A branched modified egf(a) analogue and uses thereof

CN117186201BActive Publication Date: 2026-09-15LEPU MEDICAL TECH (BEIJING) CO LTD
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Patent Information

Application Number
CN202210601400.2
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2022-05-30
Publication Date
2026-09-15
Estimated Expiration
2042-05-30

AI Technical Summary

Technical Problem

[0005]EGF(A)(表皮生长因子样结构域A)多肽片段是PCSK9的结合位点，是天然的PCSK9抑制剂(参见文献：Hong-mei Gu.Characterization of the role of EGF-A of lowdensity lipoprotein receptor in PCSK9 binding.Journal of Lipid Research[J],2013,54(12):3345-3357)，但是，EGF(A)属于生物体内产生的因子，一般很快被体内的酶降解，半衰期较短，成药性差，无法应用于临床

Benefits of technology

[0039]This invention provides branched EGF(A) analogs, the chemical formula of which is Gly-Thr-Asn-Glu-Cys-Leu-Asp-Asn-Leu-Gly-Gly-Cys-Ser-His-Val-Cys-Arg-Asp-Leu-Glu-Ile-Gly-Tyr-Glu-Cys-Leu-Cys-Pro-A1-Gly-Phe-Gln-Leu-Val-Ala-Lys(R)-Arg-Arg-Cys-A2-Lys(R), or Gly-Thr-Asn-Glu -Cys-Leu-Asp-Asn-Leu-Gly-Gly-Cys-Ser-His-Val-Cys-Arg-Asp-Leu-Glu-Ile-Gly-Tyr-Glu-Cys-Leu-Cys-Pro-A1-Gly-Phe-Gln-Leu-Val-Ala-Lys(R)-Arg-Arg-Cys-A2-A3-Lys(R), where A1 is Asp or Glu, A2 is Glu, Asp, Gln or Asn, A3 is Gly, Gln, Asn or Gly-Gly, and R is HO2C(CH2). n1 CO-(γGlu) n2 [NH-(CH2CH2O) n3 (CH2) n4 CO] n5 -or CH3O(CH2CH2O) m CH2CO-, where n1 is an integer from 10 to 20, n2 is an integer from 1 to 5, n3 is an integer from 2 to 15, n4 is an integer from 1 to 5, n5 is an integer from 1 to 5, and m is an integer from 10 to 40; the EGF(A) analogue has the advantage of a long half-life (up to 147 to 198 hours) and is of great promise for clinical treatment of cardiovascular diseases, dyslipidemia and/or metabolic syndrome.

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Abstract

The present application relates to a kind of branched chain modified EGF (A) analog and its application, belong to medical technology field.The present application provides a kind of branched chain modified EGF (A) analog, its main chain is composed of the polypeptide of amino acid sequence such as any one shown in SEQ ID NO.1-SEQ ID NO.40, and its main chain Lys amino acid residue is modified with branched chain R;The R is HO2C (CH2) n1 CO‑(γGlu) n2 [NH‑(CH2CH2O) n3 (CH2) n4 CO] n5 ‑ or CH3O (CH2CH2O) m CH2CO‑;The branched chain modified EGF (A) analog has the advantage of long half-life, in cardiovascular disease, dyslipidemia and / or metabolic syndrome clinical treatment has very application prospect.
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