kyuman Oh

L'invention concerne des conjugues proteine-principe actif ayant un motif acide amine qui peut etre reconnu par une isoprenoide transferase. L'invention concerne egalement des compositions contenant les conjugues, ainsi que des procedes de fabrication des conjugues et des compositions. L'invention concerne en outre des procedes d'utilisation des conjugues pour administrer le principe actif a une cellule cible, ainsi que des procedes d'utilisation des conjugues pour traiter un sujet en ayant besoin (par exemple un sujet ayant besoin du principe actif).

Klebsiella pneumoniae is one of the important clinical organisms that causes various infectious diseases, including urinary tract infections, necrotizing pneumonia, and surgical wound infections. The increase in the incidence of multidrug-resistance K. pneumoniae is a major problem in public healthcare. Therefore, a novel antibacterial agent is needed to treat this pathogen. Here, we studied the in vitro and in vivo activities of a novel antibiotic LCB10-0200, a siderophore-conjugated cephalosporin, against clinical isolates of K. pneumoniae. In vitro susceptibility study found that LCB10-0200 showed potent antibacterial activity against K. pneumoniae, including the beta-lactamase producing strains. The in vivo efficacy of LCB10-0200 was examined in three different mouse infection models, including systemic, thigh, and urinary tract infections. LCB10-0200 showed more potent in vivo activity than ceftazidime in the three in vivo models against the drug-susceptible and drug-resistant ...

Infections caused by multidrug-resistant bacteria, including Pseudomonas aeruginosa, are threating public health worldwide. Therefore, a novel antibacterial agent is needed for treating these infections. Here, we investigated the in vitro and in vivo activities of a novel siderophore-conjugated cephalosporin LCB10-0200 against the clinical isolates of Gram-negative baeria, including multidrug-resistant P. aeruginosa. In vitro susceptibility to LCB10-0200 was assessed by performing a two-fold agar dilution method, as described by Clinical and Laboratory Standards Institute. LCB10-0200 showed the most potent antibacterial activity against P. aeruginosa clinical isolates, including beta-lactamase-producing strains. Moreover, LCB10-0200 showed better antibacterial activity against recently isolated clinical isolates than its comparators, except colistin. The in vivo activity of LCB10-0200 was examined using four mouse models of systemic, thigh, respiratory tract, and urinary tract infec...

LCB01-0648 is a novel oxazolidinone compound that shows potent antibacterial activities against most Gram-positive cocci, including the multi-drug resistant Staphylococcus aureus. In this study, in vivo activity of LCB01-0699, a LCB01-0648 prodrug, against S. aureus was evaluated in comparison with that of Linezolid. The results of the systemic infection study demonstrated that LCB01-0699 was more potent than Linezolid against methicillin-susceptible and -resistant S. aureus strains. The in vivo efficacy of LCB01-0699 against methicillin-susceptible and -resistant S. aureus strains in a skin infection model showed more potent activity than Linezolid. LCB01-0699 shows potent in vivo activity against methicillin-susceptible and -resistant S. aureus strains, suggesting that LCB01-0699 would be a novel candidate for the treatment of these infectious diseases caused by S. aureus.