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Title:
NOVEL MODIFIED STRUCTURE OF GROWTH HORMONE RELEASE HORMONE-LIKE PEPTIDE AND DIMERIZATION PREPARATION AND USE THEREFOR
Document Type and Number:
WIPO Patent Application WO/2021/160188
Kind Code:
A1
Abstract:
Provided are a molecularly modified structure of an hGRH-like peptide and a dimer thereof, the dimer being made from two same modified hGHRH-like peptide monomers containing single cysteine molecules and connected by means of disulfide bonds formed by the cysteine, and taking an H-shaped structure (a single substitution of Ser→Cys occurring inside the molecule). Fatty acid chain modification is further performed on a side chain ε-amino group of one lysine in the GHRH-like peptied. By means of fatty acid modification, the sustained release time of GH of the GHRH-like peptide monomer or the dimer in the body is extended, reaching up to 17 days. The invention can thus treat GH deficiency, infertility, senile dementia, diabetes, and strengthen immunity. The GHRH dimer having long-lasting activity features an Aib→2Ala substitution, 18C- 18C disulfide bond formation, C20 fatty acid chain modification, and a C-terminus amidation structure.

Inventors:
TANG SONGSHAN (CN)
ZHANG XUDONG (CN)
LUO QUN (CN)
YANG LI (CN)
TAN HONGMEI (CN)
TANG JINGXUAN (CN)
YOU JUAN (CN)
Application Number:
PCT/CN2021/080679
Publication Date:
August 19, 2021
Filing Date:
March 15, 2021
Export Citation:
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Assignee:
NANJING FINEPEPTIDE BIOPHARMACEUTICAL CO LTD (CN)
International Classes:
C07K14/60; A61K38/25; A61P3/10; A61P5/06; A61P15/08; A61P25/28; A61P37/04
Domestic Patent References:
WO2009009727A22009-01-15
WO2009108364A22009-09-03
Foreign References:
CN109180800A2019-01-11
CN104558150A2015-04-29
CN110845601A2020-02-28
EP1052286A22000-11-15
CN111533800A2020-08-14
Other References:
CHEN FEI, TANG SONGSHAN, YOU JUAN, ZHANG JUANHUI, ZHOU DONG: "Bioactive study of six novel GHRH analogs", GUANGDONG YIXUE - GUANGDONG MEDICAL JOURNAL, GUANGDONG SHENG YIXUE QINGBAO YANJIUSUO, GUANGZHOU, CN, vol. 35, no. 15, 1 August 2014 (2014-08-01), CN, pages 2309 - 2311, XP055835228, ISSN: 1001-9448, DOI: 10.13820/j.cnki.gdyx.2014.15.001
TANG, S.S. ; DU, M.H. ; ZHANG, J.H. ; KONG, X. ; LIU, J.J.: "Structure and function relationships of three novel hGHRH-GGC analogs", REGULATORY PEPTIDES, ELSEVIER SCIENCE BV, NL, vol. 159, no. 1-3, 8 January 2010 (2010-01-08), NL, pages 87 - 92, XP026798391, ISSN: 0167-0115
Attorney, Agent or Firm:
GUANGZHOU KEYUE I. P. LAW OFFICE (CN)
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