A class of hapten and fatty acid double modified bim bh3 mimic peptide, and preparation method and application thereof
By using BimBH3 mimic peptides modified with both hapten and fatty acids, the selectivity and stability issues of PTP1B target drugs have been resolved, achieving highly efficient inhibition of PTP1B and a long-lasting hypoglycemic effect once a week, which is suitable for the treatment of type 2 diabetes and obesity.
CN118420740BActive Publication Date: 2026-05-29QINGDAO UNIV OF SCI & TECH
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- QINGDAO UNIV OF SCI & TECH
- Filing Date
- 2024-04-27
- Publication Date
- 2026-05-29
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Figure CN118420740B_ABST
Abstract
The application discloses a new type of hapten and fatty acid double modified long-acting hypoglycemic BimBH3 mimetic peptide compound targeting PTP1B as well as a preparation method and application thereof. The structural general formula of the Bim BH3 mimetic peptide is shown as formula I: wherein the compound is derived from a core region peptide segment of a Bim-BH3 domain, a non-natural amino acid is used to replace the second amino acid by site-specific substitution to increase the stability of the peptide segment against DPP-4 enzyme, and a long-chain fatty acid (hexadecanoic acid or octadecanedioic acid) is conjugated to the N terminal to modify to ensure better PTP1B inhibitory activity, so that the BimBH3 mimetic peptide has longer duration and higher activity and plays a role in hypoglycemia by inhibiting the target PTP1B. The compounds are prepared by using 2-CTC resin by polypeptide solid-phase synthesis method, and the crude product is cut, purified and freeze-dried to obtain a pure target compound.
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