Peptides for treatment and prevention of hyperglycaemia
Inventors
Marion, Vincent • Petrovsky, Nikolai
Assignees
VAXINE Pty Ltd • Institut National de la Sante et de la Recherche Medicale INSERM • Universite de Strasbourg
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Publication Number
US-11332503-B2
Publication Date
2022-05-17
Expiration Date
Abstract
The present invention relates to peptides for the treatment or prevention of diabetes mellitus and associated disorders.
Core Innovation
The invention relates to a peptide that induces insulin-independent adipocyte glucose transport. The peptide has a length of at least 15 amino acids and less than 40 amino acids, and the peptide sequence comprises a sequence selected from a defined group of SEQ ID NO variants. The described peptide sequences include constructs built around an alphaPKC segment and are associated with insulin-independent glucose transport in adipocytes.
The core mechanism described in the provided material is that the peptide induces insulin-independent glucose transport in adipocytes through binding/blocking of an αPKC–ALMS1 interaction. The described αPKC segment is preferably derived from PKC alpha (αPKC), and the peptide sequences are characterized by inclusion of methionine, proline, and arginine and by an alpha-helical preference. The document also describes chemical cross-linking/stapling forms, including stapling positions on R8 and S5.
The provided material further states that the peptide sequences include specific listed PKC/peptide sequences (including SEQ ID variants) and modified forms, such as variants with optional terminal group modifications and chemical stapling/cross-linking. The described therapeutic approach includes pharmaceutical compositions and combination therapy with anti-diabetic/weight-loss agents, and therapeutic uses for treating or delaying progression of type 2 diabetes and related metabolic/diabetic conditions.
Claims Coverage
The claims coverage centers on one independent claim defining an insulin-independent adipocyte glucose-transport peptide and several dependent claims that refine peptide sequence/structure and extend coverage to pharmaceutical compositions and combination use. The main inventive elements are limited peptide length and a restricted set of enumerated SEQ ID NO sequences, optionally with chemical and terminal group modifications; additional claim coverage includes formulation and inclusion of an anti-diabetic agent from an enumerated drug class list.
Insulin-independent adipocyte glucose transport peptide length
A peptide that induces insulin-independent adipocyte glucose transport, wherein the peptide has a length of at least 15 amino acids and less than 40 amino acids.
Restricted peptide sequence from enumerated SEQ ID variants
The peptide sequence comprises a sequence selected from the group consisting of SEQ ID NO: 9, 21–31, and 33, including variants such as VECTMVEKRVLALLDKPPFLTQLHS and the listed R8/S5-containing constructs (e.g., H-VECTM-R8-EKRVLA-S5-LDKPPFLTQLHS-OH and related variants).
Chemical cross-linking peptide modification
The peptide is defined with a chemical cross-linking modification (as a refinement of the peptide definition of the independent claim).
Hydroxyl end group peptide terminal feature
The peptide has a hydroxyl end group (as a refinement of the peptide definition of the independent claim).
Pharmaceutical composition comprising the peptide
A pharmaceutical composition is provided that includes a peptide as defined in the independent claim.
Pharmaceutical composition with selected anti-diabetic agent
The pharmaceutical composition further includes an anti-diabetic agent selected from a specified group of anti-diabetic drugs, or a combination thereof.
Overall, claim coverage is directed to a narrowly defined peptide (length-limited and restricted to enumerated SEQ ID NO variants) that induces insulin-independent adipocyte glucose transport, with additional dependent coverage for chemical cross-linking and hydroxyl end group terminal features, and further extension to pharmaceutical compositions including optional combination with an enumerated anti-diabetic agent group.
Stated Advantages
Induces insulin-independent adipocyte glucose transport.
Treats or delays progression of type 2 diabetes and related metabolic/diabetic conditions.
Documented Applications
Therapeutic use for treating or delaying progression of type 2 diabetes and related metabolic/diabetic conditions.
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