PEGylation of cyanovirin-N, an entry inhibitor of HIV.
Adv Drug Deliv Rev
; 60(1): 79-87, 2008 Jan 03.
Article
in En
| MEDLINE
| ID: mdl-17884238
ABSTRACT
Cyanovirin-N (CV-N) is a potent inhibitor of human immunodeficiency virus and many other viruses. It has a high potential for use as a systemic compound to control viral load or in the development of microbicides to prevent primary viral infection. Due to its cyanobacterial origin it is likely to show the typical drawbacks associated with pharmaceutical use of foreign proteins such as short plasma half-life, proteolysis and immunogenicity. Several strategies were used to covalently bond poly(ethylene glycol) (PEGylate) to CV-N. Random PEGylation at lysine residues resulted in poor retention of antiviral activity. Many site-directed mutants were made to test site-specific PEGylation. One mutant, where glutamine 62 was replaced with cysteine (CV-N(Q62C)) and PEGylated with maleimide activated PEG, retained significant anti-HIV activity in vitro.
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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Polyethylene Glycols
/
Bacterial Proteins
/
Carrier Proteins
/
HIV Infections
/
Anti-HIV Agents
Limits:
Humans
Language:
En
Journal:
Adv Drug Deliv Rev
Journal subject:
FARMACOLOGIA
/
TERAPIA POR MEDICAMENTOS
Year:
2008
Document type:
Article
Affiliation country:
United States