A less toxic heparin antagonist--low molecular weight protamine.
A new thirteen amino acid peptide, named low molecular weight protamine (LMWP), was obtained through the enzymatic digestion of native protamine. Both in vitro and in vivo results showed that LMWP fully maintained the heparin neutralization function of protamine but had much lower immunogenicity and antigenicity. Unlike protamine, neither LMWP nor LMWP/heparin complexes caused significant blood platelet aggregation in rats. These results suggest that LMWP can be used as a substitute for protamine for developing a new generation of nontoxic heparin antagonists.
Liang
J F
JF
College of Pharmacy, The University of Michigan, Ann Arbor, MI 48109-1065, USA. junfeng@umich.edu
Zhen
L
L
Chang
L-C
LC
Yang
V C
VC
D000818:Animals; D000941:Antigens / Q000276:immunology; D005260:Female; D006493:Heparin / Q000378:metabolism*; D006494:Heparin Antagonists / Q000009:adverse effects / Q000737:chemistry* / Q000276:immunology / Q000494:pharmacology*; D051379:Mice; D011479:Protamines / Q000009:adverse effects / Q000737:chemistry / Q000276:immunology / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013997:Time Factors
D000941:Antigens; D006494:Heparin Antagonists; D011479:Protamines; D006493:Heparin