Title:
ANTI-HIV POLYPEPTIDE MODIFIED WITH HIGH MOLECULAR PEG, PREPARATION THEREFOR, AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2021/223422
Kind Code:
A1
Abstract:
Provided is an anti-HIV polypeptide modified with polyethylene glycol (PEG). Specifically, cysteine is added to the N-terminus, C-terminus, or position 10 of a C34 polypeptide, and the C34 polypeptide is subjected to a Michael addition reaction to couple a maleimide-modified PEG group to said cysteine, so as to modify the C34 polypeptide via PEGylation, wherein the molecular weight of the PEG moiety is 10000 or higher, preferably from 10000 to 100000, and more preferably from 10000 to 50000. The modified C34 polypeptide has an obvious increase in water solubility and serum half-life in rats, can enter lymph nodes more easily, and has a stronger antiviral activity against HIV in rhesus monkeys acutely infected with SHIV SF162P3. Also provided are a preparation method for the anti-HIV polypeptide modified with PEG, and a use of the anti-HIV polypeptide modified with PEG.
Inventors:
LI XUEBING (CN)
CHENG SHUIHONG (CN)
LI MINGLI (CN)
MA LIYING (CN)
CHENG SHUIHONG (CN)
LI MINGLI (CN)
MA LIYING (CN)
Application Number:
PCT/CN2020/132063
Publication Date:
November 11, 2021
Filing Date:
November 27, 2020
Export Citation:
Assignee:
INST MICROBIOLOGY CAS (CN)
NAT CENTER FOR AIDS/STD CONTROL AND PREVENTION CHINESE CENTER FOR DISEASE CONTROL AND PREVENTION (CN)
NAT CENTER FOR AIDS/STD CONTROL AND PREVENTION CHINESE CENTER FOR DISEASE CONTROL AND PREVENTION (CN)
International Classes:
C07K14/16; A61K38/16; A61K47/60; A61P31/18; C07K1/107
Domestic Patent References:
| WO2014099984A1 | 2014-06-26 | |||
| WO2006105201A2 | 2006-10-05 |
Foreign References:
| CN110551179A | 2019-12-10 | |||
| CN111574597A | 2020-08-25 | |||
| CN102883740A | 2013-01-16 | |||
| CN103483428A | 2014-01-01 |
Other References:
WANG, DANDAN: "Site-Specific PEGylation and Glycosylation of Anti-HIV Peptide", CHINESE MASTER’S THESES FULL-TEXT DATABASE, ENGINEERING SCIENCE AND TECHNOLOGY I, no. 4, 15 April 2012 (2012-04-15), pages 1 - 61, XP055864382
WANG, C. ET AL.: "Long-Acting HIV-1 Fusion Inhibitory Peptides and their Mechanisms of Action", VIRUSES, vol. 11, no. 811, 2 September 2019 (2019-09-02), pages 1 - 13, XP055864385
LI MINGLI, CHENG SHUIHONG, DING YIBO, WANG CHEN, FENG YONG, WANG WENZHAO, MA LIYING, LI XUEBING: "Polyethylene Glycol 40-Modified Peptide with High Therapeutic Efficacy in Simian-Human Immunodeficiency Virus-Acutely Infected Rhesus Monkeys", JOURNAL OF VIROLOGY, vol. 94, no. 14, 1 July 2020 (2020-07-01), US , XP055864389, ISSN: 0022-538X, DOI: 10.1128/JVI.00386-20
WANG, C. ET AL.: "Long-Acting HIV-1 Fusion Inhibitory Peptides and their Mechanisms of Action", VIRUSES, vol. 11, no. 811, 2 September 2019 (2019-09-02), pages 1 - 13, XP055864385
LI MINGLI, CHENG SHUIHONG, DING YIBO, WANG CHEN, FENG YONG, WANG WENZHAO, MA LIYING, LI XUEBING: "Polyethylene Glycol 40-Modified Peptide with High Therapeutic Efficacy in Simian-Human Immunodeficiency Virus-Acutely Infected Rhesus Monkeys", JOURNAL OF VIROLOGY, vol. 94, no. 14, 1 July 2020 (2020-07-01), US , XP055864389, ISSN: 0022-538X, DOI: 10.1128/JVI.00386-20
Attorney, Agent or Firm:
BEIJING SUNHOPE INTELLECTUAL PROPERTY LTD. (CN)
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