216774-64-0Relevant articles and documents
NOVEL LUMINESCENT LANTHANIDE CHELATE REPORTERS, BIOSPECIFIC BINDING REACTANTS LABELLED WITH NOVEL LUMINESCENT LANTHANIDE CHELATE REPORTERS AND THEIR USE
-
Page/Page column 53; 67, (2021/01/23)
The present invention relates to novel luminescent lanthanide chelate reporters which are formed from two to three separate lanthanide chelate moieties covalently conjugated to each other to act as an unique labelling reactant, and which can be attached to a biospecific reactant and used in various assays.
Evaluation of the antibacterial and antibiofilm activities of novel CRAMP-vancomycin conjugates with diverse linkers
Mishra, Nigam M.,Briers, Yves,Lamberigts, Chris,Steenackers, Hans,Robijns, Stijn,Landuyt, Bart,Vanderleyden, Jos,Schoofs, Liliane,Lavigne, Rob,Luyten, Walter,Van Der Eycken, Erik V.
, p. 7477 - 7486 (2015/07/15)
We report the design, synthesis and antibacterial activity analysis of conjugates of vancomycin and cathelicidin-related antimicrobial peptides (CRAMP). Vancomycin inhibits the nascent peptidoglycan synthesis and is highly active against Gram-positive bacteria, whereas Gram-negative bacteria are generally insensitive due to a protective outer membrane. CRAMP is known to translocate across the Gram-negative outer membrane by a self-promoted uptake mechanism. Vancomycin-CRAMP conjugates were synthesized using click chemistry with diverse hydrophilic and hydrophobic linkers, with CRAMP functioning as a carrier peptide for the transfer of vancomycin through the outer membrane. Small hydrophobic linkers with an aromatic group result in the most active conjugates against planktonic Gram-negative bacteria, while maintaining the high activity of vancomycin against Gram-positive bacteria. These conjugates thus show a broad-spectrum activity, which is absent in CRAMP or vancomycin alone, and which is strongly improved compared to an equimolar mixture of CRAMP and vancomycin. In addition, these conjugates also show a strong inhibitory activity against S. Typhimurium biofilm formation.
Evaluation of the antibacterial and antibiofilm activities of novel CRAMP-vancomycin conjugates with diverse linkers
Mishra, Nigam M.,Briers, Yves,Lamberigts, Chris,Steenackers, Hans,Robijns, Stijn,Landuyt, Bart,Vanderleyden, Jos,Schoofs, Liliane,Lavigne, Rob,Luyten, Walter,Van Der Eycken, Erik V.
supporting information, p. 7477 - 7486 (2015/11/27)
We report the design, synthesis and antibacterial activity analysis of conjugates of vancomycin and cathelicidin-related antimicrobial peptides (CRAMP). Vancomycin inhibits the nascent peptidoglycan synthesis and is highly active against Gram-positive bacteria, whereas Gram-negative bacteria are generally insensitive due to a protective outer membrane. CRAMP is known to translocate across the Gram-negative outer membrane by a self-promoted uptake mechanism. Vancomycin-CRAMP conjugates were synthesized using click chemistry with diverse hydrophilic and hydrophobic linkers, with CRAMP functioning as a carrier peptide for the transfer of vancomycin through the outer membrane. Small hydrophobic linkers with an aromatic group result in the most active conjugates against planktonic Gram-negative bacteria, while maintaining the high activity of vancomycin against Gram-positive bacteria. These conjugates thus show a broad-spectrum activity, which is absent in CRAMP or vancomycin alone, and which is strongly improved compared to an equimolar mixture of CRAMP and vancomycin. In addition, these conjugates also show a strong inhibitory activity against S. Typhimurium biofilm formation.
