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Publication Number
US-11952414-B2
Publication Date
2024-04-09
Expiration Date
Abstract
Provided is a peptide provided herein includes at least one peptide unit, and the peptide unit may include at least one B-cell epitope, at least one Th epitope, and an appropriate number of auxiliary parts. The peptide unit is a portion designed to uniformly induce only the intended antibody while exhibiting a certain level of immunogenicity in the body of a subject. In addition, the peptide unit is designed with a relatively short length, and thus has the characteristics of easy synthesis and a low production cost. The peptide has properties suitable for use as an immunotherapeutic due to the characteristics of the peptide unit described above. In the present specification, the design principles of the peptide and the peptide unit are disclosed in detail.
Core Innovation
The patent describes peptide unit compositions for inducing uniform, intended antibody responses and humoral immunity. Each peptide unit includes CD4+ helper T epitopes and B-cell epitopes derived from apolipoprotein B-100 fragments or mimotopes, with arrangements such as one B-cell epitope with one Th epitope, two Th epitopes, or two B-cell epitopes with variations in linking order.
Auxiliary parts include linkers, Th-protective functions configured to resist degradation, cyclic-forming via terminal cysteines, solubility improving or dummy segments, and nonstandard amino acids including D-form alanine (a), L-cyclohexylalanine (Cha), and 6-aminohexanoic acid (Z). The document also provides representative epitope sequences, peptide assembly strategies including single unit, concatemer, string-of-beads, mixed design, and cyclic forms, and example peptide sequences used in the document's experimental examples.
The patent further describes pharmaceutical compositions using nucleic acids, including codon-equivalent RNA/DNA sequences, to deliver and induce an immune response, with nucleic acid constructs and formulation options including viral and non-viral vectors and nanoparticle delivery modalities. It also expands to therapeutic use in treating obesity by using antibody responses targeting ApoB-100 sites in LDL/VLDL, using peptide compositions and nucleic acids encoding the peptides.
Claims Coverage
The provided claim content centers on one independent claim directed to a specific peptide sequence defined with special residue designations. Dependent claims further narrow the peptide by requiring that it consists of the stated sequence.
Defined peptide sequence with special residue designations
A peptide comprising the amino acid sequence RNVPPIFNDVYWIAFZaK(Cha)VAAWTLKAACR (SEQ ID NO: 161), wherein a denotes D-form alanine, (Cha) denotes L-cyclohexylalanine, and Z denotes 6-aminohexanoic acid.
Strict sequence definition using consists of
The peptide of the defined sequence where the amino acid sequence consists of RNVPPIFNDVYWIAFZaK(Cha)VAAWTLKAACR (SEQ ID NO: 161), with a as D-form alanine, (Cha) as L-cyclohexylalanine, and Z as 6-aminohexanoic acid.
Across the provided claims, protection is directed to a particular peptide sequence (SEQ ID NO: 161) using explicit residue notations for D-form alanine (a), L-cyclohexylalanine ((Cha)), and 6-aminohexanoic acid (Z), with dependent claims additionally constraining the peptide as consists of that sequence.
Stated Advantages
Induce uniform, intended antibody responses and humoral immunity.
Provides peptides and nucleic acids to prepare obesity immunotherapeutics via humoral immunity.
Documented Applications
Treating obesity by using antibody responses targeting ApoB-100 sites in LDL/VLDL.
Immunotherapy using peptides/nucleic acids and the disclosed compositions, including antibody titers against a B-cell epitope antigen.
In vivo mouse studies with measurement of antibody titers against a target B-cell epitope (SEQ ID NO: 6/ApoB100), along with blood lipid concentration readouts and adipocyte/lipolysis-related metrics.
Obesity treatment using peptides/nucleic acids and the disclosed compositions, with reported weight change and obesity-related outcomes in experimental examples.
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