancer pepsin of claim 1 bound to human gp96.

5. A therapeutic composition comprising a complex of the isloated irreversibly inactivated anti-cancer pepsin of claim 1 bound to a receptor disposed on human gp96.

6. The composition of claim 5, where in the receptor is CD91.

7. A pepsin isolated from a 45 kD pepsinogen fragment, said pepsin consisting of the isolated irreversibly inactivated anti-cancer pepsin of claim 1, wherein said pepsin has a binding affinity for human gp96.

8. A composition comprising the therapeutic composition of claim 4, said composition further comprising IL2.