Flavivirus-binding, entry-obstructing, protease-resistant peptide (RI57)

• US 10,639,380 B2
• Filed: 12/06/2016
• Issued: 05/05/2020
• Est. Priority Date: 12/06/2016
• Status: Active Grant

• Current Assignee: Ennaid Therapeutics, LLC
• Original Assignee: Ennaid Therapeutics, LLC
• Inventors: Michael, Scott F., Isern, Sharon
• Primary Examiner(s): Coffa, Sergio
• Application Number:
  US15/369,893
• Publication Number:
  US 20180155398A1
• Time in Patent Office: Days
• Field of Search: None
• 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 47/643 Albumins, e.g. HSA, BSA, ovalbumin or a Keyhole Limpet Hemocyanin [KHL]
• CPC Class Codes: C07K 14/001 by chemical synthesis
• CPC Class Codes: Y02A 50/30 Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Abstract

The invention pertains to inhibitors bindable to regions of a virus. More particularly, the invention relates to inhibitors bindable to regions of flaviviral envelope glycoprotein, or flaviviral virus E protein, a class II viral E protein. Even more particularly, the invention relates to peptides inhibitory to virus-to-cell fusion and virus entry into animal cells. The invention also contains methods of determining said inhibitors, bindable to regions of the flaviviral E protein complex, (e.g., those of dengue and zika viruses) as candidates for in vivo anti-viral compounds that are also resistant to degradation by peptidases and thus extraordinarily suitable for oral, in addition to other, routes of administration.

Claims

1. A protease-resistant flavivirus-targeted cell entry-inhibitory peptide consisting of 28 amino acids arranged in an enantiopure, D-amino acid sequence presented as SEQ ID NO:

1.

2. The cell entry-inhibitory peptide of claim 1, wherein the cell entry-inhibitory peptide blocks a flaviviral class II envelope protein.

3. The cell entry-inhibitory peptide of claim 2, wherein the class II envelope protein is a flaviviral E protein.

4. A pharmaceutical composition comprising the cell entry-inhibitory peptide of claim 1 and a biocompatible carrier.

5. The pharmaceutical composition of claim 4, wherein the biocompatible carrier is selected from the group consisting of saline, buffered saline, dextrose, surfactant/spreading agent, and water.