Dimyristoylated peptides incorporated into liposomes are polyvalent fertilin beta mimics.
[structure: see text]. Fertilin beta is an integral membrane sperm protein that is involved in sperm binding to the egg plasma membrane. We synthesized a dimyristoylated fertilin beta peptide and incorporated it into POPC liposomes at 1 mol %. The concentration of fertilin beta peptide required for 50% inhibition is reduced 100-fold to 5.2 +/- 1.6 microM relative to a monomeric control. Moreover, in contrast to the inhibition observed with monomeric peptides, we obtain complete inhibition with the peptidic liposomes.
Gupta
S
S
Department of Chemistry, State University of New York, Stony Brook, New York 11794-3400, USA.
Sampson
N S
NS
D051722:ADAM Proteins; D000818:Animals; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry; D000072196:Fertilins; D006801:Humans; D020128:Inhibitory Concentration 50; D008081:Liposomes / Q000378:metabolism; D008562:Membrane Glycoproteins / Q000037:antagonists & inhibitors* / Q000737:chemistry; D008666:Metalloendopeptidases / Q000037:antagonists & inhibitors* / Q000737:chemistry; D018716:Molecular Mimicry; D009227:Myristic Acids / Q000737:chemistry; D010455:Peptides / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D013084:Sperm-Ovum Interactions / Q000187:drug effects
D004791:Enzyme Inhibitors; D008081:Liposomes; D008562:Membrane Glycoproteins; D009227:Myristic Acids; D010455:Peptides; D051722:ADAM Proteins; C000606454:ADAM2 protein, human; D000072196:Fertilins; D008666:Metalloendopeptidases