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Publication Number
US-12479905-B2
Publication Date
2025-11-25
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 invention relates to immunotherapeutic peptides designed to induce a pre-designed antibody and defined humoral immunity. The peptides comprise one or more peptide units and contain at least one CD4+ Th epitope and at least one B-cell epitope, with auxiliary parts such as linkers, protective segments, solubility enhancers, dummy/His-tag sequences, and optional cyclicization via cysteine-linked ends.
The disclosure also provides peptides comprising amino acid sequences selected from a group of peptide sequence variants, including GSHHHHHHGSDDDDKZaK(Cha)VAAWTLKAAaZRNVPPIFNDVYWIAF (SEQ ID NO: 69), RNVPPIFNDVYWIAFZaK(Cha)VAAWTLKAAaZGSHHHHHHGSDDDDK (SEQ ID NO: 68), RNVPPIFNDVYWIAFZaK(Cha)VAAWTLKAAaZ (SEQ ID NO: 56), RNVPPIFNDVYWIAFK(Cha)VAAWTLKAA (SEQ ID NO: 62), and RNVPPIFNDVYWIAFK(Cha)VAAWTLKAAHHHHHH (SEQ ID NO: 67), with defined residue meanings for a, (Cha), and Z.
The specification further includes peptide compositions where peptide units are linked to form B/T linked peptide architectures, including multi-auxiliary architectures and multiple concatenation formats. It also includes pharmaceutical composition concepts and nucleic acid encoding the peptides, together with codon optimization concepts, and describes use in treating obesity by inducing antibodies targeting ApoB-100.
Claims Coverage
The claim coverage centers on two inventive features: a defined peptide sequence set and peptide-based compositions with adjuvants.
Selected peptide sequences with defined nonstandard residues
A peptide comprising an amino acid sequence selected from the group consisting of GSHHHHHHGSDDDDKZaK(Cha)VAAWTLKAAaZRNVPPIFNDVYWIAF (SEQ ID NO: 69), RNVPPIFNDVYWIAFZaK(Cha)VAAWTLKAAaZGSHHHHHHGSDDDDK (SEQ ID NO: 68), RNVPPIFNDVYWIAFZaK(Cha)VAAWTLKAAaZ (SEQ ID NO: 56), RNVPPIFNDVYWIAFK(Cha)VAAWTLKAA (SEQ ID NO: 62), and RNVPPIFNDVYWIAFK(Cha)VAAWTLKAAHHHHHH (SEQ ID NO: 67), wherein a denotes D-form alanine, (Cha) denotes L-cyclohexylamine, and Z denotes 6-aminohexanoic acid.
Peptide-containing composition with adjuvants
A composition comprising the peptide together with adjuvants.
Adjuvants including aluminium phosphate and Monophosphoryl Lipid A
The composition includes aluminium phosphate and Monophosphoryl Lipid A.
Overall, the claims are directed to a peptide defined by a specified set of amino acid sequence variants with explicit meanings for nonstandard residue symbols, and extend to peptide-containing compositions formulated with adjuvants, including aluminium phosphate and Monophosphoryl Lipid A.
Stated Advantages
The peptides are described as designed to induce a pre-designed antibody and defined humoral immunity.
The design rules are intended to enable uniform induction of the defined humoral immunity.
The use described includes treating obesity by inducing antibodies targeting ApoB-100.
Documented Applications
Immunotherapy.
Treating obesity by inducing antibodies targeting ApoB-100.
Preparation of therapeutics for first medical use and second medical use in immunotherapy and obesity treatment.
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