Fertilin beta peptidic liposomes inhibit fertilization by steric blockage.
Liposomes presenting fertilinbeta peptides are inhibitors of mouse in vitro fertilization. We undertook a study of the relationship between IC(50) and mole fraction of fertilinbeta in the liposome, and the size dependence of inhibition of fertilization to understand the mechanism of their inhibition. Our results indicate that a small number of multivalent contacts are required for efficient attachment of inhibitor to receptor on the target membrane, and that, as designed, the liposomes target the egg membrane but not the sperm membrane. The size dependence of the liposome inhibition demonstrates that the liposomes physically block access of the sperm to the egg membrane thereby preventing sperm binding to all egg receptors not just the fertilinbeta receptor.
Department of Chemistry, State University of New York, Stony Brook, NY 11794-3400, USA.
Samidha
S
Konkar
Suparna
S
Gupta
Nicole S
NS
Sampson
D051722:ADAM Proteins; D000818:Animals; D005260:Female; D000072196:Fertilins; D005307:Fertilization in Vitro / Q000379:methods; D008081:Liposomes; D008297:Male; D008562:Membrane Glycoproteins / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D008666:Metalloendopeptidases / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D051379:Mice; D010455:Peptides / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D013084:Sperm-Ovum Interactions / Q000187:drug effects* / Q000502:physiology
D008081:Liposomes; D008562:Membrane Glycoproteins; D010455:Peptides; D051722:ADAM Proteins; C000606458:Adam2 protein, mouse; D000072196:Fertilins; D008666:Metalloendopeptidases