Identification from a positional scanning peptoid library of in vivo active compounds that neutralize bacterial endotoxins.
Two peptoids that neutralize the Gram-negative lipopolysaccharide (LPS) were identified from the screening of a positional scanning library. The evaluation of the in vivo activity of these compounds in an endoxemia murine model is also reported. These peptoids did not neutralize lipid A, i.e., the hydrophobic toxic component of LPS. This fact suggests that they do not have access to the micellar core and that they should bind to the hydrophilic carbohydrate portion of LPS.
Mora
Puig
P
Departament de Bioquímica i Biologia Molecular, Universitat de València, E-46100 Burjassot, Spain.
Masip
Isabel
I
Cortés
Nuria
N
Marquina
Regina
R
Merino
Ramón
R
Merino
Jesús
J
Carbonell
Teresa
T
Mingarro
Ismael
I
Messeguer
Angel
A
Pérez-Payá
Enrique
E
D000818:Animals; D016208:Databases, Factual; D006090:Gram-Negative Bacteria / Q000737:chemistry; D008050:Lipid A / Q000737:chemistry; D008070:Lipopolysaccharides / Q000037:antagonists & inhibitors* / Q000737:chemistry; D051379:Mice; D034444:Peptoids / Q000737:chemistry* / Q000494:pharmacology; D014409:Tumor Necrosis Factor-alpha / Q000037:antagonists & inhibitors / Q000378:metabolism
D008050:Lipid A; D008070:Lipopolysaccharides; D034444:Peptoids; D014409:Tumor Necrosis Factor-alpha